Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy
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.
Wang, Hai-Bo,Jin, Xiao-Ling,Zheng, Jia-Fang,Wang, Fu,Dai, Fang,Zhou, Bo
Compounds, Compositions, and Methods for Cancer Therapy
Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.
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Paragraph 0125; 0148
(2014/02/16)
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