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Synthesis of potent oxindole CDK2 inhibitors
Apos Dermatakis1, Kin Chun Luk, Wanda DePinto
1Hoffmann-La Roche Inc., 340 Kingsland str., Nutley, NJ 07110-1199, USA. apostolos.dermatakis@roche.com
Bioorganic & Medicinal Chemistry
|March 28, 2003
Abstract:
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 IC(50) against the CDK2 enzyme and two cancer cell lines.