Document Detail

Synthesis and evaluation of a novel series of heterocyclic oleanolic acid derivatives with anti-osteoclast formation activity.
MedLine Citation:
PMID:  19171409     Owner:  NLM     Status:  MEDLINE    
Oleanolic acid with anti-bone resorption effect was an active component discovered in a medicinal plant of Achyranthes bidentata. A series of heterocyclic derivatives of oleanolic acid including indole, pyrazine, quinoxaline, quinoline moieties and their natural amino acid amides were synthesized. Their inhibitory activity on the formation of osteoclast-like multinucleated cells (OCLs) and cytotoxicity of the selected derivatives were evaluated. Among the derivatives, compounds 2a and 8a displayed quite a potent activity even at 200 nM. The structure-activity relationships of the derivatives were also discussed.
Jun-Feng Li; Yu Zhao; Min-Min Cai; Xiao-Fei Li; Jian-Xin Li
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-12-31
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  44     ISSN:  1768-3254     ISO Abbreviation:  Eur J Med Chem     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-05-04     Completed Date:  2009-07-24     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  France    
Other Details:
Languages:  eng     Pagination:  2796-806     Citation Subset:  IM    
Key Lab of Analytical Chemistry for Life Science, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, China.
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MeSH Terms
Amino Acids / chemistry
Cell Survival / drug effects
Drug Design*
Heterocyclic Compounds / chemistry*
Oleanolic Acid / analogs & derivatives,  chemical synthesis*,  chemistry,  pharmacology*
Osteoclasts / cytology*,  drug effects*
Structure-Activity Relationship
Reg. No./Substance:
0/Amino Acids; 0/Heterocyclic Compounds; 508-02-1/Oleanolic Acid

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