PMID

Data

Article Title

Organization

Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.

Univ. Lille

Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.

Novartis Institutes For Biomedical Research

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

University of Oxford

Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.

Hoffmann-La Roche

Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.

Pfizer

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.

Kyowa Hakko Kogyo

 

The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-

TBA

 

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

TBA

 

Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives

TBA

 

Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors

TBA

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Abbott Laboratories

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

Abbott Laboratories

4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.

University of Auckland

Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.

Abbott Laboratories

High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.

Hadassah Hebrew University

Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.

Johnson & Johnson Pharmaceutical Research and Development

2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.

Johnson & Johnson Pharmaceutical Research and Development

Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.

Kirin Brewery

Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.

Aventis Pharmaceuticals

Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.

Aventis Pharmaceuticals

Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.

Johnson & Johnson Pharmaceutical Research & Development

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

Abbott Bioresearch Center

Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.

Merck Research Laboratories

Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.

Novartis

Design and synthesis of a pyridone-based phosphotyrosine mimetic.

Cadus Pharmaceutical

5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.

Sterling Winthrop Pharmaceuticals Research Division

A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives.

RhôNe-Poulenc Rorer

 

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

Parke-Davis Pharmaceutical Research