thienopyrimidine and morpholine

thienopyrimidine has been researched along with morpholine* in 2 studies

Other Studies

2 other study(ies) available for thienopyrimidine and morpholine

Article	Year
Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K. Bioorganic & medicinal chemistry letters, 2010, Jan-01, Volume: 20, Issue:1 2-Aryl-4-morpholinothieno[3,2-d]pyrimidines are known PI3K inhibitors. This class of compounds also potently inhibited the homologous enzyme mTOR. Replacement of the morpholine group in these compounds with an 8-oxa-3-azabicyclo[3.2.1]octane group led to mTOR inhibitors with selectivity over PI3K. Optimization of the 2-aryl substituent led to the discovery of 2-(4-ureidophenyl)-thienopyrimidines as highly potent (IC(50) <1nM) mTOR inhibitors with excellent selectivity (up to >1000-fold) over PI3K and good potency in a cellular proliferation assay (IC(50) <50nM). Topics: Cell Line, Tumor; Drug Discovery; Humans; Intracellular Signaling Peptides and Proteins; Morpholines; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrimidines; Structure-Activity Relationship; TOR Serine-Threonine Kinases; Tropanes	2010
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). Bioorganic & medicinal chemistry letters, 2010, Jan-15, Volume: 20, Issue:2 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. Topics: Adenosine Triphosphate; Animals; Binding Sites; Binding, Competitive; Computer Simulation; Drug Discovery; Intracellular Signaling Peptides and Proteins; Mice; Microsomes; Models, Molecular; Morpholines; Protein Serine-Threonine Kinases; Pyrans; Pyrazoles; Pyridines; Pyrimidines; TOR Serine-Threonine Kinases	2010

Article

Year

Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.

Bioorganic & medicinal chemistry letters, 2010, Jan-01, Volume: 20, Issue:1

2-Aryl-4-morpholinothieno[3,2-d]pyrimidines are known PI3K inhibitors. This class of compounds also potently inhibited the homologous enzyme mTOR. Replacement of the morpholine group in these compounds with an 8-oxa-3-azabicyclo[3.2.1]octane group led to mTOR inhibitors with selectivity over PI3K. Optimization of the 2-aryl substituent led to the discovery of 2-(4-ureidophenyl)-thienopyrimidines as highly potent (IC(50) <1nM) mTOR inhibitors with excellent selectivity (up to >1000-fold) over PI3K and good potency in a cellular proliferation assay (IC(50) <50nM).

Topics: Cell Line, Tumor; Drug Discovery; Humans; Intracellular Signaling Peptides and Proteins; Morpholines; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyrimidines; Structure-Activity Relationship; TOR Serine-Threonine Kinases; Tropanes

2010

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).

Bioorganic & medicinal chemistry letters, 2010, Jan-15, Volume: 20, Issue:2

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.

Topics: Adenosine Triphosphate; Animals; Binding Sites; Binding, Competitive; Computer Simulation; Drug Discovery; Intracellular Signaling Peptides and Proteins; Mice; Microsomes; Models, Molecular; Morpholines; Protein Serine-Threonine Kinases; Pyrans; Pyrazoles; Pyridines; Pyrimidines; TOR Serine-Threonine Kinases

2010