4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.

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Alexander R, Balasundaram A, Batchelor M, Brookings D, Crepy K, Crabbe T, Deltent MF, Driessens F, Gill A, Harris S, Hutchinson G, Kulisa C, Merriman M, Mistry P, Parton T, Turner J, Whitcombe I, Wright S

4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4316-20. doi: 10.1016/j.bmcl.2008.06.076. Epub 2008 Jun 28.

PubMed ID

18625552 [ View in PubMed

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Abstract

4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
5,5-dimethyl-2-morpholin-4-yl-5,6-dihydro-1,3-benzothiazol-7(4H)-one	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	IC 50 (nM)	3453	N/A	N/A	Details