Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs |
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| Authors: | Chen Helen Y Kim Seongkon Wu Jane Y Birzin Elizabeth T Chan Wanda Yang Yi Tien Dahllund Johanna DiNinno Frank Rohrer Susan P Schaeffer James M Hammond Milton L |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. helen_chen@merck.com |
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| 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. |
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