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Issue 20, 2013
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Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitors

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Abstract

Pyrazolo[4,3-b]indole derivatives have been designed as novel CK2 inhibitor compounds based on the binding mode analysis of a previously reported phenylpyrazole-type CK2 inhibitor. A series of pyrazolo[4,3-b]indoles and related dihydropyrazolo[4,3-b]indoles were efficiently prepared from simple starting materials using a gold-catalysed three-component annulation reaction as a key step. Several of the newly synthesized compounds displayed high levels of inhibitory activity, indicating that the pyrazolo[4,3-b]indole core represents a promising scaffold for the development of potent CK2 inhibitors.

Graphical abstract: Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitors

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Publication details

The article was received on 31 Jan 2013, accepted on 07 Mar 2013 and first published on 11 Mar 2013


Article type: Paper
DOI: 10.1039/C3OB40223A
Citation: Org. Biomol. Chem., 2013,11, 3288-3296
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    Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitors

    Z. Hou, S. Oishi, Y. Suzuki, T. Kure, I. Nakanishi, A. Hirasawa, G. Tsujimoto, H. Ohno and N. Fujii, Org. Biomol. Chem., 2013, 11, 3288
    DOI: 10.1039/C3OB40223A

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