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Discovery of furan carboxylate derivatives as novel inhibitors of ATP-citrate lyase via virtual high-throughput screening.

Harvard Medical School

Design and synthesis of emodin derivatives as novel inhibitors of ATP-citrate lyase.

Harvard Medical School

Asymmetric total synthesis of tetrahydroprotoberberine derivatives and evaluation of their binding affinities at dopamine receptors.

Harvard Medical School

Structure-guided development of covalent TAK1 inhibitors.

Harvard Medical School

A benzo[b]thiophene-based selective type 4 S1P receptor agonist.

Harvard Medical School

Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.

Harvard Medical School

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor.

Harvard Medical School

Part 3: Notch-sparing¿-secretase inhibitors: SAR studies of 2-substituted aminopyridopyrimidinones.

Harvard Medical School

Part 1: Notch-sparing¿-secretase inhibitors: The identification of novel naphthyl and benzofuranyl amide analogs.

Harvard Medical School

Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.

Harvard Medical School

Development of Selective Covalent Janus Kinase 3 Inhibitors.

Harvard Medical School

Structure-activity relationship study of 4EGI-1, small molecule eIF4E/eIF4G protein-protein interaction inhibitors.

Harvard Medical School

Synthesis of rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) mimetic and their in vitro characterization as inhibitors of protein-protein interaction.

Harvard Medical School

Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies.

Harvard Medical School

Radiosynthesis and evaluation of [11C]EMPA as a potential PET tracer for orexin 2 receptors.

Harvard Medical School

Structure-activity relationship, kinetic mechanism, and selectivity for a new class of ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitors.

Harvard Medical School

Synthesis, binding affinity, and functional in vitro activity of 3-benzylaminomorphinan and 3-benzylaminomorphine ligands at opioid receptors.

Harvard Medical School

Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors.

Harvard Medical School

Aminothiazolomorphinans with mixed¿ andµ opioid activity.

Harvard Medical School

Synthesis and Biological Evaluation of N-Fluoroalkyl and 2-Fluoroalkoxy Substituted Aporphines: Potential PET Ligands for Dopamine D(2) Receptors.

Harvard Medical School

Synthesis and biological evaluation of C-12 triazole and oxadiazole analogs of salvinorin A.

Harvard Medical School

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School

Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.

Harvard Medical School

High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity.

Harvard Medical School

High-affinity carbamate analogues of morphinan at opioid receptors.

Harvard Medical School

Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.

Harvard Medical School

Stereochemical analysis of (hydroxyethyl)urea peptidomimetic inhibitors of gamma-secretase.

Harvard Medical School

Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.

Harvard Medical School

Synthesis and in vitro pharmacological studies of new C(2) modified salvinorin A analogues.

Harvard Medical School

2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.

Harvard Medical School

Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.

Harvard Medical School

Secretase targets for Alzheimer's disease: identification and therapeutic potential.

Harvard Medical School

Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine dependence.

Harvard Medical School

Synthesis and potent antifolate activity and cytotoxicity of B-ring deaza analogues of the nonpolyglutamatable dihydrofolate reductase inhibitor Nalpha-(4-amino-4-deoxypteroyl)-Ndelta-hemiphthaloyl- L-ornithine (PT523).

Harvard Medical School

2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.

Harvard Medical School

Synthesis and biological activity of N omega-hemiphthaloyl-alpha,omega- diaminoalkanoic acid analogues of aminopterin and 3',5-dichloroaminopterin.

Harvard Medical School

Side chain modified 5-deazafolate and 5-deazatetrahydrofolate analogues as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyltransferase inhibitors: synthesis and in vitro biological evaluation.

Harvard Medical School

Synthesis and biological activity of methotrexate analogues with two acid groups and a hydrophobic aromatic ring in the side chain.

Harvard Medical School

Methotrexate analogues. 34. Replacement of the glutamate moiety in methotrexate and aminopterin by long-chain 2-aminoalkanedioic acids.

Harvard Medical School

Methotrexate analogues. 33. N delta-acyl-N alpha-(4-amino-4-deoxypteroyl)-L-ornithine derivatives: synthesis and in vitro antitumor activity.

