Nine-Step Total Synthesis and Biological Evaluation of Rhizonin A
Nine-Step Total Synthesis and Biological Evaluation of Rhizonin A
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根茎素A的九步全合成及生物学评价
DOI：
10.1002/cjoc.202000222
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发表时间：
2020
影响因子：
5.4
通讯作者：
Ye Tao
中科院分区：
文献类型：
--
作者：
Liu Qingchao;Liu Langlang;Ratnayake Ranjala;Luesch Hendrik;Guo Yian;Ye Tao
主要观察和结论摘要我们以一种非常简洁和收敛的方式实现了一种结构和生物学上有趣的环状多肽rhizonin A（1）的全合成。该战略路线需要9个最长的线性步骤来将商业上可获得的材料加工成天然产物，总收率为9.7%。化学策略的明智选择促进了序列的简洁和高总产率。Rhizonin A（1）对HCT 116结直肠癌细胞的细胞活力显示出弱抑制作用，并且这种活性依赖于缺氧诱导因子。
Summary of main observation and conclusionWe have achieved the total synthesis of an architecturally and biologically intriguing cyclic polypeptide, rhizonin A (1), in an exceptionally concise and convergent fashion. The strategic route entails 9 longest linear steps to elaborate commercially available materials into the natural product with an overall yield of 9.7%. The brevity of sequence and high overall yield was fueled by the judicious selection of chemical tactics. Rhizonin A (1) showed weak inhibitory effects on the cell viability of HCT116 colorectal cancer cells and this activity was dependent on hypoxia‐inducible factors.