369 articles for thisTarget
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Design, synthesis and biological evaluation of thienopyrimidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.
Chinese Academy of Sciences
Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors.
Chinese Academy of Sciences
2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.
Chinese Academy of Sciences
A novel class ofa-glucosidase and HMG-CoA reductase inhibitors from Ganoderma leucocontextum and the anti-diabetic properties of ganomycin I in KK-A
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as Selectivea
Chinese Academy of Sciences
Eucarobustols A-I, Conjugates of Sesquiterpenoids and Acylphloroglucinols from Eucalyptus robusta.
Chinese Academy of Sciences
An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core.
Chinese Academy of Sciences
The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biological evaluation.
Chinese Academy of Sciences
The design strategy of selective PTP1B inhibitors over TCPTP.
Chinese Academy of Sciences
Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs).
Chinese Academy of Sciences
Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors as a Potential Therapy for Diabetic Macular Edema.
Chinese Academy of Sciences
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.
Chinese Academy of Sciences
Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors.
Chinese Academy of Sciences
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.
Chinese Academy of Sciences
Discovery of a Novel Series of Imidazo[1,2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors.
Chinese Academy of Sciences
Inhibitory Effects of Highly Oxygenated Lanostane Derivatives from the Fungus Ganoderma lucidum on P-Glycoprotein anda-Glucosidase.
Chinese Academy of Sciences
Lanostane Triterpenes from the Tibetan Medicinal Mushroom Ganoderma leucocontextum and Their Inhibitory Effects on HMG-CoA Reductase anda-Glucosidase.
Chinese Academy of Sciences
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.
Chinese Academy of Sciences
Polycyclic Polyprenylated Acylphloroglucinol Congeners Possessing Diverse Structures from Hypericum henryi.
Chinese Academy of Sciences
Mechanistic studies on the absorption and disposition of scutellarin in humans: selective OATP2B1-mediated hepatic uptake is a likely key determinant for its unique pharmacokinetic characteristics.
Chinese Academy of Sciences
Compounds from the insect Blaps japanensis with COX-1 and COX-2 inhibitory activities.
Chinese Academy of Sciences
Discovery of Intestinal Targeted TGR5 Agonists for the Treatment of Type 2 Diabetes.
Chinese Academy of Sciences
Hupehenols A-E, selective 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD1) inhibitors from Viburnum hupehense.
Chinese Academy of Sciences
Small molecule discoidin domain receptor kinase inhibitors and potential medical applications.
Chinese Academy of Sciences
Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis.
Chinese Academy of Sciences
Glycosylated enfuvirtide: a long-lasting glycopeptide with potent anti-HIV activity.
Chinese Academy of Sciences
Design and synthesis of novel 1,2-dithiolan-4-yl benzoate derivatives as PTP1B inhibitors.
Chinese Academy of Sciences
Novel fatty acid binding protein 4 (FABP4) inhibitors: virtual screening, synthesis and crystal structure determination.
Chinese Academy of Sciences
Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: synthesis and in vitro biological evaluation. Part 1.
Chinese Academy of Sciences
4-Quinolone-3-carboxylic acids as cell-permeable inhibitors of protein tyrosine phosphatase 1B.
Chinese Academy of Sciences
Structure-activity relationship and interaction studies of new SIRT1 inhibitors with the scaffold of 3-(furan-2-yl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole.
Chinese Academy of Sciences
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.
Chinese Academy of Sciences
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
Chinese Academy of Sciences
(R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: design, synthesis, biological evaluation, and molecular modeling.
Chinese Academy of Sciences
Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90.
Chinese Academy of Sciences
Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.
Chinese Academy of Sciences
Identifying novel selective non-nucleoside DNA methyltransferase 1 inhibitors through docking-based virtual screening.
Chinese Academy of Sciences
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors.
Chinese Academy of Sciences
Design, synthesis and evaluation of benzo[a]thieno[3,2-g]quinolizines as novel l-SPD derivatives possessing dopamine D1, D2 and serotonin 5-HT1A multiple action profiles.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class I and IIb histone deacetylase inhibitors.
Chinese Academy of Sciences
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.
Chinese Academy of Sciences
Discovery of a New Series of Naphthamides as Potent VEGFR-2 Kinase Inhibitors.
