Noé Osorio Reineke, Franziska A. V. Elsen, Hanusch A. Grab, Dietrich Mostert, Stephan A. Sieber and Thorsten Bach
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引用次数: 0
摘要
在本文中,我们介绍了全合成反肽类化合物 vioprolide B 及其类似物的方法,其中 (E)-dehydrobutyrine 氨基酸被甘氨酸取代。在生物试验中对这些化合物进行了研究,结果表明,vioprolide B 可能通过与延伸因子 eEF1A1 和染色质组装因子 CHAF1A 的半胱氨酸残基共价结合而具有细胞毒性。
Synthesis and biological evaluation of vioprolide B and its dehydrobutyrine-glycine analogue†
Herein, we describe the total synthesis of the depsipeptide vioprolide B and of an analogue, in which the (E)-dehydrobutyrine amino acid was replaced by glycine. The compounds were studied in biological assays which revealed cytotoxicity solely for vioprolide B presumably by covalent binding to cysteine residues of elongation factor eEF1A1 and of chromatin assembly factor CHAF1A.
期刊介绍:
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