化学
组合化学
固相合成
肽合成
肽
模块化设计
相(物质)
可扩展性
氨基酸
计算生物学
纳米技术
生物化学
计算机科学
有机化学
程序设计语言
生物
材料科学
数据库
作者
Yue Zhang,Alexander A. Vinogradov,Jun Shi Chang,Yuki Goto,Hiroaki Suga
出处
期刊:Organic Letters
[American Chemical Society]
日期:2022-10-25
卷期号:24 (43): 7894-7899
被引量:5
标识
DOI:10.1021/acs.orglett.2c02870
摘要
A strategy for the synthesis of de novo discovered lactazole-like thiopeptides is reported. The approach revolves around a convergent and scalable preparation of the central triheterocyclic amino acid and its utilization in Fmoc solid-phase peptide synthesis for modular peptide chain assembly. A technique for preparing C-terminally functionalized thiopeptides for biological studies is also described. The syntheses of 11 TNIK-inhibitor thiopeptides and 6 of their derivatives in multimilligram quantities highlight the practical utility of the developed protocols.
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