Chinese Academy of Sciences
Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
Chinese Academy of Sciences
4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists.
Chinese Academy of Sciences
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Chinese Academy of Sciences
Identification of a new series of potent diphenol HSP90 inhibitors by fragment merging and structure-based optimization.
Chinese Academy of Sciences
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility.
Chinese Academy of Sciences
Benzophenone C-glucosides and gallotannins from mango tree stem bark with broad-spectrum anti-viral activity.
Chinese Academy of Sciences
Highly conjugated norditerpenoid and pyrroloquinoline alkaloids with potent PTP1B inhibitory activity from Nigella glandulifera.
Chinese Academy of Sciences
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.
Chinese Academy of Sciences
Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new ROR¿ inhibitors using virtual screening, synthesis and biological evaluation.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.
Chinese Academy of Sciences
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.
Chinese Academy of Sciences
Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel 2-ethyl-5-phenylthiazole-4-carboxamide derivatives as protein tyrosine phosphatase 1B inhibitors with improved cellular efficacy.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
Chinese Academy of Sciences
The first synthesis of natural disulfide bruguiesulfurol and biological evaluation of its derivatives as a novel scaffold for PTP1B inhibitors.
Chinese Academy of Sciences
Cembrane diterpenoids from the soft coral Sarcophyton trocheliophorum Marenzeller as a new class of PTP1B inhibitors.
Chinese Academy of Sciences
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11ß-HSD1 inhibitors: potential impact in diabetes.
Chinese Academy of Sciences
Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1.
Chinese Academy of Sciences
Discovery of novel bromophenol 3,4-dibromo-5-(2-bromo-3,4-dihydroxy-6-(isobutoxymethyl)benzyl)benzene-1,2-diol as protein tyrosine phosphatase 1B inhibitor and its anti-diabetic properties in C57BL/KsJ-db/db mice.
Chinese Academy of Sciences
Development of Novel Alkene Oxindole Derivatives As Orally Efficacious AMP-Activated Protein Kinase Activators.
Chinese Academy of Sciences
1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as orally bioavailable transcriptional function suppressors of estrogen-related receptora.
Chinese Academy of Sciences
Triazole derivatives: a series of Darapladib analogues as orally active Lp-PLA2 inhibitors.
Chinese Academy of Sciences
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.
Chinese Academy of Sciences
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.
Chinese Academy of Sciences
Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors.
Chinese Academy of Sciences
Design, synthesis and SAR of piperidyl-oxadiazoles as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Chinese Academy of Sciences
Asymmetric total synthesis and identification of tetrahydroprotoberberine derivatives as new antipsychotic agents possessing a dopamine D(1), D(2) and serotonin 5-HT(1A) multi-action profile.
Chinese Academy of Sciences
Discovery and mechanism study of SIRT1 activators that promote the deacetylation of fluorophore-labeled substrate.
Chinese Academy of Sciences
Synthesis, characterization, screening and docking analysis of 4-anilinoquinazoline derivatives as tyrosine kinase inhibitors.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.
Chinese Academy of Sciences
Solubility-driven optimization of (pyridin-3-yl) benzoxazinyl-oxazolidinones leading to a promising antibacterial agent.
Chinese Academy of Sciences
Bioactive polyhydroxylated steroids from the Hainan soft coral Sinularia depressa Tixier-Durivault.
Chinese Academy of Sciences
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
Chinese Academy of Sciences
Identification of benzofuran-3-yl(phenyl)methanones as novel SIRT1 inhibitors: binding mode, inhibitory mechanism and biological action.
Chinese Academy of Sciences
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Chinese Academy of Sciences
3D QSAR studies on ketoamides of human cathepsin K inhibitors based on two different alignment methods.
Chinese Academy of Sciences
3D-QSAR and docking studies of aminopyridine carboxamide inhibitors of c-Jun N-terminal kinase-1.
Chinese Academy of Sciences
Inhibitory mode of 1,5-diarylpyrazole derivatives against cyclooxygenase-2 and cyclooxygenase-1: molecular docking and 3D QSAR analyses.
Chinese Academy of Sciences
Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists.
Chinese Academy of Sciences
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)¿isoleucine(315) mutant.
