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CK2 alpha and CK2 alpha ' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives

  作者 Janeczko, M; Orzeszko, A; Kazimierczuk, Z; Szyszka, R; Baier, A  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2012年47-1;  页码  345-350  
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[摘要]The goal of this study was to test the inhibitory activity of a series of tetrahalogenobenzimidazoles, including a number of novel derivatives, on individual catalytic subunits of human CK2. 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazoles and their newly obtained N(1)- and 2-S-carboxyalkyl derivatives showed potent inhibitory activity against both these subunits. CK2 alpha' was up to 6 times more sensitive to the studied compounds than CK2 alpha. The investigated iododerivatives showed, in most cases, stronger inhibitory properties than the respective brominated congeners, but the differences showed considerable dependence on the protein substrate used. (C) 2011 Elsevier Masson SAS. All rights reserved.

 
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