Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.

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Fensome A, Koko M, Wrobel J, Zhang P, Zhang Z, Cohen J, Lundeen S, Rudnick K, Zhu Y, Winneker R

Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1317-20.

PubMed ID

12657272 [ View in PubMed

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Abstract

During the course of our studies on 3,3-disubstituted-5-aryloxindoles derived progesterone receptor (PR) antagonists we discovered that changing the amide funtionality to a thio-amide resulted in compounds displaying potent PR agonist activity. In this communication, the synthesis, structure activity relationships (SAR) and in vivo activity of various 5-arylthio-oxindoles will be discussed.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Medroxyprogesterone acetate	Progesterone receptor	IC 50 (nM)	10.8	N/A	N/A	Details
Medroxyprogesterone acetate	Progesterone receptor	EC 50 (nM)	0.5	N/A	N/A	Details