Document Detail

Studies on chemical modification and biology of a natural product, gambogic acid (II): Synthesis and bioevaluation of gambogellic acid and its derivatives from gambogic acid as antitumor agents.
MedLine Citation:
PMID:  20605273     Owner:  NLM     Status:  MEDLINE    
Gambogic acid (GA) has been reported to be a potent apoptosis inducer. The fact that it is amenable to chemical modification makes GA an attractive molecule for the development of anticancer agents. We firstly reported the synthesis of gambogellic acid, which was generated under acid catalysis from readily available GA by a base-catalyzed diene intramolecular annelation. Sequentially, thirteen new compounds were synthesized and their inhibitory activity on HT-29, Bel-7402, BGC-823, and A549 cell lines were evaluated in vitro by MTT assay, and (38, 40)-epoxy-33-chlorogambogellic acid (4) was identified as a BGC-823 cell apoptosis inducer through MTT cell assay, observations of morphological changes, and Annexin-V/PI double-staining assay. Compound 4 showed significant effects in inducing apoptosis and might serve as a potential lead compound for discovery of new anticancer drugs. Further structure-activity relationships (SARs) of gambogic acid derivatives were discussed.
Jinxin Wang; Junhai Ma; Qidong You; Li Zhao; Fan Wang; Chong Li; Qinglong Guo
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-05-13
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  45     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-08-09     Completed Date:  2010-11-30     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  4343-53     Citation Subset:  IM    
Copyright Information:
2010 Elsevier Masson SAS. All rights reserved.
Department of Medicinal Chemistry, China Pharmaceutical University, Tongjiaxiang 24, Nanjing 210009, China.
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MeSH Terms
Annexin A5 / metabolism
Antineoplastic Agents / chemical synthesis,  chemistry,  pharmacology
Apoptosis / drug effects
Biological Products / chemical synthesis*,  chemistry,  pharmacology*
Cell Line, Tumor
Inhibitory Concentration 50
Structure-Activity Relationship
Xanthones / chemical synthesis*,  chemistry,  pharmacology*
Reg. No./Substance:
0/Annexin A5; 0/Antineoplastic Agents; 0/Biological Products; 0/Xanthones; 0/gambogellic acid; 2752-65-0/gambogic acid

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