345264-16-6Relevant academic research and scientific papers
Substituted 3-imidazo[1,2-a]pyridin-3-yl-4-(1,2,3,4-tetrahydro-[1,4] diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3
Engler, Thomas A.,Henry, James R.,Malhotra, Sushant,Cunningham, Brian,Furness, Kelly,Brozinick, Joseph,Burkholder, Timothy P.,Clay, Michael P.,Clayton, Joshua,Diefenbacher, Clive,Hawkins, Eric,Iversen, Philip W.,Li, Yihong,Lindstrom, Terry D.,Marquart, Angela L.,McLean, Johnathan,Mendel, David,Misener, Elizabeth,Briere, Daniel,O'Toole, John C.,Porter, Warren J.,Queener, Steven,Reel, Jon K.,Owens, Rebecca A.,Brier, Richard A.,Eessalu, Thomas E.,Wagner, Jill R.,Campbell, Robert M.,Vaughn, Renee
, p. 3934 - 3937 (2007/10/03)
Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose similar to insulin, making GSK3 an attractive target for the treatment of type 2 diabetes. Herein we report the discovery of a series of potent and selective GSK3 inhibitors. Compounds 7-12 show oral activity in an in vivo model of type II diabetes, and 9 and 12 have desirable PK properties.
Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors
Al-awar, Rima S.,Ray, James E.,Hecker, Kyle A.,Joseph, Sajan,Huang, Jianping,Shih, Chuan,Brooks, Harold B.,Spencer, Charles D.,Watkins, Scott A.,Schultz, Richard M.,Considine, Eileen L.,Faul, Margaret M.,Sullivan, Kevin A.,Kolis, Stanley P.,Carr, Michael A.,Zhang, Faming
, p. 3925 - 3928 (2007/10/03)
The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon carcinoma cell line and proved to be good antiproliferative agents.
