Exploitation of the 3-Quinolinecarbonitrile Template for Src Tyrosine Kinase Inhibitors

Title: Exploitation of the 3-Quinolinecarbonitrile Template for Src Tyrosine Kinase Inhibitors

Volume: 8 Issue: 10

Author(s): Diane H. Boschelli

Affiliation:

Keywords: 3-Quinolinecarbonitrile, kinase, Src, cancer, Abl, CML, SKI-606, bosutinib

Abstract: In 2000, Wyeth reported that the 3-quinolinecarbonitrile ring system was a template for EGFR inhibitors. It soon became apparent that the group at C-4 of this core was responsible for kinase selectivity. A 4-(2,4-dichloro-5- methoxyanilino) substituent provided potent inhibitors of Src, a non-receptor tyrosine kinase that plays a key role in cell signaling. One compound from this series, SKI-606, bosutinib, is currently in clinical trials for the treatment of cancer.

Cite this article as:

Boschelli H. Diane, Exploitation of the 3-Quinolinecarbonitrile Template for Src Tyrosine Kinase Inhibitors, Current Topics in Medicinal Chemistry 2008; 8 (10) . https://dx.doi.org/10.2174/156802608784911653