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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II)

Author(s): Jianping Yong, Canzhong Lu and Xiaoyuan Wu

Volume 15, Issue 10, 2015

Page: [1326 - 1332] Pages: 7

DOI: 10.2174/1871520615666150526115904

Price: $65

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Abstract

Under the guidance of our previous work, we synthesized 21 new structures of quinazolines (3a~3u) and evaluated their in vitro anticancer activity against A549, HCT116 and MCF-7 cell lines using the MTT method. Most compounds showed good to excellent anticancer activity. In particular, 3o (regarded as erlotinib analogues) has marked anticancer activity against A549, HCT116 and MCF-7 cell lines (IC50s: 4.26, 3.92 and 0.14 μM, respectively) as compared with the standard anticancer drug gefitinib (IC50s: 17.9, 21.55 and 20.68 μM, respectively), and which can be regarded as the best candidate for development of anticancer drugs.

Keywords: Anticancer evaluation, quinazoline derivatives, synthesis.

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