Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins
Rufine Akue-Gedu1, Eric Debiton, Yoan Ferandin
1Clermont Université, Université Blaise Pascal, SEESIB, Aubière, France.
Abstract:
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, CK1delta/epsilon, GSK-3alpha/beta, 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).
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