Chemical Biology and Drug Design
Chemical Biology and Drug Design
5 years ago

Synthesis and Biological Evaluation of Novel Substituted 4-Anilinoquinazolines as Antitumor Agents

Synthesis and Biological Evaluation of Novel Substituted 4-Anilinoquinazolines as Antitumor Agents
Lijuan Chen, Lei Lei, Xiaoyan Wang, Dong Cao, Zhuang Yang, Fang Wang, Liang Ma
Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their in vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC50 values of 25−682 nM against various types of cancer cell lines. In addition, 9a was confirmed that it could arrest the cell cycle at G2/M phase and trigger apoptosis. Indirect immunofluorescence staining revealed its anti-tubulin property. Importantly, 9a significantly inhibited tumor growths in SM-7721 xenograft models (57.0% tumor mass change) without causing significant loss of body weight, suggesting that 9a is a promising new anticancer agent to be developed. This article is protected by copyright. All rights reserved. Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their antiproliferative activities in vitro and anti-tumor effects in vivo.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.12706

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