1414524-13-2Relevant academic research and scientific papers
Efficient new synthesis of N-arylbenzo[b]furo[3,2-d]pyrimidin-4-amines and their benzo[b]thieno[3,2-d]pyrimidin-4-amine analogues via a microwave-assisted Dimroth rearrangement
Loidreau, Yvonnick,Dubouilh-Benard, Carole,Marchand, Pascal,Nourrisson, Marie-Renee,Duflos, Muriel,Buquet, Catherine,Corbiere, Cecile,Besson, Thierry
, p. 1187 - 1197 (2013/10/21)
A useful and rapid access to libraries of N-arylbenzo[b]furo[3,2-d] pyrimidin-4-amines (1) and their novel benzo[b]thieno[3,2-d]pyrimidin-4-amine analogues (2) was investigated for the first time. Title compounds were obtained via microwave-accelerated co
Synthesis and evaluation of apoptosis induction of thienopyrimidine compounds on KRAS and BRAF mutated colorectal cancer cell lines
Pedeboscq, Stephane,Pometan, Jean-Paul,Gravier, Denis,Casadebaig, Francoise,Hou, Genevieve,Gissot, Arnaud,Rey, Christophe,Ichas, Francois,Giorgi, Francesca De,Lartigue, Lydia
, p. 6724 - 6731,8 (2012/12/12)
Monoclonal antibodies (MoAb) and tyrosine kinase inhibitors (TKI) targeting the EGFR (Epidermal Growth Factor Receptor) pathways are currently used in colorectal cancer treatment. Despite the improvement of median overall survival, resistance is observed
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.
