Design, synthesis, cytoselective toxicity, structure–activity relationships, and pharmacophore of thiazolidinone derivatives targeting drug-resistant lung cancer cells

…, S Wu, S Zhai, A Liu, Y Sun, R Li, Y Zhang…

文献索引：Zhou, Hongyu; Wu, Shuhong; Zhai, Shumei; Liu, Aifeng; Sun, Ying; Li, Rongshi; Zhang, Ying; Ekins, Sean; Swaan, Peter W.; Fang, Bingliang; Zhang, Bin; Yan, Bing Journal of Medicinal Chemistry, 2008 , vol. 51, # 5 p. 1242 - 1251

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被引用次数: 135

摘要

Ten cytoselective compounds have been identified from 372 thiazolidinone analogues by applying iterative library approaches. These compounds selectively killed both non-small cell lung cancer cell line H460 and its paclitaxel-resistant variant H460taxR at an IC50 between 0.21 and 2.93 µM while showing much less toxicity to normal human fibroblasts at concentrations up to 195 µM. Structure–activity relationship studies revealed that (1) the ...