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几种四氢呋喃和螺缩酮衍生物的合成及作为微管活性物质的生物评价。

Synthesis and biological evaluation as microtubule-active agents of several tetrahydrofuran and spiroacetal derivatives.

机构信息

Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, E-12071 Castellón, Spain.

出版信息

Curr Med Chem. 2013;20(9):1173-82. doi: 10.2174/0929867311320090006.

DOI:10.2174/0929867311320090006
PMID:23317099
Abstract

The stereoselective preparation of several molecules containing structural fragments of the tetrahydrofuran and spiroacetal type is described. Their degree of cytotoxicity and their interactions with tubulin have been investigated. It has been confirmed that the tetrahydrofuran derivatives are cytotoxic but, in contrast to previous reports, it has been found that the cytoxicity is not due to interactions with the microtubule network. Furthermore, and also in contrast to a previous report on closely related compounds, the spiroacetal derivatives do show interactions with tubulin, even though the precise mechanism and the binding site still remain to be established.

摘要

本文描述了几种含有四氢呋喃和螺缩酮结构片段的立体选择性分子的制备方法。研究了它们的细胞毒性及其与微管蛋白的相互作用。已经证实,四氢呋喃衍生物具有细胞毒性,但与以前的报道相反,发现细胞毒性不是由于与微管网络的相互作用。此外,与以前关于密切相关化合物的报告相反,螺缩酮衍生物确实与微管蛋白相互作用,尽管确切的机制和结合位点仍有待确定。

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