Harvard Medical School

Probing pockets S2-S4' of the gamma-secretase active site with (hydroxyethyl)urea peptidomimetics.

Harvard Medical School

Synthesis of (+),(-)-neamine and their positional isomers as potential antibiotics.

Harvard Medical School

Mixed kappa agonists and mu agonists/antagonists as potential pharmacotherapeutics for cocaine abuse: synthesis and opioid receptor binding affinity of N-substituted derivatives of morphinan.

Harvard Medical School

Differential signaling properties at the kappa opioid receptor of 12-epi-salvinorin A and its analogues.

Harvard Medical School

In vivo PET imaging of histone deacetylases by 18F-suberoylanilide hydroxamic acid (18F-SAHA).

Harvard Medical School

Synthesis and binding affinity of novel mono- and bivalent morphinan ligands for κ, μ, and δ opioid receptors.

Harvard Medical School

Structure-activity relationship study of 2,4-diaminothiazoles as Cdk5/p25 kinase inhibitors.

Harvard Medical School

Expanding the diversity of allosteric bcr-abl inhibitors.

Harvard Medical School

Synthesis and biological evaluation of C-2 halogenated analogs of salvinorin A.

Harvard Medical School

Structure of acid beta-glucosidase with pharmacological chaperone provides insight into Gaucher disease.

Harvard Medical School

Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro.

Harvard Medical School

A type-II kinase inhibitor capable of inhibiting the T315I"gatekeeper" mutant of Bcr-Abl.

Harvard Medical School

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.

Harvard Medical School

Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors.

Harvard Medical School

Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.

Harvard Medical School

Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.

Harvard Medical School

A stabilized demethoxyviridin derivative inhibits PI3 kinase.

Harvard Medical School

Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.

Harvard Medical School

Synthesis and pharmacological evaluation of hydrophobic esters and ethers of butorphanol at opioid receptors.

Harvard Medical School

Slow self-activation enhances the potency of viridin prodrugs.

Harvard Medical School

Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors.

Harvard Medical School

Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.

Harvard Medical School

A small-molecule therapeutic lead for Huntington's disease: preclinical pharmacology and efficacy of C2-8 in the R6/2 transgenic mouse.

Harvard Medical School

c-Src protein kinase inhibitors block assembly and maturation of dengue virus.

Harvard Medical School

The psammaplysenes, specific inhibitors of FOXO1a nuclear export.

Harvard Medical School

Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease.

Harvard Medical School

R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.

Harvard Medical School

In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.

Harvard Medical School

Design of an Ultralow Molecular Weight Heparin That Resists Heparanase Biodegradation.

Harvard Medical School

Synthesis and in vitro pharmacological studies of new C(4)-modified salvinorin A analogues.

Harvard Medical School

New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.

Harvard Medical School

Design, Synthesis, and Characterization of [

Harvard Medical School

Geometric diversity through permutation of backbone configuration in cyclic peptide libraries.

Harvard Medical School

Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.

Harvard Medical School

Structure-activity relationship study of novel tissue transglutaminase inhibitors.

Harvard Medical School

Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues.

Harvard Medical School

Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.

Harvard Medical School

Synthesis and Characterization of 5-(2-Fluoro-4-[

Harvard Medical School

Discovery of a Subnanomolar helical D-tridecapeptide inhibitor of gamma-secretase.

Harvard Medical School

Imaging Autotaxin

Harvard Medical School

Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.

Harvard Medical School

Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium.

Harvard Medical School

New 2,4-diamino-5-(2',5'-substituted benzyl)pyrimidines as potential drugs against opportunistic infections of AIDS and other immune disorders. Synthesis and species-dependent antifolate activity.

Harvard Medical School

Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.

Harvard Medical School

10-Ketomorphinan and 3-substituted-3-desoxymorphinan analogues as mixed kappa and micro opioid ligands: synthesis and biological evaluation of their binding affinity at opioid receptors.

Harvard Medical School

Further studies on 2,4-diamino-5-(2',5'-disubstituted benzyl)pyrimidines as potent and selective inhibitors of dihydrofolate reductases from three major opportunistic pathogens of AIDS.

