Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.
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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
Drug Target Property Measurement pH Temperature (°C) Alvocidib Cyclin-dependent kinase 2 IC 50 (nM) 220 7.2 37 Details Alvocidib Cyclin-dependent kinase 4 IC 50 (nM) 400 7.2 37 Details