OESTROGENIC AND ANTI-OESTROGENIC ACTIVITIES OF SOME HEX-2-ENES RELATED TO DIETHYLSTILBOESTROL

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Abstract
Some members of the stilboestrol series have been reported to show significant anti-oestrogenic activity and to act as true competitive inhibitors of oestrogen at the 'receptor site' in the vagina (Emmens & Cox, 1958; Emmens, Cox & Martin, 1959). However, the compounds investigated also possessed oestrogenic activity. We have synthesized a series of nuclear methylated compounds related to diethylstilboestrol (Clark & O'Donnell, 1965) in an attempt to find true competitive anti-oestrogens which possess no oestrogenic activity. The present communication describes the investigation of three of these compounds for oestrogenic and anti-oestrogenic activity. The compounds were examined for oestrogenic activity by the Allen-Doisy vaginal smear test in ovariectomized mice, with both s.c. and intravaginal routes of administration. 3,5-Bis-(3,5-dimethyl-4-hydroxyphenyl)hex-2-ene (I) produced no oestrogenic response at s.c. doses up to 1 mg. and intravaginal doses up to 0·25 mg. 3-(3,5-Dimethyl-4-hydroxyphenyl)-4-(4-hydroxyphenyl)hex-2-ene (II) and 3,4-bis-(3-methyl-4-hydroxyphenyl)hex-2-ene (III) were assayed by a four-point quantal response assay, with

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