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

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• 作者：Yanmin Huang ; Jianguo Cui ; ^{cuijg1954@126.com} ; Sijing Chen ; Chunfang Gan ; Qiucui Yao ; Qifu Lin
• 关键词：7-Deoxycholic acid ; 12-Oxy-12a-aza-C-homo-7-deoxycholic acid derivatives ; C-homo-lactam ; Cytotoxicity ; Antiproliferative activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 April, 2013
• 年：2013
• 卷：23
• 期：7
• 页码：2265-2267
• 全文大小：186 K

文摘

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 ¦ÌM/L respectively. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.