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Synthesis and antitumor activity of N-sulfonyl-3,7-dioxo-5β-cholan-24-amides, ursodeoxycholic acid derivatives
- Source :
-
Steroids . Jan2013, Vol. 78 Issue 1, p53-58. 6p. - Publication Year :
- 2013
-
Abstract
- Abstract: A series of N-sulfonyl-3,7-dioxo-5β-cholan-24-amides, ursodeoxycholic acid derivatives, have been designed and synthesized in nine steps starting from ursodeoxycholic acid. The in vitro antitumor activity of the target compounds has been evaluated against HCT-116, MCF-7, K562, and SGC-7901 cell lines. The pharmacological results showed that most of the prepared compounds display excellent selective cytotoxicity toward HCT-116, MCF-7, and K562 cell lines. Particularly, compounds 10c, 10f and 10g show high inhibitory activity on these human cancer cell lines (IC50: 2.39–9.34μM). Conversely, all compounds are generally inactive against SGC-7901, with only 10b having IC50 below 50μM. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0039128X
- Volume :
- 78
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Steroids
- Publication Type :
- Academic Journal
- Accession number :
- 84476550
- Full Text :
- https://doi.org/10.1016/j.steroids.2012.09.009