Design and synthesis of CK2 inhibitors

被引：15

作者：

Makowska, Malgorzata ^{[2
]}

Lukowska-Chojnacka, Edyta ^{[1
]}

Winska, Patrycja ^{[1
]}

Kus, Agnieszka ^{[1
]}

Bilinska-Chomik, Aleksandra ^{[1
]}

Bretner, Maria ^{[1
,2
]}

机构：

[1] Warsaw Univ Technol, Fac Chem, PL-00664 Warsaw, Poland

[2] PAS, Inst Biochem & Biophys, PL-02106 Warsaw, Poland

来源：

MOLECULAR AND CELLULAR BIOCHEMISTRY | 2011年 / 356卷 / 1-2期

关键词：

4,5,6,7-Tetrabromo-1H-benzotriazole derivatives; 4,5,6,7-Tetrabromo-1H-benzimidazole derivatives; CK2 kinase inhibitors; PROTEIN-KINASE CK2; SQUAMOUS-CELL CARCINOMA; CK2-ALPHA; DERIVATIVES; SUBUNIT;

D O I：

10.1007/s11010-011-0953-8

中图分类号：

Q2 [细胞生物学];

学科分类号：

071009 ; 090102 ;

摘要：

A series of new polybrominated benzimidazoles and benzotriazoles has been synthesized and their influence on the activity of protein kinase CK2 was evaluated. It was revealed that the most active inhibitors are those with methyl or ethyl substituent at benzene ring, namely 5,6,7-tribromo-4-methyl-1H-benzotriazole (38, IC50 0.51 mu M) and 5,6,7-tribromo-4-ethyl-1H-benzotriazole (40, IC50 0.16 mu M). The derivatives with large aromatic or heterocyclic substituents connected to benzimidazole or benzotriazole scaffold appeared to be less potent inhibitors.

引用

页码：91 / 96

页数：6

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