کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1394434 | 1501158 | 2012 | 13 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors Synthesis and biological evaluation of N-arylbenzo[b]thieno[3,2-d]pyrimidin-4-amines and their pyrido and pyrazino analogues as Ser/Thr kinase inhibitors](/preview/png/1394434.png)
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, CK1δ/ɛ, GSK3α/β, DYRK1A and CLK1) was estimated. N-arylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-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.
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► Synthesis of 40 novel tricyclic thieno[3,2-d]pyrimidin-4-amines.
► The inhibitory potency of the final products against five kinases was evaluated.
► Three compounds are promising as new inhibitors of CK1 and CLK1 kinases.
Journal: European Journal of Medicinal Chemistry - Volume 58, December 2012, Pages 171–183