Issue 9, 2011
From the journal:

MedChemComm

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

Frédéric Pin,a   Frédéric Buron,a   Fabienne Saab,a   Lionel Colliandre,a   Stéphane Bourg,b   Françoise Schoentgen,c   Remy Le Guevel,d   Christiane Guillouzod  and  Sylvain Routier*a  

* Corresponding authors

a ICOA, University of Orleans, UMR CNRS 6005, Rue de Chartres, BP 6759, Orleans Cedex 2, France
E-mail: sylvain.routier@univ-orleans.fr
Fax: +33-238-417-354
Tel: +33-238-417-354

b Fédération de Recherche “Physique et Chimie du Vivant”, FR CNRS 2708, Rue de Charles Sadron, Orleans Cedex 2, France

c IMPMC UMR 7590 CNRS, University of Pierre et Marie Curie-Paris 6, Campus Jussieu, boîte courrier 115, 4 Place Jussieu, Paris Cedex 05, France

d Hôpital de Pontchaillou, INSERM U-522, Rennes Cedex, France

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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Article information

DOI
https://doi.org/10.1039/C1MD00141H
Article type
Concise Article
Submitted
30 May 2011
Accepted
03 Jul 2011
First published
03 Aug 2011

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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