| Literature DB >> 15012993 |
Kin-Chun Luk1, Mary Ellen Simcox, Andy Schutt, Karen Rowan, Thelma Thompson, Yi Chen, Ursula Kammlott, Wanda DePinto, Pete Dunten, Apos Dermatakis.
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.Entities:
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Year: 2004 PMID： 15012993 DOI： 10.1016/j.bmcl.2003.12.009
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823