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新型吡唑并[4,3-e][1,2,4]三嗪磺酰胺衍生物的合成及激酶抑制活性。

Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.

机构信息

Department of Chemistry, Siedlce University of Natural Sciences and Humanities, ul. 3 Maja 54, Siedlce 08-110, Poland.

Centre of the Region Haná for Biotechnological and Agricultural Research, Laboratory of Growth Regulators, Faculty of Science, Palacký University, Šlechtitelů 11, 783 71 Olomouc, Czech Republic.

出版信息

Eur J Med Chem. 2014 May 6;78:217-24. doi: 10.1016/j.ejmech.2014.03.054. Epub 2014 Mar 18.

DOI:10.1016/j.ejmech.2014.03.054
PMID:24681986
Abstract

A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine has been synthesized and characterized. Their anticancer activity was tested in vitro against multiple human cancer cell lines and were found to have dose-dependent antiproliferative effects. Furthermore, some of the new compounds inhibited the Abl protein kinase with low micromolar IC50 values and exhibited selective activity against the Bcr-Abl positive K562 and BV173 cell lines, providing starting points for the further development of this new kinase inhibitor scaffold.

摘要

已合成并表征了一系列吡唑并[4,3-e][1,2,4]三嗪的磺酰胺衍生物。它们在体外对多种人癌细胞系的抗癌活性进行了测试，结果表明它们具有剂量依赖性的抗增殖作用。此外，一些新化合物以低微摩尔的 IC50 值抑制 Abl 蛋白激酶，并对 Bcr-Abl 阳性的 K562 和 BV173 细胞系表现出选择性活性，为进一步开发这种新的激酶抑制剂骨架提供了起点。

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