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Updated: Jul 3, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Exploitation of the 3-quinolinecarbonitrile template for SRC tyrosine kinase inhibitors
1Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10956, USA. Bosched@wyeth.com
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.
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