Chinese Academy of Sciences
Potent HGF/c-Met axis inhibitors from Eucalyptus globulus: the coupling of phloroglucinol and sesquiterpenoid is essential for the activity.
Chinese Academy of Sciences
Rediocide A, an Insecticide, induces G-protein-coupled receptor desensitization via activation of conventional protein kinase C.
Chinese Academy of Sciences
Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.
Chinese Academy of Sciences
CCLab--a multi-objective genetic algorithm based combinatorial library design software and an application for histone deacetylase inhibitor design.
Chinese Academy of Sciences
Discovery and optimization of 2,4-diaminoquinazoline derivatives as a new class of potent dengue virus inhibitors.
Chinese Academy of Sciences
Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11ß-hydroxysteroid dehydrogenases.
Chinese Academy of Sciences
Identification of blapsins A and B as potent small-molecule 14-3-3 inhibitors from the insect Blaps japanensis.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine7¿°¿ methionine7¿° mutant.
Chinese Academy of Sciences
Synthesis and evaluation of piperidine urea derivatives as efficacious 11ß-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.
Chinese Academy of Sciences
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.
Chinese Academy of Sciences
Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators.
Chinese Academy of Sciences
Penicacids A-C, three new mycophenolic acid derivatives and immunosuppressive activities from the marine-derived fungus Penicillium sp. SOF07.
Chinese Academy of Sciences
Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
Chinese Academy of Sciences
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.
Chinese Academy of Sciences
Discovery of novel purine derivatives with potent and selective inhibitory activity against c-Src tyrosine kinase.
Chinese Academy of Sciences
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.
Chinese Academy of Sciences
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
Chinese Academy of Sciences
Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.
Chinese Academy of Sciences
Novel thiophene derivatives as PTP1B inhibitors with selectivity and cellular activity.
Chinese Academy of Sciences
'Click' D(1) receptor agonists with a 5-HT(1A) receptor pharmacophore producing D(2) receptor activity.
Chinese Academy of Sciences
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Chinese Academy of Sciences
Synthesis and opioid receptor activity of indolopropellanes.
Chinese Academy of Sciences
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.
Chinese Academy of Sciences
Cucurbitane-type triterpenoids from the stems of Cucumis melo.
Chinese Academy of Sciences
Discovery of thioether-bridged cyclic pentapeptides binding to Grb2-SH2 domain with high affinity.
Chinese Academy of Sciences
Synthesis and utilization of chiral alpha-methylated alpha-amino acids with a carboxyalkyl side chain in the design of novel Grb2-SH2 peptide inhibitors free of phosphotyrosine.
Chinese Academy of Sciences
Simultaneous identification of multiple receptors of natural product using an optimized cDNA phage display cloning.
Chinese Academy of Sciences
Crystal structures of Saccharomyces cerevisiae N-myristoyltransferase with bound myristoyl-CoA and inhibitors reveal the functional roles of the N-terminal region.
Chinese Academy of Sciences
Alkaloids from stems and leaves of Stemona japonica and their insecticidal activities.
Chinese Academy of Sciences
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.
Chinese Academy of Sciences
Discovery of Helicobacter pylori shikimate kinase inhibitors: bioassay and molecular modeling.
Chinese Academy of Sciences
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.
Chinese Academy of Sciences
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.
Chinese Academy of Sciences
Discovery and structural modification of inhibitors of methionine aminopeptidases from Escherichia coli and Saccharomyces cerevisiae.
Chinese Academy of Sciences
N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors.
Chinese Academy of Sciences
Synthesis and acetylcholinesterase inhibitory activity of (+/-)-14-fluorohuperzine A.
Chinese Academy of Sciences
A 3D-QSAR study on ginkgolides and their analogues with comparative molecular field analysis.
Chinese Academy of Sciences
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
Chinese Academy of Sciences
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.
Chinese Academy of Sciences
C-aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Chinese Academy of Sciences
Structure-activity study on a series ofa-glutamic acid scaffold based compounds as new ADAMTS inhibitors.
Chinese Academy of Sciences
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.
Chinese Academy of Sciences
New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein.
Chinese Academy of Sciences
Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase.
Chinese Academy of Sciences
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.
Chinese Academy of Sciences
Further SAR study on 11-O-substituted aporphine analogues: identification of highly potent dopamine D3 receptor ligands.
