Article
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.
Journal of medicinal chemistry - 8 Apr 2010
Pawar Vijaykumar G, Sos Martin L, Rode Haridas B, Rabiller Matthias, Heynck Stefanie, van Otterlo Willem A L, Thomas Roman K, Rauh Daniel
Abstract excerpt
The mutant receptor tyrosine kinase EGFR is a validated and therapeutically amenable target for genotypically selected lung cancer patients. Here we present the synthesis and biological evaluation of a series of 6- and 7-substituted 4-anilinoquinolines as potent type I inhibitors of clinically relevant mutant variants of EGFR. Quinolines 3a and 3e were found to be highly active kinase inhibitors in biochemical...
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