Document Detail


Synthesis and biological evaluation of novel sarsasapogenin derivatives as potential anti-tumor agents.
MedLine Citation:
PMID:  25456170     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Based on the fact that timosaponin A-III (TA-III) exhibits potent cytotoxic effects and has been considered as a potential anti-tumor agent, a range of novel sarsasapogenin derivatives 1, 2a-2g, 3, 4, 5, 6a-6g have been synthesized by a simple and facile synthetic route. The in vitro cytotoxic activity of these synthetic compounds has been evaluated against ten human cancer cell lines. The pharmacological results showed that most of the sarsasapogenin derivatives displayed excellent selective cytotoxicity toward the cancer cell lines. An amino group at C-3 or C-26 position of the sapogenin had a profound influence on the cytotoxic activity. In particular, compound 6c exhibited significantly inhibitory activity against A375-S2 (IC50=0.56μM) and HT1080 (IC50=0.72μM) cells. However, introducing a bromo or morpholinyl substituent at the C-3 and C-26 position of the sapogenin generally rendered it inactive against the human cancer cell lines. This research provides a theoretical reference for the exploration of new anti-tumor drugs.
Authors:
Yuan Yin; Xun-Chen Zhao; Shao-Jie Wang; Ping-Yi Gao; Ling-Zhi Li; Takshi Ikejima; Shao-Jiang Song
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-10-19
Journal Detail:
Title:  Steroids     Volume:  -     ISSN:  1878-5867     ISO Abbreviation:  Steroids     Publication Date:  2014 Oct 
Date Detail:
Created Date:  2014-12-2     Completed Date:  -     Revised Date:  2014-12-3    
Medline Journal Info:
Nlm Unique ID:  0404536     Medline TA:  Steroids     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2014. Published by Elsevier Inc.
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