1174765-73-1Relevant articles and documents
Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
Kaplan, Joshua,Verheijen, Jeroen C.,Brooijmans, Natasja,Toral-Barza, Lourdes,Hollander, Irwin,Yu, Ker,Zask, Arie
scheme or table, p. 640 - 643 (2010/06/14)
The morpholine hinge-region binding group on a series of pyrazolopyrimidine and thienopyrimidine mammalian target of rapamycin (mTOR) inhibitors was replaced with 3,6-dihydro-2H-pyran (DHP), giving compounds of equivalent potency and selectivity versus PI3K. These results establish the DHP group as a hinge-region binding motif for the preparation of highly potent and selective mTOR inhibitors.