Document Detail


Synthesis and Biological Evaluation of Sophoridinol Derivatives as a Novel Family of Potential Anticancer Agents.
MedLine Citation:
PMID:  25408835     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
New N-substituted sophoridinic acid/ester and sophoridinol derivatives were synthesized and evaluated for their cytotoxic activity in human HepG2 hepatoma cells from the lead sophoridine (1). Among the newly synthesized compounds, sophoridinol 7i displayed a potential antiproliferative activity with an IC50 of 3.1 μM. Importantly, it exerted an almost equipotent effect against both wild MCF-7 and adriamycin (AMD)-resistant MCF-7 (MCF-7/AMD) breast carcinoma cell lines. Its mode of action was to arrest the cell cycle at the G0/G1 phase, consistent with that of the parent 1. In addition, compound 7i also showed a reasonable ClogP value and favorable pharmacokinetic property with an area under the concentration-time curve (AUC) of 10.3 μM·h in rats, indicating an ideal druggable characteristic. We consider sophoridinol derivatives to be a novel family of promising antitumor agents with an advantage of inhibiting drug-resistant cancer cells.
Authors:
Chongwen Bi; Caixia Zhang; Yinghong Li; Sheng Tang; Shenggang Wang; Rongguang Shao; Haigen Fu; Feng Su; Danqing Song
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-9-22
Journal Detail:
Title:  ACS medicinal chemistry letters     Volume:  5     ISSN:  1948-5875     ISO Abbreviation:  ACS Med Chem Lett     Publication Date:  2014 Nov 
Date Detail:
Created Date:  2014-11-19     Completed Date:  -     Revised Date:  2014-11-20    
Medline Journal Info:
Nlm Unique ID:  101521073     Medline TA:  ACS Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  1225-1229     Citation Subset:  -    
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