Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent |
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| Authors: | Myers Michael R He Wei Hanney Barbara Setzer Natalie Maguire Martin P Zulli Allison Bilder Glenda Galzcinski Helen Amin Dilip Needle Saul Spada Alfred P |
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| Institution: | Aventis Pharmaceuticals, Route 202/206, Bridgewater, NJ 08807, USA. myers_michael_r@lilly.com |
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| Abstract: | 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. |
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