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. 2004 Jul 16;14(14):3753-5.
doi: 10.1016/j.bmcl.2004.04.101.

Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins

Qiang Tan  1 , Elizabeth T Birzin, Wanda Chan, Yi Tien Yang, Lee-Yuh Pai, Edward C Hayes, Carolyn A DaSilva, Frank DiNinno, Susan P Rohrer, James M Schaeffer, Milton L Hammond
Affiliations

Estrogen receptor ligands. Part 6: Synthesis and binding affinity of dihydrobenzodithiins

Qiang Tan et al. Bioorg Med Chem Lett. .

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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