Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators |
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| Authors: | Kim Seongkon Wu Jane Y Birzin Elizabeth T Frisch Katalin Chan Wanda Pai Lee-Yuh Yang Yi Tien Mosley Ralph T Fitzgerald Paula M D Sharma Nandini Dahllund Johanna Thorsell Ann-Gerd DiNinno Frank Rohrer Susan P Schaeffer James M Hammond Milton L |
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| Institution: | Department of Medicinal Chemistry, Atherosclerosis and Endocrinology, Merck Research Laboratories, P.O. Box 2000, 800-B109 Rahway, New Jersey 07065, USA. Seongkon_kim@merck.com |
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| Abstract: | The discovery and synthesis of dihydrobenzoxathiins as potent, ERalpha subtype selective ligands are described. The most active analogue, 4-D, was found to be 50-fold selective in a competitive binding assay and 100-fold selective in a transactivation assay in HEK-293 cells. The alpha selectivity was postulated to lie in the interaction of the sulfur atom of the benzoxathiin ring with the two discriminating residues in the binding pocket of the receptor isoforms. |
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