1190312-37-8Relevant articles and documents
Design of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats
Bengtsson, Christoffer,Blaho, Stefan,Saitton, David Blomberg,Brickmann, Kay,Broddefalk, Johan,Davidsson, ?jvind,Drmota, Tomas,Folmer, Rutger,Hallberg, Kenth,Hallén, Stefan,Hovland, Ragnar,Isin, Emre,Johannesson, Petra,Kull, Bengt,Larsson, Lars-Olof,L?fgren, Lars,Nilsson, Kristina E.,Noeske, Tobias,Oakes, Nick,Plowright, Alleyn T.,Schnecke, Volker,Sthlberg, Pernilla,S?rme, Pernilla,Wan, Hong,Wellner, Eric,?ster, Linda
, p. 3039 - 3053 (2011/06/27)
Inhibition of acetyl-CoA carboxylases has the potential for modulating long chain fatty acid biosynthesis and mitochondrial fatty acid oxidation. Hybridization of weak inhibitors of ACC2 provided a novel, moderately potent but lipophilic series. Optimization led to compounds 33 and 37, which exhibit potent inhibition of human ACC2, 10-fold selectivity over inhibition of human ACC1, good physical and in vitro ADME properties and good bioavailability. X-ray crystallography has shown this series binding in the CT-domain of ACC2 and revealed two key hydrogen bonding interactions. Both 33 and 37 lower levels of hepatic malonyl-CoA in vivo in obese Zucker rats.
NOVEL DERIVATIVES OF PYRROLOINDOLE WHICH ARE INHIBITORS OF HSP90, COMPOSITIONS CONTAINING SAME, AND USE THEREOF
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, (2011/08/06)
Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R′1 which are the same or different; R is