145325-40-2Relevant articles and documents
Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
Balo, Timea,Berger, Sylvie,Cattin, Marie-Elodie,Faucher, Nicolas,Kiss, Arpad,Kotschy, Andras,Paysant, Jérome,Raimbaud, Eric,Sapi, Attila
, (2022/03/03)
Bicyclic heteroaromatic motifs with hydrogen bond donor–acceptor hinge binder motifs are frequently used as ATP-mimetic kinase inhibitors. Althought the thieno[2,3-c]pyridine scaffold also meets these criteria its use was limited so far by the availability of synthetic building blocks. Inspired by two X-ray structures of kinase bound thieno[2,3-c]pyridines we prepared a diverse collection of simple thieno[2,3-c]pyridine derivatives that could serve as starting points for future drug discovery programs. In our search for inhibitors of the GRK2 kinase we also identified a hit compound bearing the thieno[2,3-c]pyridine moiety. Following a structure-driven optimization process a collection of potent and highly ligand efficient inhibitors were prepared and characterized, which could form the basis of a future drug discovery program. Graphical abstract: [Figure not available: see fulltext.]
AMPK INHIBITORS
-
Page/Page column 58, (2019/06/17)
The 5'-AMP-activated protein kinase AMPK functions as a master switch to maintain cellular and whole-body energy homeostasis and abnormal activity profiles of AMPK may cause pathological disorders. The present invention relates to a series of compounds (I
AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
-
Page/Page column 135, (2013/09/12)
The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.