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Chetracins E and F, cytotoxic epipolythiodioxopiperazines from the marine-derived fungus Acrostalagmus luteoalbus HDN13-530

机译:源自海洋真菌 Acrostalagmus luteoalbus HDN13-530的细胞毒素E和F,细胞毒素表聚硫代二氧杂哌嗪

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Two new epipolythiodioxopiperazines, named chetracins E and F (1 and 2), along with the known chetracin C (3), were isolated from the fungus Acrostalagmus luteoalbus HDN13-530. Their structures were elucidated based on the NMR, MS and CD data, as well as chemical conversion. All of the compounds exhibited cytotoxicity against the tested five cancer lines in low-micromolar or nanomolar IC50 values. The computational docking indicated that compounds 1–3 could bind to the C-terminal of heat shock protein 90 (Hsp90), which was in line with the experimental observation of decreases in levels and active forms of Hsp90 client proteins.
机译:从真菌 Acrostalagmus luteoalbus HDN13-530中分离出两种新的表聚硫代二氧杂哌嗪,分别称为chetracins E和F(1和2)以及已知的螯合霉素C(3)。根据NMR,MS和CD数据以及化学转化率阐明了它们的结构。所有化合物均以低微摩尔或纳摩尔IC 50 值显示出对所测试的5种癌症细胞系的细胞毒性。计算对接表明,化合物1-3可与热休克蛋白90(Hsp90)的C末端结合,这与对Hsp90客户蛋白水平和活性形式降低的实验观察一致。

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