Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.

Article Details

Citation

Perry B, Alexander R, Bennett G, Buckley G, Ceska T, Crabbe T, Dale V, Gowers L, Horsley H, James L, Jenkins K, Crepy K, Kulisa C, Lightfoot H, Lock C, Mack S, Morgan T, Nicolas AL, Pitt W, Sabin V, Wright S

Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4700-4. doi: 10.1016/j.bmcl.2008.06.104. Epub 2008 Jul 5.

PubMed ID
18644721 [ View in PubMed
]
Abstract

The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
5,5-dimethyl-2-morpholin-4-yl-5,6-dihydro-1,3-benzothiazol-7(4H)-onePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoformIC 50 (nM)1660N/AN/ADetails