Potent quinoxaline-Based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR Exploration and Effective Bioisosteric Replacement of a phenyl substituent
作者:Michael R. Myers、Wei He、Barbara Hanney、Natalie Setzer、Martin P. Maguire、Allison Zulli、Glenda Bilder、Helen Galzcinski、Dilip Amin、Saul Needle、Alfred P. Spada
DOI:10.1016/s0960-894x(03)00654-1
日期:2003.9
Novel substituted 2-anilino- and 2-cycloalkylaminoquinoxalines have been found to be useful and selective inhibitors of PDGF-R autophosphorylation. Replacement of an anilino-substituent with substituted cyclohexylamino- or norbornylamino substituents led to significant improvements in the pharmacokinetic profile of these analogues. (C) 2003 Elsevier Ltd. All rights reserved.