1. Academic Validation
  2. The synthesis of alpha,beta-unsaturated carbonyl derivatives with the ability to inhibit both glutathione S-transferase P1-1 activity and the proliferation of leukemia cells

The synthesis of alpha,beta-unsaturated carbonyl derivatives with the ability to inhibit both glutathione S-transferase P1-1 activity and the proliferation of leukemia cells

  • Bioorg Med Chem. 2007 Apr 1;15(7):2701-7. doi: 10.1016/j.bmc.2007.01.037.
Guisen Zhao 1 Chuan Liu Rui Wang Dandan Song Xiaobing Wang Hongxiang Lou Yongkui Jing
Affiliations

Affiliation

  • 1 College of Pharmacy, Shandong University, Ji'nan, Shandong Province 250012, PR China.
Abstract

Ethacrynic acid (EA), an alpha,beta-unsaturated carbonyl compound, is a Glutathione S-transferase P1-1 (GSTP1-1) inhibitor. Twenty-one novel EA derivatives have been synthesized. The effects of these compounds on GSTP1-1 activity and on the proliferation of human leukemia HL-60 cells have been determined. Compounds with a halogen substitution at the 3'-position of the aromatic ring have greater inhibitory effects on GSTP1-1 activity than those of compounds with a methyl substitution there. Compounds with substitutions at both the 2'- and 3'-positions of the aromatic ring have more antiproliferative ability than those with one substitution at 3'-position. Esterification of the carboxyl group appears to increase the antiproliferative ability.

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