Synthesis and structure-activity relationships of new non-steroidal progesterone receptor ligands.
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.
Drug Discovery, Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
K
K
Kurihara
K
K
Tanabe
Y
Y
Yamamoto
R
R
Shinei
K
K
Ajito
T
T
Okonogi
D005663:Furans / Q000138:chemical synthesis; D007700:Kinetics; D008024:Ligands; D009284:Naphthols / Q000138:chemical synthesis; D010407:Penicillium / Q000737:chemistry; D011980:Receptors, Progesterone / Q000737:chemistry*; D012717:Sesquiterpenes; D013329:Structure-Activity Relationship
D005663:Furans; D008024:Ligands; D009284:Naphthols; C106748:PF 1092A; D011980:Receptors, Progesterone; D012717:Sesquiterpenes