Chinese Academy of Sciences
Synthesis, modification, and evaluation of (R)-de-O-methyllasiodiplodin and analogs as nonsteroidal antagonists of mineralocorticoid receptor.
Chinese Academy of Sciences
Fatty acid synthase inhibitors of phenolic constituents isolated from Garcinia mangostana.
Chinese Academy of Sciences
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.
Chinese Academy of Sciences
ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Design, synthesis, and pharmacological evaluation of N-(4-mono and 4,5-disubstituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl)propanamides as glucokinase activators.
Chinese Academy of Sciences
Dammaranes from Gynostemma pentaphyllum and synthesis of their derivatives as inhibitors of protein tyrosine phosphatase 1B.
Chinese Academy of Sciences
Discovery of highly selective inhibitors of human fatty acid binding protein 4 (FABP4) by virtual screening.
Chinese Academy of Sciences
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Chinese Academy of Sciences
Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B.
Chinese Academy of Sciences
A series of alpha-heterocyclic carboxaldehyde thiosemicarbazones inhibit topoisomerase IIalpha catalytic activity.
Chinese Academy of Sciences
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.
Chinese Academy of Sciences
Chemical constituents from the aerial parts of Artemisia minor.
Chinese Academy of Sciences
Discovery and SAR of thiazolidine-2,4-dione analogues as insulin-like growth factor-1 receptor (IGF-1R) inhibitors via hierarchical virtual screening.
Chinese Academy of Sciences
Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Chinese Academy of Sciences
Pyrrolidinoindoline alkaloids from Selaginella moellendorfii.
Chinese Academy of Sciences
Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors.
Chinese Academy of Sciences
Halogen bonding--a novel interaction for rational drug design?
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase.
Chinese Academy of Sciences
Design, synthesis, and evaluation of potent, nonpeptidic mimetics of second mitochondria-derived activator of caspases.
Chinese Academy of Sciences
A novel sesquiterpene quinone from Hainan sponge Dysidea villosa.
Chinese Academy of Sciences
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring.
Chinese Academy of Sciences
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.
Chinese Academy of Sciences
N-Propylnoraporphin-11-O-yl carboxylic esters as potent dopamine D(2) and serotonin 5-HT(1A) receptor dual ligands.
Chinese Academy of Sciences
Oleanolic acid and its derivatives: new inhibitor of protein tyrosine phosphatase 1B with cellular activities.
Chinese Academy of Sciences
Illudalic acid as a potential LAR inhibitor: synthesis, SAR, and preliminary studies on the mechanism of action.
Chinese Academy of Sciences
Synthesis and pharmacological investigation of novel 2-aminothiazole-privileged aporphines.
Chinese Academy of Sciences
Selective cyclooxygenase-2 inhibitors from Calophyllum membranaceum.
Chinese Academy of Sciences
Bioactive abietane and seco-abietane diterpenoids from Salvia prionitis.
Chinese Academy of Sciences
Anti-Helicobacter pylori and thrombin inhibitory components from Chinese dragon's blood, Dracaena cochinchinensis.
Chinese Academy of Sciences
Microascones, Decahydrofluorene-Class Alkaloids from the Marine-Derived Fungus
Chinese Academy of Sciences
Aza analogues of equol: novel ligands for estrogen receptor beta.
Chinese Academy of Sciences
Selective Covalent Targeting of Pyruvate Kinase M2 Using Arsenous Warheads.
Chinese Academy of Sciences
Structure-based discovery of IHMT-IDH1-053 as a potent irreversible IDH1 mutant selective inhibitor.
Chinese Academy of Sciences
Discovery of potential novel TRPC5 inhibitors by virtual screening and bioassay.
Chinese Academy of Sciences
Synthesis and pharmacological evaluation of 6,7-indolo/thiazolo-morphinans--further SAR of levorphanol.
Chinese Academy of Sciences
Discovery of Pyrrolo[2,3-d]pyrimidine derivatives as potent and selective colony stimulating factor 1 receptor kinase inhibitors.
Chinese Academy of Sciences
Indole derivatives as potent inhibitors of 5-lipoxygenase: design, synthesis, biological evaluation, and molecular modeling.
