Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds

被引：43
作者：
Chen, Wen [1 ]
Deng, Xiao-Yan [1 ]
Li, Yan [2 ]
Yang, Li-Juan [3 ,4 ]
Wan, Wei-Chao [1 ]
Wang, Xue-Quan [1 ]
Zhang, Hong-Bin [1 ]
Yang, Xiao-Dong [1 ]
机构：
[1] Yunnan Univ, Sch Chem Sci & Technol, Minist Educ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China
[2] Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650204, Peoples R China
[3] Yunnan Univ Nationalities, State Ethn Affairs Commiss, Key Lab Ethn Med Resource Chem, Kunming 650031, Peoples R China
[4] Yunnan Univ Nationalities, Minist Educ, Kunming 650031, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 15期
关键词：
Hybrid compound; Benzofuran; Imidazole; Triazole; Structure-activity relationships; ANTITUMOR-ACTIVITY; NATURAL-PRODUCTS; DRUG DISCOVERY; DESIGN; DERIVATIVES; BENZOFURANS; IODIDES; ANALOGS; TRANS;
D O I：
10.1016/j.bmcl.2013.06.001
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：4297 / 4302
页数：6
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