Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis

…, WJ Rocque, D Rusnak, L Shewchuk…

文献索引：Bramson; Holmes; Hunter; Lackey; Lovejoy; Luzzio; Montana; Rocque; Rusnak; Shewchuk; Veal; Corona; Walker; Kuyper; Davis; Dickerson; Edelstein; Frye; Gampe Jr.; Harris; Hassell Journal of Medicinal Chemistry, 2001 , vol. 44, # 25 p. 4339 - 4358

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被引用次数: 232

摘要

Two closely related classes of oxindole-based compounds, 1 H-indole-2, 3-dione 3- phenylhydrazones and 3-(anilinomethylene)-1, 3-dihydro-2 H-indol-2-ones, were shown to potently inhibit cyclin-dependent kinase 2 (CDK2). The initial lead compound was prepared as a homologue of the 3-benzylidene-1, 3-dihydro-2 H-indol-2-one class of kinase inhibitor. Crystallographic analysis of the lead compound bound to CDK2 provided the basis for ...