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

Yanmin Huang, Jianguo Cui, Sijing Chen, Chunfang Gan, Qiucui Yao, Qifu Lin

College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.

Bioorganic & medicinal chemistry letters 2013 Apr 1

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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 μM/L respectively. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs. Copyright © 2012 Elsevier Ltd. All rights reserved.

Citation

Yanmin Huang, Jianguo Cui, Sijing Chen, Chunfang Gan, Qiucui Yao, Qifu Lin. Synthesis and antiproliferative activity of C-homo-lactam derivatives of 7-deoxycholic acid. Bioorganic & medicinal chemistry letters. 2013 Apr 1;23(7):2265-7