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

Article Details

Citation

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

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

J Med Chem. 2002 Apr 25;45(9):1741-7.

PubMed ID
11960485 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AlvocidibCyclin-dependent kinase 2IC 50 (nM)2207.237Details
AlvocidibCyclin-dependent kinase 4IC 50 (nM)4007.237Details