期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 -, 页码 171-183出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.10.006
关键词
Microwave-assisted chemistry; Dimroth rearrangement; Thieno[3,2-d]pyrimidine; Dimethylformamide dimethylacetal; Kinase inhibitor; Alzheimer's disease
资金
- Region Haute-Normandie
- ISCE-CHEM program
- Fonds Unique Interministeriel (FUI) PHARMASEA project
- Association France-Alzheimer (Finistere)
- CRITT-Sante Bretagne
A useful and rapid access to libraries of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues was designed and optimized for the first time via microwave-accelerated condensation and Dimroth rearrangement of the starting anilines with N'-(2-cyanoaryl)-N,N-dimethylformimidamides obtained by reaction of thiophene precursors with dimethylformamide dimethylacetal. The inhibitory potency of the final products against five protein kinases (CDK5/p25, CK1 delta/epsilon, GSK3 alpha/beta, DYRK1A and CLK1) was estimated. N-arylpyrido[3',2':4,5]thieno[3,2-dlpyrimidin-4-amine series of compounds (4a-j) turned out to be particularly promising for the development of new pharmacological inhibitors of CK1 and CLK1 kinases. (C) 2012 Elsevier Masson SAS. All rights reserved.
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