Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors - CNRS - Centre national de la recherche scientifique Accéder directement au contenu
Article Dans Une Revue MedChemComm Année : 2011

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

Résumé

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.
Fichier non déposé

Dates et versions

hal-00720699 , version 1 (25-07-2012)

Identifiants

Citer

Frédéric Pin, Frédéric Buron, Fabienne Saab, Lionel Colliandre, Stéphane Bourg, et al.. Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors. MedChemComm, 2011, 2 (9), pp.899-903. ⟨10.1039/c1md00141h⟩. ⟨hal-00720699⟩
258 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More