Harvard Medical School

Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523).

Harvard Medical School

Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines: marked improvement in potency relative to trimethoprim and species selectivity relative to piritrexim.

Harvard Medical School

Synthesis of potential antidipsotropic isoflavones: inhibitors of the mitochondrial monoamine oxidase-aldehyde dehydrogenase pathway.

Harvard Medical School

Quinoline and thiazolopyridine allosteric inhibitors of MALT1.

Harvard Medical School

Synthesis and pharmacokinetic study of a

Harvard Medical School

Virtual Screening for Ligand Discovery at the σ

Harvard Medical School

Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6

Harvard Medical School

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.

Harvard Medical School

Benzopyrimidodiazepinone inhibitors of TNK2.

Harvard Medical School

The mitochondrial monoamine oxidase-aldehyde dehydrogenase pathway: a potential site of action of daidzin.

Harvard Medical School

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

Harvard Medical School

Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.

Harvard Medical School

5-deazafolate analogues with a rotationally restricted glutamate or ornithine side chain: synthesis and binding interaction with folylpolyglutamate synthetase.

Harvard Medical School

Discovery of a potent dual ALK and EGFR T790M inhibitor.

Harvard Medical School

Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.

Harvard Medical School

Identification of fluorinated (R)-(-)-aporphine derivatives as potent and selective ligands at serotonin 5-HT

Harvard Medical School

Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.

Harvard Medical School

Peptide-based covalent inhibitors of MALT1 paracaspase.

Harvard Medical School

2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.

Harvard Medical School

2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.

Harvard Medical School

Part 2. Notch-sparing γ-secretase inhibitors: The study of novel γ-amino naphthyl alcohols.

Harvard Medical School

Cytoprotective effects of hydrogen sulfide-releasing

Harvard Medical School

Imaging evaluation of 5HT2C agonists, [(11)C]WAY-163909 and [(11)C]vabicaserin, formed by Pictet-Spengler cyclization.

Harvard Medical School

2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.

Harvard Medical School

Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.

Harvard Medical School

1,2,3,4,6-Penta-O-galloyl-β-D-glucopyranose inhibits angiogenesis via inhibition of capillary morphogenesis gene 2.

Harvard Medical School

Phenolic compounds as antiangiogenic CMG2 inhibitors from Costa Rican endophytic fungi.

Harvard Medical School

Methotrexate analogues. 32. Chain extension, alpha-carboxyl deletion, and gamma-carboxyl replacement by sulfonate and phosphonate: effect on enzyme binding and cell-growth inhibition.

Harvard Medical School

The 2-desamino and 2-desamino-2-methyl analogues of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture.

Harvard Medical School

Optimization of a series of heterocycles as survival motor neuron gene transcription enhancers.

Harvard Medical School

Characterization of a highly selective inhibitor of the Aurora kinases.

Harvard Medical School

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).

Harvard Medical School

Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2.

Harvard Medical School

Synthesis and in vitro biological activity of new deaza analogues of folic acid, aminopterin, and methotrexate with an L-ornithine side chain.

Harvard Medical School

Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity.

Harvard Medical School

N-[4-[[(3,4-dihydro-4-oxo-1,2,3-benzotriazin-6- yl)methyl]amino]benzoyl]-L-glutamic acid, a novel A-ring analogue of 2-desamino-5,8-dideazafolic acid.

Harvard Medical School

Phenylmorphans and analogues: opioid receptor subtype selectivity and effect of conformation on activity.

Harvard Medical School

2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, preparation method and medicinal use thereof

Shanghai Haiyan Pharmaceutical Technology

PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof

Epizyme

Substituted N,2-diarylquinoline-4-carboxamides and the use thereof as anti-inflammatory agents

Bayer Pharma Aktiengesellschaft

Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Amgen

Ligand structure-activity requirements and phospholipid dependence for the binding of phorbol esters to protein kinase D.

University of Pittsburgh

Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.

Amgen

Discovery of 5-Substituted-6-chlorouracils as Efficient Inhibitors of Human Thymidine Phosphorylase.

Gilead Sciences

Kinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine.

Weizmann Institute of Science

Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.

Dupont Pharmaceuticals