Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 8, Pages 2633-2639Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.031
Keywords
glycyrrhetinate analogs; growth inhibition; bladder cancer; pancreatic cancer
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Funding
- NCI NIH HHS [R01 CA108718, CA108718, R01 CA108718-04, R01 CA108718-03] Funding Source: Medline
- NIEHS NIH HHS [P30 ES009106, ES09106, P30 ES009106-09] Funding Source: Medline
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Derivatives of oleanolic acid, ursolic acid and glycyrrhetinic acid substituted with electron-withdrawing groups at the 2-position in the A-ring which also contains a 1-en-3-one structure are potent inhibitors of cancer cell growth. In this study, we have compared the effects of several 2-substituted analogs of triterpenoid acid methyl esters derived from ursolic and glycyrrhetinic acid on proliferation of KU7 and 253JB-V bladder and Panc-1 and Panc-28 pancreatic cancer cells. The results show that the 2-cyano and 2-trifluoromethyl derivatives were the most active compounds. The glycyrrhetinic acid derivatives with the rearranged C-ring containing the 9( 11)-en-12-one structure were generally more active than the corresponding 12-en-11-one isomers. However, differences in growth inhibitory IC(50) values were highly variable and dependent on the 2-substituent (CN vs CF(3)) and cancer cell context. (c) 2008 Elsevier Ltd. All rights reserved.
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