Antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1, 1, 2, 2-tetraalkyl-1, 2-diphenylethanes

…, E Von Angerer, H Schoenenberger

Index: Hartmann, Rolf W.; Kranzfelder, Gerhard; Angerer, Erwin, v.; Schoenenberger, Helmut Journal of Medicinal Chemistry, 1980 , vol. 23, # 8 p. 841 - 848

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Citation Number: 54

Abstract

Among the newly synthesized 1, 1, 2, 2-tetraallryl-l, 2-diphenylethanes, 1, 1, 2, 2-tetramethyl- 1, 2-bis (4'-hydroxyphenyl) ethane (23) and 1, 1, 2, 2-tetramethyl-1, 2-bis (3'-hydroxyphenyl) ethane (26) were the most active compounds regarding estradiol receptor affinity, exhibiting K, values of 0.73 X los and 0.67 X lo8 Ml, respectively. In vivo, 23 and 26 showed only very small uterotrophic activity in the mouse. They strongly inhibited (73%) the estrone- ...