设计并合成结构简化的紫檀芪类似物及其与微管相互作用的研究。

Design and synthesis of pironetin analogues with simplified structure and study of their interactions with microtubules.

机构信息

Department de Q. Orgánica, University de Valencia, c/ D. Moliner 50, E-46100 Burjassot, Valencia, Spain.

出版信息

Eur J Med Chem. 2011 May;46(5):1630-7. doi: 10.1016/j.ejmech.2011.02.011. Epub 2011 Feb 22.

DOI:10.1016/j.ejmech.2011.02.011

Abstract

The preparation of a series of pironetin analogues with simplified structure is described. Their cytotoxic activity and their interactions with tubulin have been investigated. It has been found that, while less active than the parent molecule, the pironetin analogues still share the mechanism of action of the latter and compete for the same binding site to α-tubulin. Variations in the configurations of their stereocenters do not translate into relevant differences between biological activities.

摘要

本文描述了一系列结构简化的紫檀芪类似物的制备，并研究了它们的细胞毒性活性及其与微管蛋白的相互作用。结果发现，虽然这些紫檀芪类似物的活性比母体分子低，但它们仍然具有后者的作用机制，并与α-微管蛋白竞争相同的结合位点。它们手性中心的构型变化并没有转化为生物活性的相关差异。