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新型 4,4'-联吡啶-5,5'-全氟烷基-2,2'-联恶唑双吡啶盐的合成及生物活性。

Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles.

机构信息

Departamento de Ciencias, Escuela Politécnica, Universidad Europea de Madrid, Villaviciosa de Odón 28670, Madrid, Spain.

出版信息

Eur J Med Chem. 2011 Nov;46(11):5662-7. doi: 10.1016/j.ejmech.2011.09.046. Epub 2011 Oct 2.

Abstract

A series of bispyridinium compounds were synthesized by a short sequence of reactions from symmetric diamides. All compounds were tested for their antiproliferative activity against HT-29, a cell line derived from a human colon adenocarcinoma, and their inhibitory activity against choline kinase (ChoK), a novel anticancer molecular target already in clinical trials. Most of the compounds analyzed showed good antiproliferative activities, in the micromolar range, with the identification of promising lead molecules as a new family of potential inhibitors of ChoK.

摘要

一系列双吡啶化合物是由对称二酰胺通过短序列反应合成的。所有化合物均针对源自人结肠腺癌的 HT-29 细胞系进行了抗增殖活性测试,并针对胆碱激酶 (ChoK) 进行了抑制活性测试,ChoK 是一种已进入临床试验的新型抗癌分子靶标。分析的大多数化合物均表现出良好的抗增殖活性,在微摩尔范围内,确定了有前途的先导分子,它们是 ChoK 的新型潜在抑制剂家族。

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