Potential antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1, 2-dialkyl-1, 2-bis (3'-hydroxyphenyl) ethanes

RW Hartmann, H Buchborn, G Kranzfelder…

Index: Hartmann, Rolf W.; Buchborn, Helga; Kranzfelder, Gerhard; Schoenenberger, Helmut; Bogden, Arthur Journal of Medicinal Chemistry, 1981 , vol. 24, # 10 p. 1192 - 1197

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Citation Number: 27

Abstract

C3H7 (22), C4Hg (23), i-C4H9 (24), and C6H11 (2511 and of d, l-3, 4-bis (3'-hydroxyphenyl) hexane (21) are described. In vitro these compounds inhibited the [%] estradiol receptor interaction competitively, exhibiting K, values between 0.20 X log (20) and 0.11 X los M- '(24). In vivo the mew compounds reduced the estrone-stimulated mouse uterine growth; the most effective compounds were 20, 22, and 23 (53, 50, and 45% inhibition, respectively). ...