Design and synthesis of macrocyclic inhibitors of phosphatase Cdc25B

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 phosphata...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-04, Vol.14 (7), p.1673-1677
Main Authors: Bäurle, Stefan, Blume, Thorsten, Günther, Judith, Henschel, Daniela, Hillig, Roman C., Husemann, Manfred, Mengel, Anne, Parchmann, Christian, Schmid, Elke, Skuballa, Werner
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
cdc25 Phosphatases - antagonists & inhibitors
cdc25 Phosphatases - metabolism
Cell Cycle Proteins - antagonists & inhibitors
Cell Cycle Proteins - metabolism
Drug Design
General aspects
Macrocycles
Medical sciences
Miscellaneous
Molecular modeling
Pharmacology. Drug treatments
Phosphatases
Protease Inhibitors - chemical synthesis
Protease Inhibitors - metabolism
Steroids
Structure-Activity Relationship
Templates
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Summary: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. Based on molecular modeling studies, macrocyclic inhibitors of phosphatase cdc25B in the low micromolar range were synthetically derived from steroids.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.01.052