Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins |
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| Authors: | Tan Qiang Birzin Elizabeth T Chan Wanda Yang Yi Tien Pai Lee-Yuh Hayes Edward C DaSilva Carolyn A 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, 800B-107, Rahway, NJ 07065, USA. qiang_tan@merck.com |
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| Abstract: | ![]()
Dihydrobenzodithiin compounds (1-6) were prepared to explore the expansion of the dihydrobenzoxathiin lead compounds I-III as SERAMs (Selective Estrogen Receptor Alpha Modulators). The dihydrobenzodithiin compounds generally maintained a high degree of selectivity for ERalpha over ERbeta, however, they lacked the in vivo antagonism/agonism activity exhibited by the lead class in an immature rat uterine growth model. |
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