Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 18, Pages 5058-5062Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.08.003
Keywords
betulinic acid; anticancer; cytotoxicity
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A new series of betulinic acid derivatives have been synthesized by introducing heterocyclic ring between C-2 and C-3 positions of betulinic acid. Further modi. cations were also carried out by reduction of C-20(29) unsaturated bond and substitution of C-28 carboxyl group by ester and amide linkage to enhance the selectivity. Compound 11 resulted in IC50 of 2.44, 2.5, and 2.7 mu g/ml on MIAPaCa, PA-1, and SW620 cancer cell lines, respectively. Compound 38 resulted in IC50 of 0.67 mu g/ml on MIAPaCa cell line. (C) 2008 Elsevier Ltd. All rights reserved.
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