| Synthesis of 3-O-acyl/3-benzylidene/3-hydrazone/3-hydrazine/17-carboxyacryloyl ester derivatives of betulinic acid as anti-angiogenic agents. | |
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MedLine Citation:
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PMID: 15149668 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Rama Mukherjee; Manu Jaggi; Praveen Rajendran; Sanjay K Srivastava; Mohammad J A Siddiqui; Anand Vardhan; Anand C Burman |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 14 ISSN: 0960-894X ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2004 Jun |
Date Detail:
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Created Date: 2004-05-19 Completed Date: 2005-01-06 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 3169-72 Citation Subset: IM |
Affiliation:
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Divisions of Experimental Oncology, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201 010, UP, India. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Angiogenesis Inhibitors
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chemical synthesis*,
pharmacology Benzylidene Compounds / chemical synthesis, pharmacology Cell Line, Tumor HT29 Cells Humans Triterpenes / chemical synthesis*, pharmacology |
| Chemical | |
Reg. No./Substance:
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0/Angiogenesis Inhibitors; 0/Benzylidene Compounds; 0/Triterpenes; 472-15-1/betulinic acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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