Chinese Academy of Sciences
Nanomolar β-glucosidase and β-galactosidase inhibition by enantiomeric α-1-C-alkyl-1,4-dideoxy-1,4-imino-arabinitol derivatives.
Chinese Academy of Sciences
Quinoxalinylurea derivatives as a novel class of JSP-1 inhibitors.
Chinese Academy of Sciences
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1
Chinese Academy of Sciences
Design, synthesis, and anti-inflammatory activity characterization of novel brain-permeable HDAC6 inhibitors.
Chinese Academy of Sciences
Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization.
Chinese Academy of Sciences
Discovery of a First-in-Class Degrader for the Lipid Kinase PIKfyve.
Chinese Academy of Sciences
Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.
Chinese Academy of Sciences
Synthesis and biological evaluation of glycosidase inhibitors: gem-difluoromethylenated nojirimycin analogues.
Chinese Academy of Sciences
Chemical synthesis and pharmacological properties of heparin pentasaccharide analogues.
Chinese Academy of Sciences
Two novel aromatic valerenane-type sesquiterpenes from the Chinese green alga Caulerpa taxifolia.
Chinese Academy of Sciences
Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.
Chinese Academy of Sciences
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.
Chinese Academy of Sciences
Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes.
Chinese Academy of Sciences
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.
Chinese Academy of Sciences
trans, trans-2-C-Aryl-3,4-dihydroxypyrrolidines as potent and selective β-glucosidase inhibitors: Pharmacological chaperones for Gaucher disease.
Chinese Academy of Sciences
Novel indole alpha-methylene-gamma-lactones as potent inhibitors for AKT-mTOR signaling pathway kinases.
Chinese Academy of Sciences
Design, synthesis and glycosidase inhibition of C-4 branched LAB and DAB derivatives.
Chinese Academy of Sciences
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.
Chinese Academy of Sciences
Discovery of Phenolic Matrix Metalloproteinase Inhibitors by Peptide Microarray for Osteosarcoma Treatment.
Chinese Academy of Sciences
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.
Chinese Academy of Sciences
Synthesis of AC1903 analogs as potent transient receptor potential canonical channel 4/5 inhibitors and biological evaluation.
Chinese Academy of Sciences
Pyrrospirones K-Q, Decahydrofluorene-Class Alkaloids from the Marine-Derived Fungus
Chinese Academy of Sciences
Structure-Activity Relationships and Antileukemia Effects of the Tricyclic Benzoic Acid FTO Inhibitors.
Chinese Academy of Sciences
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.
Chinese Academy of Sciences
Benzothieno[3,2-b]indole derivatives as potent selective estrogen receptor modulators.
Chinese Academy of Sciences
Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.
Chinese Academy of Sciences
Natural products from mangrove sediments-derived microbes: Structural diversity, bioactivities, biosynthesis, and total synthesis.
Chinese Academy of Sciences
Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.
Chinese Academy of Sciences
Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 1: SAR studies on the determination of the key scaffold.
Chinese Academy of Sciences
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
Chinese Academy of Sciences
Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors.
Chinese Academy of Sciences
Computational and Structure-Based Development of High Potent Cell-Active Covalent Inhibitor Targeting the Peptidyl-Prolyl Isomerase NIMA-Interacting-1 (Pin1).
Chinese Academy of Sciences
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders.
Chinese Academy of Sciences
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.
Chinese Academy of Sciences
Identification of Novel Fused Heteroaromatics-Based MALT1 Inhibitors by High-Throughput Screening to Treat B Cell Lymphoma.
Chinese Academy of Sciences
Design, synthesis, and structure-activity relationships of haloenol lactones: site-directed and isozyme-selective glutathione S-transferase inhibitors.
Chinese Academy of Sciences
Rational Design and Development of Novel CDK9 Inhibitors for the Treatment of Acute Myeloid Leukemia.
Chinese Academy of Sciences
Identification of Betulinic Acid Derivatives as Potent TGR5 Agonists with Antidiabetic Effects via Humanized TGR5
Chinese Academy of Sciences
Structure-Activity Relationship Studies of Coumarin-like Diacid Derivatives as Human G Protein-Coupled Receptor-35 (hGPR35) Agonists and a Consequent New Design Principle.
