title: Synthesis and biological activities of aminopyrimidyl-indoles structurally related to meridianins.
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).
authors.affiliation: Clermont Université, Université Blaise Pascal, SEESIB, Aubière, France.
authors.forename: Rufine
authors.initials: R
authors.lastname: Akue-Gedu
authors.forename: Eric
authors.initials: E
authors.lastname: Debiton
authors.forename: Yoan
authors.initials: Y
authors.lastname: Ferandin
authors.forename: Laurent
authors.initials: L
authors.lastname: Meijer
authors.forename: Michelle
authors.initials: M
authors.lastname: Prudhomme
authors.forename: Fabrice
authors.initials: F
authors.lastname: Anizon
authors.forename: Pascale
authors.initials: P
authors.lastname: Moreau
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002478:Cells, Cultured; D005347:Fibroblasts / Q000166:cytology; D006801:Humans; D026121:Indole Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011494:Protein Kinases / Q000378:metabolism*; D051381:Rats; D013329:Structure-Activity Relationship; D013552:Swine
chemical_list: D026121:Indole Alkaloids; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases