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Title: Novel semisynthetic derivatives of betulin and betulinic acid with cytotoxic activity
Authors: Santos, Rita C. 
Salvador, Jorge A. R. 
Marín, Silvia 
Cascante, Marta 
Keywords: Triterpenoids; Betulinic acid; Imidazole; Cytotoxicity
Issue Date: 1-Sep-2009
Publisher: Elsevier Ltd.
Citation: Bioorganic & Medicinal Chemistry. 17:17 (2009) 6241-6250
Abstract: A series of new imidazole carboxylic esters (carbamates) and N-acylimidazole derivatives of betulin and betulinic acid (14-29) have been synthesized. The new compounds were screened for in vitro cytotoxicity activity against human cancer cell lines HepG2, Jurkat and HeLa. A number of compounds have shown IC50 values lower than 2 [mu]M against the cancer cell lines tested and the vast majority has shown a better cytotoxicity profile than betulinic acid, including the betulin derivatives. N-Acylimidazole derivatives 26 and 27 (IC50 0.8 and 1.7 [mu]M in HepG2 cells) and the C-3 carbamate derivative 16 (IC50 2.0 [mu]M in HepG2 cells) were the most promising compounds. Based on the observed cytotoxicity, structure-activity relationships have been established
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2009.07.050
Rights: openAccess
Appears in Collections:FFUC- Artigos em Revistas Internacionais

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