Schiller, Claus D. and Schneider, Martin R. and Angerer, Erwin von (1990) 3-(Cyclohexenonyl)-4-(4-hydroxyphenyl)-hexanes: antiandrogenes derived from the estrogen hexestrol. Archiv der Pharmazie 323 (7), pp. 417-420.
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Selective Birch-reduction of one of the phenolic rings of meso- or d,l-HES led to compounds 6a and 6b which exert a higher binding affinity to the androgen receptor as the respective parent HES. In vivo testing of 6a and 6b shows that 6a has the same potency in reducing accessory sex organ weights and testosterone levels in the intact mouse as has meso-HES, but strongly decreased estrogenic activity. Syntheses and testing of 7 having no ethyl side chains revealed the necessity of these groups for biological activity.
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Owner:||Prof. Armin Buschauer|
|Deposited On:||11 Dec 2008 18:02|
|Last Modified:||05 Aug 2009 15:48|
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