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

Chunyang Jin; G Manikumar; John A Kepler; C Edgar Cook; George F Allan; Margaret Kiddoe; Sheela Bhattacharjee; Olivia Linton; Scott G Lundeen; Zhihua Sui

doi:10.1016/j.bmcl.2007.08.064

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. doi: 10.1016/j.bmcl.2007.08.064. Epub 2007 Aug 29.

Authors

Chunyang Jin¹, G Manikumar, John A Kepler, C Edgar Cook, George F Allan, Margaret Kiddoe, Sheela Bhattacharjee, Olivia Linton, Scott G Lundeen, Zhihua Sui

Affiliation

¹ Center for Organic and Medicinal Chemistry, RTI International, PO Box 12194, Research Triangle Park, NC 27709, USA. [email protected]

PMID: 17855092
DOI: 10.1016/j.bmcl.2007.08.064

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Line
Humans
Oxazoles / chemical synthesis*
Oxazoles / pharmacology*
Progesterone / antagonists & inhibitors*

Substances

Oxazoles
Progesterone