Pasquier, Benoit

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