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Bioorg Med Chem Lett. 2003 Sep 15;13(18):3091-5.

Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.

Author information

1
Aventis Pharmaceuticals, Route 202/206, Bridgewater, NJ 08807, USA. myers_michael_r@lilly.com

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.

PMID:
12941341
DOI:
10.1016/s0960-894x(03)00654-1
[Indexed for MEDLINE]

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