120 articles for thisTarget
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Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists.
Peking Union Medical College
Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.
Peking Union Medical College
A Novel Parkinson's Disease Drug Candidate with Potent Anti-neuroinflammatory Effects through the Src Signaling Pathway.
Peking Union Medical College
Polycyclic Polyprenylated Acylphloroglucinol Congeners from Hypericum scabrum.
Peking Union Medical College
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.
Peking Union Medical College
Development of hydroxy-based sphingosine kinase inhibitors and anti-inflammation in dextran sodium sulfate induced colitis in mice.
Peking Union Medical College
Synthesis, identification, and biological activity of metabolites of two novel selective S1P1 agonists.
Peking Union Medical College
Discovery of novel 5-fluoro-N(2),N(4)-diphenylpyrimidine-2,4-diamines as potent inhibitors against CDK2 and CDK9.
Peking Union Medical College
Cembranoids from the Gum Resin of Boswellia carterii as Potential Antiulcerative Colitis Agents.
Peking Union Medical College
Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
Peking Union Medical College
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.
Peking Union Medical College
Identification of 3,5,6-substituted indolin-2-one's inhibitors of Aurora B by development of a luminescent kinase assay.
Peking Union Medical College
Discovery of novel indole derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.
Peking Union Medical College
Discovery of novel non-covalent inhibitors selective to theß5-subunit of the human 20S proteasome.
Peking Union Medical College
Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands.
Peking Union Medical College
Discovery of oxazole and triazole derivatives as potent and selective S1P(1) agonists through pharmacophore-guided design.
Peking Union Medical College
Design, synthesis and in vitro and in vivo antitumour activity of 3-benzylideneindolin-2-one derivatives, a novel class of small-molecule inhibitors of the MDM2-p53 interaction.
Peking Union Medical College
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.
Peking Union Medical College
Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPAR¿.
Peking Union Medical College
Design, synthesis and biological evaluation of 7-nitro-1H-indole-2-carboxylic acid derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase.
Peking Union Medical College
Discovery of novel PTP1B inhibitors via pharmacophore-oriented scaffold hopping from Ertiprotafib.
Peking Union Medical College
Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors.
Peking Union Medical College
Antidepressant abietane diterpenoids from Chinese eaglewood.
Peking Union Medical College
A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling.
Peking Union Medical College
Synthesis, biological evaluation, and molecular modeling of glycyrrhizin derivatives as potent high-mobility group box-1 inhibitors with anti-heart-failure activity in vivo.
Peking Union Medical College
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening.
Peking Union Medical College
Structure and bioassay of triterpenoids and steroids isolated from Sinocalamus affinis.
Peking Union Medical College
Synthesis and biological evaluation of novel human Pin1 inhibitors with benzophenone skeleton.
Peking Union Medical College
3D QSAR and docking study of flavone derivatives as potent inhibitors of influenza H1N1 virus neuraminidase.
Peking Union Medical College
A discovery of novel Mycobacterium tuberculosis pantothenate synthetase inhibitors based on the molecular mechanism of actinomycin D inhibition.
Peking Union Medical College
Synthesis and biological evaluation of novel quinazoline-derived human Pin1 inhibitors.
Peking Union Medical College
Discovery and optimization of novel 3-piperazinylcoumarin antagonist of chemokine-like factor 1 with oral antiasthma activity in mice.
Peking Union Medical College
Identification of peptide substrate and small molecule inhibitors of testis-specific serine/threonine kinase1 (TSSK1) by the developed assays.
Peking Union Medical College
Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.
Peking Union Medical College
Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity.
Peking Union Medical College
Structure based design and evaluation of benzoheterocycle derivatives as potential dual HIV-1 protease and reverse transcriptase inhibitors.
Peking Union Medical College
Evolution and Discovery of Matrine Derivatives as a New Class of Anti-Hepatic Fibrosis Agents Targeting Ewing Sarcoma Breakpoint Region 1 (EWSR1).
Peking Union Medical College
Development, validation, and evaluation of a deep learning model to screen cyclin-dependent kinase 12 inhibitors in cancers.
Peking Union Medical College
Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis.
Peking Union Medical College
Structure-activity relationship study of amidobenzimidazole derivatives as stimulator of interferon genes (STING) agonists.
Peking Union Medical College
Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius.
Peking Union Medical College
Synthesis and antineoplastic activity of ethylene glycol phenyl aminoethyl ether derivatives as FOXM1 inhibitors.
Peking Union Medical College
Current approaches and strategies to identify Hedgehog signaling pathway inhibitors for cancer therapy.
Peking Union Medical College
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
Peking Union Medical College
Identification of N, C-capped di- and tripeptides as selective immunoproteasome inhibitors.
Peking Union Medical College
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism.
Peking Union Medical College
Design, synthesis and biological evaluation of protease inhibitors containing morpholine cores with remarkable potency against both HIV-1 subtypes B and C.
Peking Union Medical College
Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury.
Peking Union Medical College
The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates.
Peking Union Medical College
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.
Peking Union Medical College
A kind of HIV-1 protease inhibitors containing phenols with antiviral activity against DRV-resistant variants.
Peking Union Medical College
Discovery of 3, 6-disubstituted isobenzofuran-1(3H)-ones as novel inhibitors of monoamine oxidases.
Peking Union Medical College
Identification of novel xanthine oxidase inhibitors via virtual screening with enhanced characterization of molybdopterin binding groups.
