Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs
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 ERα over ERβ, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.
Chen, Helen Y.,Kim, Seongkon,Wu, Jane Y.,Birzin, Elizabeth T.,Chan, Wanda,Yang, Yi Tien,Dahllund, Johanna,DiNinno, Frank,Rohrer, Susan P.,Schaeffer, James M.,Hammond, Milton L.
p. 2551 - 2554
(2007/10/03)
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