title: Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.
abstract: A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ER alpha over ER beta, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. helen_chen@merck.com
authors.forename: Helen Y
authors.initials: HY
authors.lastname: Chen
authors.forename: Seongkon
authors.initials: S
authors.lastname: Kim
authors.forename: Jane Y
authors.initials: JY
authors.lastname: Wu
authors.forename: Elizabeth T
authors.initials: ET
authors.lastname: Birzin
authors.forename: Wanda
authors.initials: W
authors.lastname: Chan
authors.forename: Yi Tien
authors.initials: YT
authors.lastname: Yang
authors.forename: Johanna
authors.initials: J
authors.lastname: Dahllund
authors.forename: Frank
authors.initials: F
authors.lastname: DiNinno
authors.forename: Susan P
authors.initials: SP
authors.lastname: Rohrer
authors.forename: James M
authors.initials: JM
authors.lastname: Schaeffer
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
mesh_terms: D000818:Animals; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D009929:Organ Size / Q000187:drug effects; D051381:Rats; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors*; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014599:Uterus / Q000166:cytology
chemical_list: D006576:Heterocyclic Compounds, 4 or More Rings; D008024:Ligands; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators