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.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II)
Volume: 15 Issue: 10
Author(s): Jianping Yong, Canzhong Lu and Xiaoyuan Wu
Affiliation:
Keywords: Anticancer evaluation, quinazoline derivatives, synthesis.
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.
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Cite this article as:
Yong Jianping, Lu Canzhong and Wu Xiaoyuan, Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II), Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (10) . https://dx.doi.org/10.2174/1871520615666150526115904
DOI https://dx.doi.org/10.2174/1871520615666150526115904 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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