| Literature DB >> 11960485 |
Joseph Schoepfer1, Heinz Fretz, Bhabatosh Chaudhuri, Lionel Muller, Egge Seeber, Laurent Meijer, Olivier Lozach, Eric Vangrevelinghe, Pascal Furet.
Abstract
Novel 2-benzylidene-benzofuran-3-ones were designed and synthesized to mimic flavopiridol, a well-established inhibitor of cyclin-dependent kinases (CDKs) which is currently undergoing clinical evaluation. The underlying design concepts as well as the synthesis and structure-activity relationships (CDKs 1, 2, and 4 enzyme assays) of these mimics are described. Inhibitors of CDKs 1 and 2 that are more potent and selective than flavopiridol were obtained.Entities:
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Year: 2002 PMID： 11960485 DOI： 10.1021/jm0108348
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446