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ID: ALA3992503
Journal: Eur J Med Chem
Title: Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy.
Authors: Wang HB, Jin XL, Zheng JF, Wang F, Dai F, Zhou B.
Abstract: We report a case of successful design of glutathione S-transferase (GST) inhibitors via a natural product-inspired and electrophilicity-based strategy. Based on this strategy, a novel piperlongumine analog (PL-13) bearing a para-trifluoromethyl group and an α-chlorine on its aromatic and lactam rings, respectively, surfaced as a promising GST inhibitor, thereby overcoming cisplatin resistance in lung cancer A549 cells.
CiteXplore: 27914365