Discovery and preliminary structure–activity relationship studies of novel benzotriazine based compounds as Src inhibitors

Autor:	Chi Ching Mak, Xianchang Gong, Elena Dneprovskaia, Andrew McPherson, Ved P. Pathak, J. Hood, Binqi Zeng, Boris Klebansky, Richard M. Fine, W. Liao, Wolfgang Wrasidlo, Glenn Noronha, Joel Renick, Ningning Zhao, Y. Zhou, Kathy Barrett, Colleen Gritzen, Moorthy S. S. Palanki, Xinshan Kang, Ge Li, Ute Splittgerber, Richard M. Soll, Daniel L. Lohse, Jianguo Cao
Rok vydání:	2006
Předmět:	Molecular model Bicyclic molecule biology Triazines Kinase Stereochemistry Chemistry Proto-Oncogene Proteins pp60(c-src) Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Small molecule Structure-Activity Relationship Enzyme inhibitor Drug Discovery biology.protein Humans Molecular Medicine Structure–activity relationship Signal transduction Molecular Biology Proto-oncogene tyrosine-protein kinase Src
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:5546-5550
ISSN:	0960-894X
Popis:	We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kinase inhibitors. The 3-(2-(1-pyrrolidinyl)ethoxy)phenyl analogue (43) was identified as one of the most potent inhibitors of Src kinase.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77c3a59d9d64cb5d6108ec85b738a7b4 https://doi.org/10.1016/j.bmcl.2006.08.035 Zobrazit plný text záznamu Full Text from ScienceDirect