Synthesis and antiproliferative activity of C-homo-lactam derivatives of 7-deoxycholic acid

被引：17
|
作者：
Huang, Yanmin [1 ]
Cui, Jianguo [1 ]
Chen, Sijing [1 ]
Gan, Chunfang [1 ]
Yao, Qiucui [1 ]
Lin, Qifu [1 ]
机构：
[1] Guangxi Teachers Educ Univ, Coll Chem & Life Sci, Nanning 530001, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 07期
关键词：
7-Deoxycholic acid; 12-Oxy-12a-aza-C-homo-7-deoxycholic acid derivatives; C-homo-lactam; Cytotoxicity; Antiproliferative activity; INDUCE APOPTOSIS;
D O I：
10.1016/j.bmcl.2012.08.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Using deoxycholic acid as starting materials, a series of 12a-aza-C-homo-12-one 7-deoxycholic acid derivatives were synthesized The antiproliferative activity of the synthesized compounds against some carcinoma cell lines was investigated. The results showed that some 12-oxy-12a-aza-C-homo-7-deoxycholic acid derivatives displayed distinct cytotoxicity to HeLa (human cervical carcinoma) and Tu 686 (laryngocarcinoma) tumor cell lines. In particular, the IC50 values of the compounds 6 and 7 against Tu 686 cells are 16.7 and 19.8 mu M/L respectively. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2265 / 2267
页数：3
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