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3-(Cyclohexenonyl)-4-(4-hydroxyphenyl)-hexanes: antiandrogenes derived from the estrogen hexestrol

Schiller, Claus D. ; Schneider, Martin R. ; Angerer, Erwin von


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 ...


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