Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.

Article Details

Citation

Copy to clipboard

Jin C, Manikumar G, Kepler JA, Cook CE, Allan GF, Kiddoe M, Bhattacharjee S, Linton O, Lundeen SG, Sui Z

Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5754-7. Epub 2007 Aug 29.

PubMed ID

17855092 [ View in PubMed

]

Abstract

A series of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs have been evaluated for their antagonist hormonal properties using the T47D cell-based alkaline phosphatase assay and the A549 cell-based functional assay. Some of the compounds showed highly potent, and more selective antiprogestational activity against antiglucocorticoid activity than mifepristone (RU 486).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mifepristone	Glucocorticoid receptor	IC 50 (nM)	6	N/A	N/A	Details
Mifepristone	Progesterone receptor	IC 50 (nM)	0.054	N/A	N/A	Details