Synthesis and in vitro antitumor activity of substituted quinazoline and quinoxaline derivatives: Search for anticancer agent
Synthesis and in vitro antitumor activity of substituted quinazoline and quinoxaline derivatives: Search for anticancer agent
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DOI：
10.1016/j.ejmech.2011.03.015
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发表时间：
2011-06-01
影响因子：
6.7
通讯作者：
Chauhan, Ankit
中科院分区：
文献类型：
--
作者：
Noolvi, Malleshappa N.;Patel, Harun M.;Chauhan, Ankit
研究了一些 2-呋喃-4(3H)-喹唑啉酮、二酰胺（开环喹唑啉）、喹喔啉的合成及其使用美国国家癌症研究所 (NCI) 疾病导向抗肿瘤筛选方案作为抗肿瘤药物的生物学评价。在合成的化合物中，有 17 种化合物获得了 NSC 代码，并在美国国家癌症研究所 (NCI) 在完整的 NCI 60 细胞组中筛选了单次高剂量 (10-5 M) 的抗癌活性。在所选化合物中，3-(2-氯亚苄基胺)-2-(呋喃-2-基)喹唑啉-4(3h)-one 21被发现是该系列中最活跃的候选化合物，在针对卵巢OVCAR-4和非小细胞肺癌NCI-H522的五个剂量水平筛选中，GI(50)分别为1.82和2.14μM。理性方法和 QSAR 技术使我们能够了解喹唑啉、二酰胺和喹喔啉衍生物的药效要求。 (C) 2011 Elsevier Masson SAS。版权所有。
The synthesis of some 2-furano-4(3H)-quinazolinones, diamides (open ring quinazolines), quinoxalines and their biological evaluation as antitumor agents using National Cancer Institute (NCI) disease oriented antitumor screen protocol are investigated. Among the synthesize compounds, seventeen compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10-5 M) in full NCI 60 cell panel. Among the selected compounds, 3-(2-chloro benzylideneamine)-2-(furan-2-yl) quinazoline-4(3h)-one 21 was found to be the most active candidate of the series at five dose level screening against Ovarian OVCAR-4 and Non-small cell lung cancer NCI-H522 with GI(50) 1.82 & 2.14 mu M respectively. Rational approach and QSAR techniques enabled the understanding of the pharmacophoric requirement for quinazoline, diamides and quinoxaline derivatives. (C) 2011 Elsevier Masson SAS. All rights reserved.