1328362-87-3Relevant academic research and scientific papers
Discovery of potent antiproliferative agents targeting EGFR tyrosine kinase based on the pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4-amine scaffold
Aziz, Yasmine Mohamed Abdel,Said, Mohamed Mokhtar,El Shihawy, Hosam Ahmed,Tolba, Mai Fathy,Abouzid, Khaled Abouzid Mohamed
, p. 1015 - 1028 (2015)
A series of pyridothieno[3,2-d]pyrimidin-4-amines was designed and synthesized as congeners to the classical 4-anilinoquinazolines as ATP-competitive epidermal growth factor receptor (EGFR) inhibitors. Compound 5a exhibited the most potent and selective i
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
Loidreau, Yvonnick,Marchand, Pascal,Dubouilh-Benard, Carole,Nourrisson, Marie-Renée,Duflos, Muriel,Lozach, Olivier,Loa?c, Nadège,Meijer, Laurent,Besson, Thierry
, p. 171 - 183 (2013/02/22)
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/ε, 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.
