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Bioorg Med Chem Lett ; 14(7): 1673-7, 2004 Apr 05.
Article in English | MEDLINE | ID: mdl-15026048

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.


Subject(s)
Cell Cycle Proteins/antagonists & inhibitors , Drug Design , Protease Inhibitors/chemical synthesis , cdc25 Phosphatases/antagonists & inhibitors , Cell Cycle Proteins/metabolism , Protease Inhibitors/metabolism , Structure-Activity Relationship , cdc25 Phosphatases/metabolism
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