Document Detail


Synthesis of 3-O-acyl/3-benzylidene/3-hydrazone/3-hydrazine/17-carboxyacryloyl ester derivatives of betulinic acid as anti-angiogenic agents.
MedLine Citation:
PMID:  15149668     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
New 3-O-acyl, 3-benzylidene, 3-hydrazone, 3-hydrazine, 17-carboxyacryloyl ester derivatives of betulinic acid (2-6, 8-11, 13, 17, 18, 21, and 22) were synthesized and evaluated in vitro for anti-angiogenic activity on endothelial cell cytotoxicity, specificity, and tube-formation ability. All derivatives reported here showed IC(50)<4 microg/mL. Compounds 3, 9, 10, 17, 21, and 22 have shown better cytotoxicity (IC(50)<1.2 microg/mL) than betulinic acid (1) and improved endothelial cell specificity (ECS>10) in some cases. Compounds 10, 17, and 18 have shown 20%, 32%, and 48% reduction in TLS, respectively, and were found better than betulinic acid (1). We have shown that 20,29-dihydrobetulinic acid derivatives have better anti-angiogenic activity as compared to betulinic acid or its other derivatives.
Authors:
Rama Mukherjee; Manu Jaggi; Praveen Rajendran; Sanjay K Srivastava; Mohammad J A Siddiqui; Anand Vardhan; Anand C Burman
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  14     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2004 Jun 
Date Detail:
Created Date:  2004-05-19     Completed Date:  2005-01-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3169-72     Citation Subset:  IM    
Affiliation:
Divisions of Experimental Oncology, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201 010, UP, India.
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MeSH Terms
Descriptor/Qualifier:
Angiogenesis Inhibitors / chemical synthesis*,  pharmacology
Benzylidene Compounds / chemical synthesis,  pharmacology
Cell Line, Tumor
HT29 Cells
Humans
Triterpenes / chemical synthesis*,  pharmacology
Chemical
Reg. No./Substance:
0/Angiogenesis Inhibitors; 0/Benzylidene Compounds; 0/Triterpenes; 472-15-1/betulinic acid

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