Estrogen Receptor Ligands. II. Discovery of Benzoxathiins as Potent, Selective Estrogen Receptor α Modulators
Journal of Medicinal Chemistry2004Vol. 47(9), pp. 2171–2175
Citations Over TimeTop 10% of 2004 papers
Seongkon Kim, Jane Y. Wu, Elizabeth T. Birzin, Katalin Frisch, Wanda Chan, Lee-Yuh Pai, Yi Yang, Ralph T. Mosley, Paula M.D. Fitzgerald, Nandini Sharma, Johanna Dahllund, A.G. Thorsell, Frank DiNinno, Susan P. Rohrer, James M. Schaeffer, Milton L. Hammond
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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