Chinese Academy of Sciences
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
Chinese Academy of Sciences
Talaromynoids A-I, Highly Oxygenated Meroterpenoids from the Marine-Derived Fungus
Chinese Academy of Sciences
Synthesis and glycosidase inhibition of 5-C-alkyl-DNJ and 5-C-alkyl-l-ido-DNJ derivatives.
Chinese Academy of Sciences
5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma.
Chinese Academy of Sciences
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.
Chinese Academy of Sciences
Discovery of chiral N-2'-aryletheryl-1'-alkoxy-ethyl substituted arylisoquinolones with anti-inflammatory activity from the nucleophilic addition reactions of the thiophenols and oxazolinium.
Chinese Academy of Sciences
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.
Chinese Academy of Sciences
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment.
Chinese Academy of Sciences
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
Chinese Academy of Sciences
Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of
Chinese Academy of Sciences
Dihydro-β-agarofuran-Type Sesquiterpenoids from the Seeds of
Chinese Academy of Sciences
Structure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists.
Chinese Academy of Sciences
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.
Chinese Academy of Sciences
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.
Chinese Academy of Sciences
Discovery of Novel Bromophenol-Thiosemicarbazone Hybrids as Potent Selective Inhibitors of Poly(ADP-ribose) Polymerase-1 (PARP-1) for Use in Cancer.
Chinese Academy of Sciences
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.
Chinese Academy of Sciences
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.
Chinese Academy of Sciences
Molecular docking and 3D-QSAR studies on gag peptide analogue inhibitors interacting with human cyclophilin A.
Chinese Academy of Sciences
Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists.
Chinese Academy of Sciences
3-Pyrroline containing arylacetamides: a novel series of remarkably selective kappa-agonists.
Chinese Academy of Sciences
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.
Chinese Academy of Sciences
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.
Chinese Academy of Sciences
Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.
Chinese Academy of Sciences
The discovery, design and synthesis of potent agonists of adenylyl cyclase type 2 by virtual screening combining biological evaluation.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors.
Chinese Academy of Sciences
Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.
Chinese Academy of Sciences
Elucidating the inhibiting mode of AHPBA derivatives against HIV-1 protease and building predictive 3D-QSAR models.
Chinese Academy of Sciences
Ene-yne Hydroquinones from a Marine-derived Strain of the Fungus
Chinese Academy of Sciences
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.
Chinese Academy of Sciences
Discovery of Lipophilic Bisphosphonates That Target Bacterial Cell Wall and Quinone Biosynthesis.
Chinese Academy of Sciences
Limonoids and Triterpenoids as 11β-HSD1 Inhibitors from Walsura robusta.
Chinese Academy of Sciences
Synthesis and bioactivity of novel isoxazole chalcone derivatives on tyrosinase and melanin synthesis in murine B16 cells for the treatment of vitiligo.
Chinese Academy of Sciences
4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors.
Chinese Academy of Sciences
Structure-Based Design of Potent Nicotinamide Phosphoribosyltransferase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.
Chinese Academy of Sciences
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Chinese Academy of Sciences
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.
Chinese Academy of Sciences
Suppression of Tumor Growth and Metastases by Targeted Intervention in Urokinase Activity with Cyclic Peptides.
Chinese Academy of Sciences
Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel.
Chinese Academy of Sciences
Discovery and optimization of a series of 3-substituted indazole derivatives as multi-target kinase inhibitors for the treatment of lung squamous cell carcinoma.
Chinese Academy of Sciences
Fragment-based drug discovery of triazole inhibitors to block PDEδ-RAS protein-protein interaction.
Chinese Academy of Sciences
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.
Chinese Academy of Sciences
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.
Chinese Academy of Sciences
Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer.
Chinese Academy of Sciences
Discovery of a Potent and Selective NF-κB-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo.
Chinese Academy of Sciences
Toward a treatment of diabesity: In vitro and in vivo evaluation of uncharged bromophenol derivatives as a new series of PTP1B inhibitors.
Chinese Academy of Sciences
Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia.
Chinese Academy of Sciences
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Chinese Academy of Sciences
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Chinese Academy of Sciences
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor α.
Chinese Academy of Sciences
Polybenzyls from Gastrodia elata, their agonistic effects on melatonin receptors and structure-activity relationships.
