1742-00-3Relevant academic research and scientific papers
Potential Antiestrogens. Synthesis and Evaluation of Mammary Tumor Inhibiting Activity of 1,2-Dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes
Hartmann, Rolf W.,Buchborn, Helga,Kranzfelder, Gerhard,Schoenenberger, Helmut,Bogden, Arthur
, p. 1192 - 1197 (2007/10/02)
The syntheses of the meso-1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes and of d,l-3,4-bis(3'-hydroxyphenyl)hexane (21) are described.In vitro these compounds inhibited the estradiol receptor interaction competitively, exhibiting Ka values between 0.20*109 (20) and 0.11*106 M-1 (24).In vivo the meso compounds reduced the estrone-stimulated mouse uterine growth; the most effective compounds were 20, 22, and 23 (53, 50, and 45percent inhibition, respectively).Compounds 20 and 22-24 showed weak estrogenic activity in the mouse uterine weight test and in the vaginal cornification test.Compounds 19 (NSC-297169), 20 (NSC-297170), and 22 (NSC-297171) exhibited a dose-dependent growth inhibition on the MCF-7 human breast tumor cell line (10-6 to 10-9 M).These compounds also showed a marked dose-dependent inhibition on the DMBA-induced, hormone-dependent mammary carcinoma of the Sprague-Dawley rat corresponding to their association constants.
Novel di-(3'-hydroxyphenyl)-alkane compounds, process of preparation and their use in medicine
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, (2008/06/13)
Compounds of di-(3'-hydroxyphenyl)-alkanes and their methyl ethers, of the formula STR1 wherein R is alkyl and R' is H or methyl, have activity against hormone-dependent breast carcinoma.