Peking Union Medical College
Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.
Peking Union Medical College
Discovery and radiosensitization research of ursolic acid derivatives as SENP1 inhibitors.
Peking Union Medical College
Discovery of Natural Ursane-type SENP1 Inhibitors and the Platinum Resistance Reversal Activity Against Human Ovarian Cancer Cells: A Structure-Activity Relationship Study.
Peking Union Medical College
Bioevaluation of a dual PI3K/HDAC inhibitor for the treatment of diffuse large B-cell lymphoma.
Peking Union Medical College
Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors.
Peking Union Medical College
Design, synthesis, and structure-activity relationship of PD-1/PD-L1 inhibitors with a benzo[d]isoxazole scaffold.
Peking Union Medical College
Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy.
Peking Union Medical College
Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants.
Peking Union Medical College
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.
Peking Union Medical College
Design, synthesis and biological evaluation of exiguamine A analogues as IDO1 inhibitors.
Peking Union Medical College
Identification of 3, 4-disubstituted pyridine derivatives as novel CDK8 inhibitors.
Peking Union Medical College
Discovery and optimization of 2-((1H-indol-3-yl)thio)-N-benzyl-acetamides as novel SARS-CoV-2 RdRp inhibitors.
Peking Union Medical College
Design, synthesis, and pharmacological evaluation of sinomenine derivatives on rings A and C: Novel compounds screening for aplastic anemia targeting on cytotoxic T lymphocyte.
Peking Union Medical College
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.
Peking Union Medical College
Design, synthesis, evaluation, and SAR of 4-phenylindoline derivatives, a novel class of small-molecule inhibitors of the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) interaction.
Peking Union Medical College
Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold.
Peking Union Medical College
Berberine Directly Targets the NEK7 Protein to Block the NEK7-NLRP3 Interaction and Exert Anti-inflammatory Activity.
Peking Union Medical College
Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
Peking Union Medical College
Identification of benzofused five-membered sultams, potent dual NOD1/NOD2 antagonists in vitro and in vivo.
Peking Union Medical College
Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.
Peking Union Medical College
Design and Synthesis of Cajanine Analogues against Hepatitis C Virus through Down-Regulating Host Chondroitin Sulfate N-Acetylgalactosaminyltransferase 1.
Peking Union Medical College
Synthesis and Pin1 inhibitory activity of thiazole derivatives.
Peking Union Medical College
Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy.
Peking Union Medical College
Bioactivity-Guided Discovery of Human Carboxylesterase Inhibitors from the Roots of
Peking Union Medical College
Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors.
Peking Union Medical College
Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors.
Peking Union Medical College
Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
Peking Union Medical College
Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells.
Peking Union Medical College
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.
Peking Union Medical College
Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors.
Peking Union Medical College
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite.
Peking Union Medical College
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants.
Peking Union Medical College
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.
Peking Union Medical College
Yanhusanines A-F, Isoquinoline-Derived Alkaloid Enantiomers from
Peking Union Medical College
Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.
Peking Union Medical College
Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
Peking Union Medical College
C15-methoxyphenylated 18-deoxy-herbimycin A analogues, their in vitro anticancer activity and heat shock protein 90 binding affinity.
Peking Union Medical College
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
Peking Union Medical College
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
Peking Union Medical College
Design, synthesis and biological evaluation of novel HIV-1 protease inhibitors with pentacyclic triterpenoids as P2-ligands.
Peking Union Medical College
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
Peking Union Medical College
Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors.
Peking Union Medical College
Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands.
Peking Union Medical College
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.
Peking Union Medical College
Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV-1 variants.
Peking Union Medical College
Discovery of novel indirubin-3'-monoxime derivatives as potent inhibitors against CDK2 and CDK9.
Peking Union Medical College
Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists.
Peking Union Medical College
Structure-activity relationship of flavonoids as influenza virus neuraminidase inhibitors and their in vitro anti-viral activities.
Peking Union Medical College
Design, synthesis and in vitro anti-Zika virus evaluation of novel Sinefungin derivatives.
Peking Union Medical College
Small-molecule compounds targeting the STAT3 DNA-binding domain suppress survival of cisplatin-resistant human ovarian cancer cells by inducing apoptosis.
Peking Union Medical College
Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings.
Peking Union Medical College
Synthesis and biological evaluation of pyrimidine derivatives as novel human Pin1 inhibitors.
Peking Union Medical College
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.
Peking Union Medical College
Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids.
Peking Union Medical College
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.
Peking Union Medical College
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.
Peking Union Medical College
Bysspectin A, an unusual octaketide dimer and the precursor derivatives from the endophytic fungus Byssochlamys spectabilis IMM0002 and their biological activities.
Peking Union Medical College
Design and synthesis of potent HIV-1 protease inhibitors with (S)-tetrahydrofuran-tertiary amine-acetamide as P2-ligand: Structure-activity studies and biological evaluation.
Peking Union Medical College
Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors.
Peking Union Medical College
Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in vivo anti-tumor activity.
Peking Union Medical College
Discovery of 1,4-Benzodiazepine-2,5-dione (BZD) Derivatives as Dual Nucleotide Binding Oligomerization Domain Containing 1/2 (NOD1/NOD2) Antagonists Sensitizing Paclitaxel (PTX) To Suppress Lewis Lung Carcinoma (LLC) Growth in Vivo.
Peking Union Medical College