Chinese Academy of Sciences
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer.
Chinese Academy of Sciences
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.
Chinese Academy of Sciences
1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.
Chinese Academy of Sciences
Discovery of Novel Retigabine Derivatives as Potent KCNQ4 and KCNQ5 Channel Agonists with Improved Specificity.
Chinese Academy of Sciences
Spirostaphylotrichin X from a Marine-Derived Fungus as an Anti-influenza Agent Targeting RNA Polymerase PB2.
Chinese Academy of Sciences
Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia.
Chinese Academy of Sciences
Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of 6-deoxy O-spiroketal C-arylglucosides as novel renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Chinese Academy of Sciences
Congenetic Hybrids Derived from Dearomatized Isoprenylated Acylphloroglucinol with Opposite Effects on Ca
Chinese Academy of Sciences
Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors.
Chinese Academy of Sciences
Selective Blockade of Neuronal BK (α + β4) Channels Preventing Epileptic Seizure.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.
Chinese Academy of Sciences
Rational design of 5-((1H-imidazol-1-yl)methyl)quinolin-8-ol derivatives as novel bromodomain-containing protein 4 inhibitors.
Chinese Academy of Sciences
Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.
Chinese Academy of Sciences
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an
Chinese Academy of Sciences
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors.
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria.
Chinese Academy of Sciences
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
Chinese Academy of Sciences
Exploring the Natural Piericidins as Anti-Renal Cell Carcinoma Agents Targeting Peroxiredoxin 1.
Chinese Academy of Sciences
Leucoflavonine, a new bioactive racemic flavoalkaloid from the leaves of Leucosceptrum canum.
Chinese Academy of Sciences
Discovery of Novel Disruptor of Silencing Telomeric 1-Like (DOT1L) Inhibitors using a Target-Specific Scoring Function for the (S)-Adenosyl-l-methionine (SAM)-Dependent Methyltransferase Family.
Chinese Academy of Sciences
1,9-seco-Bicyclic Polyprenylated Acylphloroglucinols from Hypericum uralum.
Chinese Academy of Sciences
Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.
Chinese Academy of Sciences
Discovery of a Negative Allosteric Modulator of GABAB Receptors.
Chinese Academy of Sciences
Structure-based optimization of the piperazino-containing 1,3-disubstituted ureas affording sub-nanomolar inhibitors of soluble epoxide hydrolase.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties.
Chinese Academy of Sciences
A novel necroptosis inhibitor-necrostatin-21 and its SAR study.
Chinese Academy of Sciences
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.
Chinese Academy of Sciences
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel pyrimidine, 3-cyanopyridine and m-amino-N-phenylbenzamide based monocyclic EGFR tyrosine kinase inhibitors.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
Chinese Academy of Sciences
Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.
Chinese Academy of Sciences
Structure-based design and synthesis of C-1- and C-4-modified analogs of zanamivir as neuraminidase inhibitors.
Chinese Academy of Sciences
Specific interactions between adenosine and streptavidin/avidin.
Chinese Academy of Sciences
Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties.
Chinese Academy of Sciences
Identification and synthesis of substituted pyrrolo[2,3-d]pyrimidines as novel firefly luciferase inhibitors.
Chinese Academy of Sciences
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.
Chinese Academy of Sciences
Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.
Chinese Academy of Sciences
Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.
Chinese Academy of Sciences
Design of HIV-1 integrase inhibitors targeting the catalytic domain as well as its interaction with LEDGF/p75: a scaffold hopping approach using salicylate and catechol groups.
Chinese Academy of Sciences
Synthesis and biological evaluation of 2,4,5-substituted pyrimidines as a new class of tubulin polymerization inhibitors.
Chinese Academy of Sciences
Nigranoic acid, a triterpenoid from Schisandra sphaerandra that inhibits HIV-1 reverse transcriptase.
Chinese Academy of Sciences
Efficient synthesis and utilization of phenyl-substituted heteroaromatic carboxylic acids as aryl diketo acid isosteres in the design of novel HIV-1 integrase inhibitors.
Chinese Academy of Sciences
Novel dimeric aryldiketo containing inhibitors of HIV-1 integrase: effects of the phenyl substituent and the linker orientation.
