PMID

Data

Article Title

Organization

Synthesis and optimization of furano[3,2-d]pyrimidines as selective spleen tyrosine kinase (Syk) inhibitors.

Abbvie Bioresearch Center

Identification of a selective inhibitor of transforming growth factorß-activated kinase 1 by biosensor-based screening of focused libraries.

Chugai Pharmaceutical

Hemicholinium and related lipids: inhibitors of protein kinase C.

Louisiana State University

Design of potent protein kinase inhibitors using the bisubstrate approach.

Ura Cnrs 1309

Synthesis of quaternary amine ether lipids and evaluation of neoplastic cell growth inhibitory properties.

University of North Carolina

Synthesis of N-alkyl substituted indolocarbazoles as potent inhibitors of human cytomegalovirus replication.

Glaxosmithkline

Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.

Purdue University

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Merck

Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.

Southeast University

Discovery and optimization of 1,7-disubstituted-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-ones as potent and selective PKC¿ inhibitors.

Takeda Pharmaceutical

Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School of Medicine At Mount Sinai

Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit.

Abbvie Bioresearch Center

Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.

Astrazeneca

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

Exelixis

Design and optimization of selective protein kinase C¿ (PKC¿) inhibitors for the treatment of autoimmune diseases.

Vertex Pharmaceuticals

Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.

Pfizer

C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.

Wyeth Research

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.

University of California

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.

University of Oxford

Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.

Abbott Laboratories

Kinase inhibitors: not just for kinases anymore.

Northwestern University

Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family.

Millennium Pharmaceuticals

Structure-activity relationship studies of flavopiridol analogues.

Mitotix

 

Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructure

TBA

Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.

Glaxosmithkline

Novel and selective spiroindoline-based inhibitors of Sky kinase.

Pfizer

4-benzimidazolyl-3-phenylbutanoic acids as novel PIF-pocket-targeting allosteric inhibitors of protein kinase PKC¿.

Saarland University

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.

Bristol-Myers Squibb

5-amino-pyrazoles as potent and selective p38a inhibitors.

Bristol-Myers Squibb Research and Development

Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Wyeth Research

Synthesis and PKCtheta inhibitory activity of a series of 5-vinyl phenyl sulfonamide-3-pyridinecarbonitriles.

Wyeth Research

First generation 5-vinyl-3-pyridinecarbonitrile PKCtheta inhibitors.

Wyeth Research

C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.

Wyeth Research

 

Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK II

TBA

 

A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation

TBA

 

Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol

TBA

 

Synthesis of bisindolylmaleimide macrocycles

TBA

 

Novel PKC inhibitory analogs of balanol with replacement of the ester functionality

TBA

 

Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C

TBA

Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Wyeth Research

2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.

Wyeth Research

Spheciosterol sulfates, PKCzeta inhibitors from a philippine sponge Spheciospongia sp.

University of Utah

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.

Hefei University of Technology

Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center

Development of inhibitors targeting glycogen synthase kinase-3? for human diseases: Strategies to improve selectivity.

West China Hospital

Fragment-to-Lead Medicinal Chemistry Publications in 2020.

Vrije Universiteit Amsterdam

Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.

Johnson & Johnson Pharmaceutical Research & Development

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Bristol-Myers Squibb Pharmaceutical Research Institute

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

Bristol-Myers Squibb Pharmaceutical Research Institute

Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.

Eli Lilly

Novel IKK inhibitors: beta-carbolines.

Millennium Pharmaceuticals

Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.

Eli Lilly

Optimization of 2-phenylaminoimidazo[4,5-h]isoquinolin-9-ones: orally active inhibitors of lck kinase.

Boehringer Ingelheim Pharmaceuticals

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University

Synthesis and kinase inhibitory activity of 3'-(S)-epi-K-252a.

Cephalon

Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.

Abbott Bioresearch Center

Beta-carbolines as specific inhibitors of cyclin-dependent kinases.

Institute of Molecular and Cell Biology

Mixed lineage kinase activity of indolocarbazole analogues.

