Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs

  • Bioorg Med Chem Lett. 2004 May 17;14(10):2551-4. doi: 10.1016/j.bmcl.2004.02.084.
Helen Y Chen  1 ,  Seongkon Kim ,  Jane Y Wu ,  Elizabeth T Birzin ,  Wanda Chan ,  Yi Tien Yang ,  Johanna Dahllund ,  Frank DiNinno ,  Susan P Rohrer ,  James M Schaeffer ,  Milton L Hammond
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. [email protected]
PMID: 15109649 DOI: 10.1016/j.bmcl.2004.02.084
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.