1383659-91-3Relevant academic research and scientific papers
Exploring kinase inhibition properties of 9hpyrimido[5,4-b]- and [4,5-b]indol-4-amine derivatives
Loidreau, Yvonnick,Dubouilh-Benard, Carole,Nourrisson, Marie-Renée,Loa?c, Nadège,Meijer, Laurent,Besson, Thierry,Marchand, Pascal
, (2020/05/29)
We previously highlighted the interest in 6,5,6-fused tricyclic analogues of 4-aminoquinazolines as kinase inhibitors in the micromolar to the nanomolar range of IC50 values. For the generation of chemical libraries, the formamide-mediated cyclization of the cyanoamidine precursors was carried out under microwave irradiation in an eco-friendly approach. In order to explore more in-depth the pharmacological interest in such tricyclic skeletons, the central five member ring, i.e., thiophène or furan, was replaced by a pyrrole to afford 9H-pyrimido[5,4-b]- and [4,5-b]indol-4-amine derivatives inspired from harmine. The inhibitory potency of the final products was determined against four protein kinases (CDK5/p25, CK1δ/ε, GSK3α/β and DYRK1A). As a result, we have identified promising compounds targeting CK1δ/ε and DYRK1A and displaying micromolar and submicromolar IC50 values.
Study of N1-alkylation of indoles from the reaction of 2(or 3)-aminoindole-3-(or 2)carbonitriles with DMF-dialkylacetals
Loidreau, Yvonnick,Melissen, Sigismund,Levacher, Vincent,Loge, Cedric,Graton, Jerome,Le Questel, Jean-Yves,Besson, Thierry
experimental part, p. 4916 - 4925 (2012/07/28)
The condensation of 2-aminoindole-3-carbonitriles and their 3-aminoindole-2-carbonitrile isomers with various DMF-dialkoxyacetals was investigated under microwaves. The appearance of reactive and versatile alkoxyiminium species allowed convenient access t
