78682-41-4Relevant academic research and scientific papers
Influence of Alkyl Chain Ramification on Estradiol Receptor Binding Affinity and Intrinsic Activity of 1,2-Dialkylated 1,2-Bis(4- or 3-hydroxyphenyl)ethane Estrogens and Antiestrogens
Hartmann, Rolf W.
, p. 1668 - 1674 (2007/10/02)
The influence of a symmetrical introduction of CH3 substituents in the α or β positions of the 1,2-dialkyl-1,2-bis(4-hydroxyphenyl)ethene estrogens hexestrol (ethyl, HES) and octestrol (n-propyl, OCES) isopropyl (1), tert-butyl (2), sec-butyl (3), isobut
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.
