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Issue 9, 2011
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Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors

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Abstract

The synthesis of several novel 4-azaindoles was carried out by novel Fischer reaction which offers as a main advantage, the synthesis of the bisfunctionalized 4-azaindolic building block in one step. The final compounds were evaluated on a panel of 5 kinases in order to evaluate their selectivity and on 7 cancer cell lines to determine their cytotoxic effects. RAF-1 and DYRK1A inhibitions were found, docking studies explain fully the results.

Graphical abstract: Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors

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Publication details

The article was received on 30 May 2011, accepted on 03 Jul 2011 and first published on 03 Aug 2011


Article type: Concise Article
DOI: 10.1039/C1MD00141H
Med. Chem. Commun., 2011,2, 899-903

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    Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors

    F. Pin, F. Buron, F. Saab, L. Colliandre, S. Bourg, F. Schoentgen, R. Le Guevel, C. Guillouzo and S. Routier, Med. Chem. Commun., 2011, 2, 899
    DOI: 10.1039/C1MD00141H

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