Abstract
A new series of 3,3-disubstituted-5-aryloxindoles has been synthesized and evaluated for progesterone receptor antagonist (PR) activity in a T47D cell alkaline phosphatase assay and for their ability to bind PR in competition binding studies. In this communication, the synthesis and structure-activity relationships (SARs) of various 3,3-substituents are discussed where it is clear that small alkyl and spiroalkyl groups are required to achieve better PR antagonist activity.
MeSH terms
-
Alkaline Phosphatase / metabolism
-
Animals
-
Binding, Competitive
-
Biological Assay
-
Breast Neoplasms
-
Cyclohexanes / chemistry*
-
Cyclohexanes / pharmacology*
-
Decidua / drug effects
-
Female
-
Humans
-
Indoles / chemistry*
-
Indoles / pharmacology*
-
Inhibitory Concentration 50
-
Rats
-
Receptors, Progesterone / antagonists & inhibitors*
-
Receptors, Progesterone / metabolism
-
Structure-Activity Relationship
-
Tumor Cells, Cultured
Substances
-
Cyclohexanes
-
Indoles
-
Receptors, Progesterone
-
Alkaline Phosphatase