Vioprolide B 及其脱氢丁炔甘氨酸类似物的合成与生物学评价

IF 4.2 2区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
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。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis and biological evaluation of vioprolide B and its dehydrobutyrine-glycine analogue†

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.

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来源期刊
Chemical Communications
Chemical Communications 化学-化学综合
CiteScore
8.60
自引率
4.10%
发文量
2705
审稿时长
1.4 months
期刊介绍: ChemComm (Chemical Communications) is renowned as the fastest publisher of articles providing information on new avenues of research, drawn from all the world''s major areas of chemical research.
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