Antiestrogens. 3. Estrogen receptor affinities and antiproliferative effects in MCF-7 cells of phenolic analogs of trioxifene,[3, 4-dihydro-2-(4-methoxyphenyl)-1- …

…, LC Blaszczak, ME Goettel, T Suarez…

Index: Jones, Charles D.; Blaszczak, Larry C.; Goettel, Mary E.; Suarez, Tulio; Crowell, Thomas A.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 5 p. 931 - 938

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Citation Number: 105

Abstract

Benzothiophenes 3 and 4, derived from the acrylophenone antiestrogen trioxifene (2), are characterized by high estrogen receptor (ER) affinity and low residual estrogenicity compared to tamoxifen (la). In order to characterize further the growth suppression mechanism for these structural types we have prepared structural variants of 2 bearing hydroxy groups positioned to maximize ER affinity. Thus, dihydronaphthalenes 5 and 6 ...