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https://hdl.handle.net/10316/12885
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 | URI: | https://hdl.handle.net/10316/12885 | 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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Novel semisynthetic derivatives.pdf | 903.12 kB | Adobe PDF | View/Open |
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