Bäurle Stefan, Blume Thorsten, Günther Judith, Henschel Daniela, Hillig Roman C, Husemann Manfred, Mengel Anne, Parchmann Christian, Schmid Elke, Skuballa Werner
Schering AG, Research Center Europe, D-13342 Berlin, Germany.
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1673-7. doi: 10.1016/j.bmcl.2004.01.052.
Based on molecular modeling studies, macrocyclic inhibitors of phosphatase cdc25B were synthetically derived from steroids. A preliminary SAR for this new template was elaborated. A series of compounds shows inhibition of cdc25B in the low micromolar range and good selectivity versus other phosphatases. The compounds did not show a significant antiproliferative effect in MaTu or HaCaT cells.