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2004
Dithiane derivatives
R 0490
Estrogen Receptor Ligands. Part 6. Synthesis and Binding Affinity of Dihydro— The dihydrobenzoxathiin core of selective estrogen receptor alpha
46- 147 benzodithiins.
modulators is replaced by a dihydrobenzodithiin core to explore the expansion of dihydrobenzoxathiin lead compounds. The synthesis of six dihydrobenzodithiins such as
(XI) and (XII) is carried out by utilizing a literature method. The racemic dihydrobenzodithiins generally maintain the selectivity for ERα or ERβ but lack the in vivo antagonism/agonism activity in a uterine growth model. — (TAN*, Q.; et al.; Bioorg. Med.
Chem. Lett. 14 (2004) 14, 3753-3755; Dep. Med. Chem., Merck Res. Lab., Rahway,
NJ 07065, USA; Eng.) — H. Hoennerscheid
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