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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles.
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Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles.

机译:4,4'-双吡啶基-5,5'-全氟烷基-2,2'-双恶唑的新双吡啶鎓盐的合成及生物活性。

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摘要

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.
机译:通过对称的二酰胺的短序列反应合成了一系列双吡啶鎓化合物。测试了所有化合物的抗HT-29(一种源自人类结肠腺癌的细胞系)的抗增殖活性,以及​​它们对胆碱激酶(ChoK)的抑制活性,ChoK是一种已经在临床试验中的新型抗癌分子靶标。分析的大多数化合物在微摩尔范围内均显示出良好的抗增殖活性,并且鉴定出有前途的先导分子作为ChoK潜在抑制剂的新家族。

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