Discovery of (2S)-8-[(3R)-3-methylmorpholin-4-yl]-1-(3-methyl-2-oxobutyl)-2-(trifluoromethyl)-3,4-dihydro-2H-pyrimido[1,2-a]pyrimidin-6-one: a novel potent and selective inhibitor of Vps34 for the treatment of solid tumors. [electronic resource]
- Journal of medicinal chemistry Jan 2015
- 376-400 p. digital
Publication Type: Journal Article
1520-4804
10.1021/jm5013352 doi
Amino Acid Sequence Animals Antineoplastic Agents--chemistry Area Under Curve Bridged Bicyclo Compounds, Heterocyclic--chemistry Caco-2 Cells Cell Line, Tumor Class III Phosphatidylinositol 3-Kinases--antagonists & inhibitors Crystallography, X-Ray Drug Discovery Enzyme Inhibitors--chemistry HeLa Cells Humans Male Mice, SCID Models, Chemical Models, Molecular Molecular Sequence Data Molecular Structure Neoplasms--drug therapy Protein Binding Protein Structure, Tertiary Pyrimidinones--chemistry Rats, Sprague-Dawley Sequence Homology, Amino Acid Thermodynamics Xenograft Model Antitumor Assays