A new series of potent oxindole inhibitors of CDK2.

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Luk KC, Simcox ME, Schutt A, Rowan K, Thompson T, Chen Y, Kammlott U, DePinto W, Dunten P, Dermatakis A

A new series of potent oxindole inhibitors of CDK2.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):913-7.

PubMed ID

15012993 [ View in PubMed

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Abstract

A novel series of oxindole-type inhibitors of CDK2 that have heteroatom substituted alkynyl moieties at their C-4 position is described. These novel 4-alkynyl-substituted inhibitors have superior potency relative to their parent compound in free enzyme and in cell based assays. The crystal structure of CDK2 in complex with one of these analogues was determined and gives insight to their increased potency. The biochemical evaluation of a representative derivative is also described.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
4-((3r,4s,5r)-4-Amino-3,5-Dihydroxy-Hex-1-Ynyl)-5-Fluoro-3-[1-(3-Methoxy-1h-Pyrrol-2-Yl)-Meth-(Z)-Ylidene]-1,3-Dihydro-Indol-2-One	Cyclin-dependent kinase 2	IC 50 (nM)	3	7.5	22	Details