New Ursolic and Betulinic Derivatives as Potential Cytotoxic Agents
Open Access
- 1 April 2003
- journal article
- research article
- Published by Taylor & Francis in Journal of Enzyme Inhibition and Medicinal Chemistry
- Vol. 18 (2) , 111-117
- https://doi.org/10.1080/1475636031000093543
Abstract
Fifteen new ursolic and betulinic triterpenoids, bearing various functionalities at C-3 and C-28 were synthesized as potential cytotoxic agents. All compounds were obtained by a hemisynthetic route via ursolic and betulinic acids. Preliminary screening of these compounds on human HT 29 colon cancer cells revealed inhibitory activity for three of them. β-D-Glucopyranosyl-3β-hydroxyurs-12(13)-en-28-oate 1c, 3β-3-(3-pyridyl)-prop-2-enoyloxyurs-12(13)-en-28-oic acid 1i and the potassium salt of 3β-cinnamoyloxylup-20(29)-en-28-oic acid 2d demonstrated cytotoxic activity in the micromolar range: 8.0, 45.0 and 8.0 μM, respectively.Keywords
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