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Synthesis and structure-activity relationships of new non-steroidal progesterone receptor ligands
K Kurihara1, K Tanabe, Y Yamamoto
1Drug Discovery, Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
Bioorganic & Medicinal Chemistry Letters
|July 16, 1999
Abstract:
In order to study structure-activity relationships, a series of new non-steroidal progesterone receptor ligands based on PF1092A was synthesized with structural modifications (mostly introduction or removal of a methyl group) at the 3-, 4-, 5-, 7- or 9-position in the 6-acetoxy-4a, 5, 6, 7-tetrahydro-3, 4a, 5-trimethylnaphtho[2,3-b]furan-2(4H)-one skeleton. Critical positions for high binding affinity to the progesterone receptor were identified.