4.7 Article

Synthesis of potent oxindole CDK2 inhibitors

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 11, 期 8, 页码 1873-1881

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(03)00036-1

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A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to the parent indolinone and nanomolar range IC50 against the CDK2 enzyme and two cancer cell lines. (C) 2003 Elsevier Science Ltd. All rights reserved.

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