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Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
Fensome A,
Bender R,
Chopra R,
Cohen J,
Collins MA,
Hudak V,
Malakian K,
Lockhead S,
Olland A,
Svenson K,
Terefenko EA,
Unwalla RJ,
Wilhelm JM,
Wolfrom S,
Zhu Y,
Zhang Z,
Zhang P,
Winneker RC,
Wrobel J.
Chemical and Screening Sciences, Women's Health Research Institute, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. fensoma@wyeth.com
Tanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives. Additional SAR, biological activity, and structural information from a tanaproget/hPR-LBD (hPR-LBD = human progesterone receptor ligand binding domain) cocrystal structure will also be presented.
PMID: 16078826 [PubMed - indexed for MEDLINE]
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