Potent quinoxaline-Based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR Exploration and Effective Bioisosteric Replacement of a phenyl substituent
摘要:
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.