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Accueil > Publications > Recherche par années > Années 2010 > 2011

Pin, F., Buron, F., Saab, F., Colliandre, L., Bourg, S., Schoentgen, F., Le Guevel, R., Guillouzo, C. and Routier, S.

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

Medchemcomm 2 (9) 899-903

par Frapart - publié le

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.