title: Design and synthesis of macrocyclic inhibitors of phosphatase cdc25B.
abstract: 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.
authors.affiliation: Schering AG, Research Center Europe, D-13342 Berlin, Germany. stefan.baeurle@schering.de
authors.forename: Stefan
authors.initials: S
authors.lastname: Bäurle
authors.forename: Thorsten
authors.initials: T
authors.lastname: Blume
authors.forename: Judith
authors.initials: J
authors.lastname: Günther
authors.forename: Daniela
authors.initials: D
authors.lastname: Henschel
authors.forename: Roman C
authors.initials: RC
authors.lastname: Hillig
authors.forename: Manfred
authors.initials: M
authors.lastname: Husemann
authors.forename: Anne
authors.initials: A
authors.lastname: Mengel
authors.forename: Christian
authors.initials: C
authors.lastname: Parchmann
authors.forename: Elke
authors.initials: E
authors.lastname: Schmid
authors.forename: Werner
authors.initials: W
authors.lastname: Skuballa
mesh_terms: D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015195:Drug Design; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism; D013329:Structure-Activity Relationship; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D018797:Cell Cycle Proteins; D011480:Protease Inhibitors; D020687:cdc25 Phosphatases