title: Synthesis and antiproliferative activity of C-homo-lactam derivatives of 7-deoxycholic acid.
abstract: 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.
authors: College of Chemistry and Life Science, Guangxi Teachers Education University, Nanning 530001, PR China.
authors: Yanmin
authors: Y
authors: Huang
authors: Jianguo
authors: J
authors: Cui
authors: Sijing
authors: S
authors: Chen
authors: Chunfang
authors: C
authors: Gan
authors: Qiucui
authors: Q
authors: Yao
authors: Qifu
authors: Q
authors: Lin
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003840:Deoxycholic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D007769:Lactams / Q000737:chemistry*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007769:Lactams; D003840:Deoxycholic Acid