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Issue 25, 2012
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Design and synthesis of a novel class of CK2 inhibitors: application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles

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Abstract

Two classes of fused nitrogen heterocycles were designed as CK2 inhibitor candidates on the basis of previous structure–activity relationship (SAR) studies. Various dipyrrolo[3,2-b:2′,3′-e]pyridine and benzo[g]indazole derivatives were prepared using transition-metal-catalysed cascade and/or multicomponent reactions. Biological evaluation of these candidates revealed that benzo[g]indazole is a promising scaffold for potent CK2 inhibitors. The inhibitory activities on cell proliferation of these potent CK2 inhibitors are also presented.

Graphical abstract: Design and synthesis of a novel class of CK2 inhibitors: application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles

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Publication details

The article was received on 10 Feb 2012, accepted on 24 Apr 2012 and first published on 25 Apr 2012


Article type: Paper
DOI: 10.1039/C2OB25298H
Citation: Org. Biomol. Chem., 2012,10, 4907-4915
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    Design and synthesis of a novel class of CK2 inhibitors: application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles

    Y. Suzuki, S. Oishi, Y. Takei, M. Yasue, R. Misu, S. Naoe, Z. Hou, T. Kure, I. Nakanishi, H. Ohno, A. Hirasawa, G. Tsujimoto and N. Fujii, Org. Biomol. Chem., 2012, 10, 4907
    DOI: 10.1039/C2OB25298H

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