Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds
Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds
复制标题
新型杂化2-苯基-3-烷基苯并呋喃和咪唑/三唑化合物的合成和细胞毒活性
DOI：
10.1016/j.bmcl.2013.06.001
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发表时间：
2013-08-01
影响因子：
2.7
通讯作者：
Yang, Xiao-Dong
中科院分区：
文献类型：
--
作者：
Chen, Wen;Deng, Xiao-Yan;Yang, Xiao-Dong
合成了一系列新型的2-苯基-3-烷基苯并呋喃与咪唑或三氮唑的杂化化合物，并进行了体外抗肿瘤活性评价。结果表明，2-乙基咪唑环和咪唑基-3-位被2-溴苄基或萘酰基取代是调节抑制活性的关键。其中，杂化化合物31对5株人肿瘤细胞株的IC50值为0.08-0.55µM，对乳腺癌(MCF-7)和结肠癌(SW480)的IC50值分别为顺铂(DDP)的40.8倍和40.1倍。(C)2013爱思唯尔有限公司。保留所有权利。
A series of novel hybrid compounds of 2-phenyl-3-alkylbenzofuran and imidazole or triazole were prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 2-ethyl-imidazole ring, and substitution of the imidazolyl-3-position with a 2-bromobenzyl or naphthylacyl group, were vital for modulating inhibitory activity. In particular, hybrid compound 31 was found to be the most potent derivative with IC50 values of 0.08-0.55 mu M against five strains human tumor cell lines and was found to be more selective against breast carcinoma (MCF-7) and colon carcinoma (SW480) (IC50 values 40.8-fold and 40.1-fold lower than cisplatin (DDP)). (C) 2013 Elsevier Ltd. All rights reserved.