Design, synthesis, and structure-activity relationships of haloenol lactones: site-directed and isozyme-selective glutathione S-transferase inhibitors

…, H Jiang, K Chen, P Zimniak, J Zheng

Index: Wu, Zhixing; Minhas, Gurpreet Singh; Wen, Dingyi; Jiang, Hualiang; Chen, Kaixian; Zimniak, Piotr; Zheng, Jiang Journal of Medicinal Chemistry, 2004 , vol. 47, # 12 p. 3282 - 3294

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Citation Number: 61

Abstract

Overexpression of glutathione S-transferase (GST), particularly the GST-π isozyme, has been proposed to be one of the biochemical mechanisms responsible for drug resistance in cancer chemotherapy, and inhibition of overexpressed GST has been suggested as an approach to combat GST-induced drug resistance. 3-Cinnamyl-5 (E)- bromomethylidenetetrahydro-2-furanone (1a), a lead compound of site-directed GST-π ...