877994-06-4Relevant articles and documents
Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors
Kendall, Jackie D.,O'Connor, Patrick D.,Marshall, Andrew J.,Frédérick, Rapha?l,Marshall, Elaine S.,Lill, Claire L.,Lee, Woo-Jeong,Kolekar, Sharada,Chao, Mindy,Malik, Alisha,Yu, Shuqiao,Chaussade, Claire,Buchanan, Christina,Rewcastle, Gordon W.,Baguley, Bruce C.,Flanagan, Jack U.,Jamieson, Stephen M.F.,Denny, William A.,Shepherd, Peter R.
, p. 69 - 85 (2012/03/08)
We have made a novel series of pyrazolo[1,5-a]pyridines as PI3 kinase inhibitors, and demonstrated their selectivity for the p110α isoform over the other Class Ia PI3 kinases. We investigated the SAR around the pyrazolo[1,5-a]pyridine ring system, and found compound 5x to be a particularly potent example (p110α IC50 0.9 nM). This compound inhibits cell proliferation and phosphorylation of Akt/PKB, a downstream marker of PI3 kinase activity, and showed in vivo activity in an HCT-116 human xenograft model.
Bicyclic melatonin receptor agonists containing a ring-junction nitrogen: Synthesis, biological evaluation, and molecular modeling of the putative bioactive conformation
Elsner, Jan,Boeckler, Frank,Davidson, Kathryn,Sugden, David,Gmeiner, Peter
, p. 1949 - 1958 (2007/10/03)
Employing 1,3-dipolar cycloaddition for the synthesis of the 7a-azaindole nucleus, analogues of melatonin have been synthesized and tested against human and amphibian melatonin receptors. Introducing a phenyl substituent in position 2 of the heterocyclic