Kyowa Hakko Kogyo

Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidines as atypical protein kinase C inhibitors to control retinal vascular permeability and cytokine-induced edema.

University of Michigan

Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy.

Asahi Kasei Pharma

Variegatic acid from the edible mushroom Tylopilus ballouii inhibits TNF-? production and PKC?1 activity in leukemia cells.

Tokyo University of Agriculture

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.

Merck And

Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I.

Basf Bioresearch

Optimization of an azetidine series as inhibitors of colony stimulating factor-1 receptor (CSF-1R) Type II to lead to the clinical candidate JTE-952.

Japan Tobacco

Synthesis and biological activities of NB-506 analogues modified at the glucose group.

Banyu Tsukuba Research Institute

4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.

Celltech Therapeutics

Synthesis and biological activities of NB-506 analogues: Effects of the positions of two hydroxyl groups at the indole rings.

Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories

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

Discovery of 4

TBA

Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.

Toho University

A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs.

China Pharmaceutical University

ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University of Florida

Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.

Takeda Pharmaceutical

Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.

Eli Lilly

(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.

Eli Lilly

Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.

Abbvie Bioresearch Center

Discovery and optimization of 1,3,5-trisubstituted pyrazolines as potent and highly selective allosteric inhibitors of protein kinase C-?.

Saarland University

Synthesis and structure-activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors.

Penn State University College of Medicine

Glycoglycerolipid analogues inhibit PKC translocation to the plasma membrane and downstream signaling pathways in PMA-treated fibroblasts and human glioblastoma cells, U87MG.

University of Milan

Antitumor studies -- part 2: structure-activity relationship study for flavin analogs including investigations on their in vitro antitumor assay and docking simulation into protein tyrosine kinase.

Okayama University

A novel phorbol ester from Excoecaria agallocha.

National Cancer Institute

Kinase inhibitors from Polygonum cuspidatum.

Purdue University

Bioactive peroxides as potential therapeutic agents.

The Hebrew University of Jerusalem

Methylpendolmycin, an indolactam from a Nocardiopsis sp.

Sterling Research Group

Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.

Universit£

Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.

Universit£

Fused pyrrolo[2,3-c]carbazol-6-ones: novel immunostimulants that enhance human interferon-gamma activity.

Cephalon

An aminopyridazine-based inhibitor of a pro-apoptotic protein kinase attenuates hypoxia-ischemia induced acute brain injury.

Northwestern University

Isolation of Phorbol Esters from Euphorbia grandicornis and Evaluation of Protein Kinase C- and Human Platelet-Activating Effects of Euphorbiaceae Diterpenes.

Kaohsiung Medical University

A novel 2,4-diaminopyrimidine derivative as selective inhibitor of protein kinase C theta prevents allograft rejection in a rat heart transplant model.

Astellas Pharma

From bench (laboratory) to bed (hospital/home): How to explore effective natural and synthetic PAK1-blockers/longevity-promoters for cancer therapy.

Pak Research Center

Natural Products with Heteroatom-Rich Ring Systems.

University of Auckland

Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C.

Sanofi Recherche

Discovery of Novel Small-Molecule Inhibitors of NF-?B Signaling with Antiinflammatory and Anticancer Properties.

University of Colorado

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.

Agency For Science, Technology and Research (A*Star)

Methyl 3-(3-(4-(2,4,4-Trimethylpentan-2-yl)phenoxy)-propanamido)benzoate as a Novel and Dual Malate Dehydrogenase (MDH) 1/2 Inhibitor Targeting Cancer Metabolism.

Dongguk University

Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.

Novartis Institutes For Biomedical Research

Identification of potent and selective neuropeptide Y Y(1) receptor agonists with orexigenic activity in vivo.

Schering-Plough Research Institute

Hexosaminidase inhibitors as new drug candidates for the therapy of osteoarthritis.

The Scripps Research Institute

Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.

University of Dundee

Meridianins, a new family of protein kinase inhibitors isolated from the ascidian Aplidium meridianum.

Cnrs

 

DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS

Parke-Davis Pharmaceutical Research