Bioorganic & medicinal chemistry

Synthesis of potent oxindole CDK2 inhibitors

A Dermatakis, KC Luk, W DePinto

文献索引：Dermatakis, Apos; Luk, Kin-Chun; DePinto, Wanda Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 8 p. 1873 - 1881

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被引用次数: 43

摘要

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.