Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model

Autor:	Laura Belanger, Limei Zhang, Maria L. Webb, Yajing Rong, Quynhchi Pham, Steven G. Kultgen, Susan M. Parlato, Andrew Laird Roughton, Tiffany L. Walker, Yan Xu, Michael Ohlmeyer, Bing Hu, Koc-Kan Ho, Anthony E. Klon, David A. Dunn, Darcey Black, Peter C. Ray, James R. Beasley, Jane Wright, Jui-Hsiang Chan, Kai Xu
Rok vydání:	2009
Předmět:	Molecular model Pyrimidine Stereochemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Animals Structure–activity relationship Computer Simulation Spontaneous hypertensive rat Binding site Protein Kinase Inhibitors Molecular Biology Antihypertensive Agents Triazine rho-Associated Kinases Binding Sites biology Triazines Organic Chemistry Rats Disease Models Animal Pyrimidines chemistry Enzyme inhibitor Hypertension biology.protein Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:6027-6031
ISSN:	0960-894X
Popis:	The profile of a series of triazine and pyrimidine based ROCK inhibitors is described. An initial binding mode was established based on a homology model and the proposed interactions are consistent with the observed SAR. Compounds from the series are potent in a cell migration assay and possess a favorable kinase selectivity. In vivo activity was demonstrated for compound 1A in a spontaneous hypertensive rat model.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1cc5a6f020505ba7c250b5885d755431 https://doi.org/10.1016/j.bmcl.2009.09.046 Zobrazit plný text záznamu Full Text from ScienceDirect