2. Academic Validation
  3. Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor

Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor

  • J Med Chem. 2010 Apr 8;53(7):2892-901. doi: 10.1021/jm901877j.
Vijaykumar G Pawar 1,  Martin L Sos,  Haridas B Rode,  Matthias Rabiller,  Stefanie Heynck,  Willem A L van Otterlo,  Roman K Thomas,  Daniel Rauh
Affiliations

Affiliation

  • 1 Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.
PMID: 20222733 DOI: 10.1021/jm901877j
Abstract

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 assays and were further investigated for their biological effect on EGFR-dependent Ba/F3 cells and non-small cell lung Cancer (NSCLC) cell lines.

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