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Updated: Oct 2, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
4-Anilino-3-cyanobenzo[g]quinolines as kinase inhibitors
Nan Zhang1, Biqi Wu, Allan Wissner
1Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. zhangn@war.wyeth.com
Abstract:
A series of 4-anilino-3-cyanobenzo[g]quinolines was prepared as potent kinase inhibitors. Compared with their bicyclic 4-anilino-3-cyanoquinoline analogues, the tricyclic 4-anilino-3-cyanobenzo[g]quinolines are less active against EGF-R kinase, equally active against MAPK kinase (MEK), and more active against Src kinase. For Src kinase inhibition, the best activity is obtained when both the 7- and 8-positions are substituted with alkoxy groups. Several of these kinase inhibitors show potent growth inhibitory activity in tumor cells.
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