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

页码：2265 / 2267

页数：3

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