Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins

Rufine Akué-Gédu (1) , Eric Debiton (2) , Yoan Ferandin (3) , Laurent Meijer (3) , Michelle Prudhomme (1) , Fabrice Anizon (1) , Pascale Moreau (1)

1 SEESIB - Synthèse et étude de systèmes à intêret biologique
2 UNICANCER/CJP - Centre Jean Perrin [Clermont-Ferrand]
3 MCT - Molécules et cibles thérapeutiques

The synthesis of new meridianin derivatives substituted at the C-5 position of the 2-aminopyrimidine ring by various aryl groups and substituted or not by a methyl group on the indole nitrogen is described. These compounds were tested for their kinase inhibitory potencies toward five kinases (CDK5/p25, CK1δ/ε, GSK-3α/β, Dyrk1A and Erk2) as well as their in vitro antiproliferative activities toward a human fibroblast primary culture and two human solid cancer cell lines (MCF-7 and PA 1)

Mots clés: Meridianins; Suzuki cross-coupling; Kinase inhibitors; Dyrk1A inhibitors

Domaines: Chimie thérapeutique

Rufine Akué-Gédu, Eric Debiton, Yoan Ferandin, Laurent Meijer, Michelle Prudhomme, et al.. Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins. Bioorganic and Medicinal Chemistry, 2009, 17, pp.4420-4424. ⟨hal-00392799⟩