Journal of Natural Medicines ( IF 2.5 ) Pub Date : 2021-07-10 , DOI: 10.1007/s11418-021-01542-w Yukio Hitotsuyanagi 1
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The 14-membered cycloisodityrosine is the core structure of RA-series antitumor bicyclic peptides obtained from Rubia plants (Rubiaceae). In this study, an efficient method for the synthesis of cycloisodityrosines from commercially available l-tyrosine derivatives was developed. Using synthetic cycloisodityrosines and cycloisodityrosines with modified structures, several RA-VII analogues were designed and synthesized to explore structure–activity relationships of the cycloisodityrosine moiety of the RA-series peptides, and newly isolated natural peptides were synthesized to establish their structures.
Graphic abstract
中文翻译：
RA-VII类似物的设计与合成——一种来自茜草的抗肿瘤双环六肽
14 元环异酪氨酸是从茜草属植物（茜草科）获得的 RA 系列抗肿瘤双环肽的核心结构。在这项研究中，开发了一种从市售l-酪氨酸衍生物合成环异酪氨酸的有效方法。使用合成的环异酪氨酸和具有修饰结构的环异酪氨酸，设计和合成了几种 RA-VII 类似物以探索 RA 系列肽的环异酪氨酸部分的构效关系，并合成新分离的天然肽以建立其结构。
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