RA-VII四肽亚基和脱氧紫金牛素的关键类似物。

Key analogues of the tetrapeptide subunit of RA-VII and deoxybouvardin.

作者信息

Boger D L, Zhou J

机构信息

Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, USA.

出版信息

Bioorg Med Chem. 1996 Oct;4(10):1597-603. doi: 10.1016/0968-0896(96)00151-4.

DOI:10.1016/0968-0896(96)00151-4

PMID:8931929

Abstract

The synthesis and evaluation of the analogues 3 and 4 of deoxybouvardin (1) and RA-VII (2), which contain modifications in the tetrapeptide subunit, are described. Unlike the natural products and similar to our prior disclosure, the agents 3 and 4, which substitute (Gly)4 and (Gly)3 for the D-Ala-Ala-NMe-Tyr(OMe)-Ala tetrapeptide subunit, exist in single rigid conformations in which the central cycloisodityrosine amide adopts its preferred trans stereochemistry and both were found to be biologically inactive.

摘要

本文描述了脱氧布法地丁（1）和RA-VII（2）的类似物3和4的合成与评价，这些类似物在四肽亚基上有修饰。与天然产物不同且与我们之前的公开内容相似，用（Gly）4和（Gly）3取代D-Ala-Ala-NMe-Tyr（OMe）-Ala四肽亚基的类似物3和4以单一刚性构象存在，其中中央环异酪氨酸酰胺采取其优选的反式立体化学，并且发现两者均无生物活性。