Document Detail

The synthesis of ursolic acid derivatives with cytotoxic activity and the investigation of their preliminary mechanism of action.
MedLine Citation:
PMID:  19091579     Owner:  NLM     Status:  MEDLINE    
Nineteen ursolic acid derivatives (15 novel compounds) modified at the C-3 and the C-28 positions were synthesized. The cytotoxic activity of the derivatives was evaluated against HeLa, BGC-823 and SKOV3 cells by MTT assay. Inducing apoptosis and affecting cell cycle distribution by the derivatives in HeLa cells were assessed by flow cytometry and DNA fragmentation. Compounds 10b and 11b were particularly active to inhibit HeLa cells growth through inducing apoptosis and arresting cell cycle progression. The typical 'sub-G1 peak' and DNA ladder formation were checked and cell cycle was arrested at the S phase in a dose-dependent manner.
Yan-Qiu Meng; Dan Liu; Ling-Li Cai; Hong Chen; Bo Cao; Yi-Zheng Wang
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-11-20
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  17     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2009 Jan 
Date Detail:
Created Date:  2009-01-26     Completed Date:  2009-03-27     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  848-54     Citation Subset:  IM    
Department of Pharmaceutical Engineering, Shenyang Institute of Chemical Technology, Jing Ji Kai Fa Que 11 street, Shenyang 110142, PR China.
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MeSH Terms
Antineoplastic Agents, Phytogenic / chemical synthesis*,  pharmacology
Apoptosis / drug effects*
Cell Cycle / drug effects*
Cell Line, Tumor
Cell Survival / drug effects
DNA Fragmentation
Triterpenes / chemical synthesis*,  pharmacology
Reg. No./Substance:
0/Antineoplastic Agents, Phytogenic; 0/Triterpenes; 77-52-1/ursolic acid

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