Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase

Autor:	John T. Sisko, Christine Fernandes, Bradley K. Wong, Patrice A. Ciecko, Nancy E. Kohl, Mark T. Bilodeau, Keith W. Rickert, Laura Sepp-Lorenzino, Leonard D. Rodman, Timothy J. Koester, Jackson B. Gibbs, Cynthia Miller-Stein, Debra A. McLoughlin, Joseph J. Lynch, Carolyn A. Buser, George D. Hartman, Xianzhi Mao, Kathleen E. Coll, Kenneth A. Thomas, Jennifer M. Shipman, Thomas J. Tucker
Rok vydání:	2006
Předmět:	Stereochemistry Clinical Biochemistry hERG Pharmaceutical Science Sensitivity and Specificity Biochemistry Chemical synthesis Structure-Activity Relationship chemistry.chemical_compound Dogs Growth factor receptor Nitriles parasitic diseases Drug Discovery Animals Thiazole Protein Kinase Inhibitors neoplasms Molecular Biology chemistry.chemical_classification Molecular Structure biology Chemistry Kinase Organic Chemistry Macaca mulatta Vascular Endothelial Growth Factor Receptor-2 Rats Thiazoles Pyrimidines Enzyme Enzyme inhibitor cardiovascular system biology.protein Molecular Medicine Amine gas treating circulatory and respiratory physiology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:1146-1150
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2005.11.089
Popis:	Pyrimidino-thiazolyl carbonitriles were prepared that are potent VEGFR-2 (KDR) kinase inhibitors. The modification of lead structures resulted in 3m which exhibited the best overall profile in KDR inhibitory activity, iv/po pharmacokinetics, and reduced hERG affinity.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84e8b7d13a4632a1e8e93688c9eb9ed9 https://doi.org/10.1016/j.bmcl.2005.11.089 Zobrazit plný text záznamu Full Text from ScienceDirect