… : a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogs of (Z)-1, 2-diphenyl-1-[4-[2-(dimethylamino) ethoxy] phenyl]-1- …

DW Robertson, JA Katzenellenbogen…

Index: Robertson, David W.; Katzenellenbogen, John A.; Hayes, James R.; Katzenellenbogen, Benita S. Journal of Medicinal Chemistry, 1982 , vol. 25, # 2 p. 167 - 171

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Citation Number: 90

Abstract

A series of N-substituted (Z)-1, 2-diphenyl-l-[4-(2-aminoethoxy) phenyl]-l-butenes, analogues of the antiestrogen tamoxifen (Nolvadex), in which the side-chain basicity is varied over a wide range, has been prepared to probe the importance of basicity in evoking estrogen antagonism. All of the compounds, except the pyrrole analogue 14, were found to possess significant antiestrogenic activity in the rat, as measured by their ability to inhibit ...