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  • Title: New ursolic and betulinic derivatives as potential cytotoxic agents.
    Author: Baglin I, Poumaroux A, Nour M, Tan K, Mitaine-Offer AC, Lacaille-Dubois MA, Chauffert B, Cavé C.
    Journal: J Enzyme Inhib Med Chem; 2003 Apr; 18(2):111-7. PubMed ID: 12943194.
    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. Beta-D-Glucopyranosyl-3beta-hydroxyurs-12(13)-en-28-oate 1c, 3beta-3-(3-pyridyl)-prop-2-enoyloxyurs-12(13)-en-28-oic acid 1i and the potassium salt of 3beta-cinnamoyloxylup-20(29)-en-28-oic acid 2d demonstrated cytotoxic activity in the micromolar range: 8.0, 45.0 and 8.0 microM, respectively.
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