1033743-21-3Relevant articles and documents
Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor
Heffron, Timothy P.,Berry, Megan,Castanedo, Georgette,Chang, Christine,Chuckowree, Irina,Dotson, Jennafer,Folkes, Adrian,Gunzner, Janet,Lesnick, John D.,Lewis, Cristina,Mathieu, Simon,Nonomiya, Jim,Olivero, Alan,Pang, Jodie,Peterson, David,Salphati, Laurent,Sampath, Deepak,Sideris, Steve,Sutherlin, Daniel P.,Tsui, Vickie,Wan, Nan Chi,Wang, Shumei,Wong, Susan,Zhu, Bing-yan
scheme or table, p. 2408 - 2411 (2010/07/16)
Efforts to identify potent small molecule inhibitors of PI3 kinase and mTOR led to the discovery of the exceptionally potent 6-aryl morpholino thienopyrimidine 6. In an effort to reduce the melting point in analogs of 6, the thienopyrimidine was modified by the addition of a methyl group to disrupt planarity. This modification resulted in a general improvement in in vivo clearance. This discovery led to the identification of GNE-477 (8), a potent and efficacious dual PI3K/mTOR inhibitor.
PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page/Page column 255, (2008/06/13)
Compounds of Formulas (Ia) and (Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula (Ia) and (Ib) for in vitro, in situ, and in vivodiagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
