期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 15, 期 16, 页码 5432-5439出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.05.057
关键词
18 beta-glycyrrhetinic acid; synthesis; apoptosis; structure-activity relationship
18 beta-Glycyrrhetinic acid (GA), 3 beta-hydroxyl-11-oxo-olean-12-ene-29-oic acid, has been found to inhibit growth and to induce apoptosis in cancer cells. Through structural modification, 16 GA derivatives (12 novel compounds) with modified structures at the C-3 and C-29 positions were synthesized. The antiproliferative effects and apoptosis induction abilities of these compounds were determined in human leukemia HL-60 cells. The replacement of the hydroxyl group of GA with a carbonyl group or an oxime group at C-3 position does not influence the antiproliferative effect. However, the antiproliferative and apoptosis induction abilities of the compounds with a replaced alkoxyimino group at position C-3 and a free C-29 carboxyl group are markedly increased. (c) 2007 Elsevier Ltd. All rights reserved.
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