New ursolic and betulinic derivatives as potential cytotoxic agents

被引：21

作者：

Baglin, I

Poumaroux, A

Nour, M

Tan, K

Mitaine-Offer, AC

Lacaille-Dubois, MA

Chauffert, B

Cavé, C

机构：

[1] Univ Bourgogne, Fac Pharm, Unite Mol Interet Biol, F-21079 Dijon, France

[2] INSERM, U517, Dijon, France

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2003年 / 18卷 / 02期

关键词：

ursolic acid; betulinic acid; triterpenoids; hemisynthesis; cytotoxicity; HT; 29; cells;

D O I：

10.1080/1475636031000093543

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 muM, respectively.

引用

页码：111 / 117

页数：7

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