Chinese Academy of Sciences
Phenolic and triterpene glycosides from the stems of Ilex litseaefolia.
Chinese Academy of Sciences
Natural inhibitors targeting osteoclast-mediated bone resorption.
Chinese Academy of Sciences
Discovering potassium channel blockers from synthetic compound database by using structure-based virtual screening in conjunction with electrophysiological assay.
Chinese Academy of Sciences
Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening.
Chinese Academy of Sciences
Synthesis and biological evaluation of magnolol derivatives as melatonergic receptor agonists with potential use in depression.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.
Chinese Academy of Sciences
Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors.
Chinese Academy of Sciences
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
Chinese Academy of Sciences
Discovery of 4-(((4-(5-chloro-2-(((1s,4s)-4-((2-methoxyethyl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile (JSH-150) as a novel highly selective and potent CDK9 kinase inhibitor.
Chinese Academy of Sciences
Antibacterial Dimeric Acylphloroglucinols from Hypericum japonicum.
Chinese Academy of Sciences
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.
Chinese Academy of Sciences
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.
Chinese Academy of Sciences
Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia.
Chinese Academy of Sciences
A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities.
Chinese Academy of Sciences
Structurally Diverse Sesquiterpenoids from the Endangered Ornamental Plant Michelia shiluensis.
Chinese Academy of Sciences
Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces.
Chinese Academy of Sciences
Structure-based optimization of a series of selective BET inhibitors containing aniline or indoline groups.
Chinese Academy of Sciences
Precise structures of fucosylated glycosaminoglycan and its oligosaccharides as novel intrinsic factor Xase inhibitors.
Chinese Academy of Sciences
Design, Synthesis, and Biological Evaluation of the First c-Met/HDAC Inhibitors Based on Pyridazinone Derivatives.
Chinese Academy of Sciences
Identification of highly potent N-acylethanolamine acid amidase (NAAA) inhibitors: Optimization of the terminal phenyl moiety of oxazolidone derivatives.
Chinese Academy of Sciences
Malonylginsenosides with Potential Antidiabetic Activities from the Flower Buds of Panax ginseng.
Chinese Academy of Sciences
Discovery of (S)-2-amino-N-(5-(6-chloro-5-(3-methylphenylsulfonamido)pyridin-3-yl)-4-methylthiazol-2-yl)-3-methylbutanamide (CHMFL-PI3KD-317) as a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor.
Chinese Academy of Sciences
Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer.
Chinese Academy of Sciences
Design, synthesis and structure-activity relationship studies of GPR40 agonists containing amide linker.
Chinese Academy of Sciences
Design, synthesis and pharmacological evaluation of ALK and Hsp90 dual inhibitors bearing resorcinol and 2,4-diaminopyrimidine motifs.
Chinese Academy of Sciences
Piperidine Alkaloids with Diverse Skeletons from Anacyclus pyrethrum.
Chinese Academy of Sciences
Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of uncharged catechol derivatives as selective inhibitors of PTP1B.
Chinese Academy of Sciences
Discovery of a series of dihydroquinoxalin-2(1H)-ones as selective BET inhibitors from a dual PLK1-BRD4 inhibitor.
Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.
Chinese Academy of Sciences
Tricyclic Polyprenylated Acylphloroglucinols from St John's Wort, Hypericum perforatum.
Chinese Academy of Sciences
Synthesis of selective 11β-HSD1 inhibitors based on dammarane scaffold.
Chinese Academy of Sciences
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.
Chinese Academy of Sciences
Allosteric Inhibitors of SHP2 with Therapeutic Potential for Cancer Treatment.
Chinese Academy of Sciences
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase Mutants in FLT3-ITD Positive AML.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles.
Chinese Academy of Sciences
Discovery and evaluation of the hybrid of bromophenol and saccharide as potent and selective protein tyrosine phosphatase 1B inhibitors.
Chinese Academy of Sciences
Synthesis and evaluation of sulfonamide derivatives as potent Human Uric Acid Transporter 1 (hURAT1) inhibitors.
Chinese Academy of Sciences
3-HYDROXY-5-(ISOXAZOL-5-YL) PYRIDINE FORMYLGLYCINE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
China Pharmaceutical University
Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro.
University of Zimbabwe
Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.
Sibia Neurosciences