Document Report Card

ID: ALA1135924

Journal: J Med Chem

Title: Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.

Authors: Schoepfer J, Fretz H, Chaudhuri B, Muller L, Seeber E, Meijer L, Lozach O, Vangrevelinghe E, Furet P.

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.

CiteXplore: 11960485

DOI: 10.1021/jm0108348