The synthesis and antitumor activity of lithocholic acid and its derivatives

- A concise synthesis of lithocholic acid and its amide derivatives was reported.
- The antiproliferative activities of these derivatives were evaluated in vitro.
- Transwell migration, colony formation and apoptosis assays were performed.

In this paper, a new and concise synthetic route of lithocholic acid (LCA) using commercially available steroid source deoxycholic acid is reported. A series of amide derivatives of LCA were also synthesized and investigated for their activity against the growth of MCF-7 and MCF-7/ADR cells using the sulforhodamine B assay. For MCF-7, the most potent compound 20 showed a 20-fold higher antitumor activity than LCA. For MCF-7/ADR, the most potent compound 24 showed a 22-fold higher antitumor activity than LCA. The transwell migration assay of 20 was evaluated on MDA-MB-231 cells. The colony formation and apoptosis assays of 20 were performed on MCF-7 and MCF-7/ADR cell lines.

A concise synthesis of lithocholic acid and its amide derivatives and evaluation of their activity against the growth of breast cancer cell lines.204