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• W2464818884 abstract "The commonly used definition of an anti-oestrogen encompasses a wide range of agents which prevent manifestation of oestrogenic activity in the intact animal. Several different types of effect may result in an anti-oestrogenic action, for example, inhibition of pituitary follicle-stimulating hormone or luteinising hormone secretion, direct inhibition of oestradiol biosynthesis or antagonism of oestrogen action at the cellular level. In this chapter only the latter type of action will be considered, restricting the definition of an anti-oestrogen to compounds which bind to target-organ oestrogen receptors and prevent the full expression of oestrogenic effects. Although there are a few examples of steroidal molecules which satisfy this definition only the non-steroidal anti-oestrogens have been extensively studied and only two, clomiphene and tamoxifen, are in clinical use. Clomiphene is used in the induction of ovulation but tamoxifen (Nolvadex, ICI) in addition is widely used in the therapy of advanced breast cancer (Mouridsen et al., 1978). The structures of some non-steroidal anti-oestrogens are illustrated in figure 1. These compounds all possess two significant structural features; they are all related to triphenylethylene and all have a basic ether side-chain. Those compounds containing an ethylenic bond are illustrated in their trans forms. It is important to recognise that only the trans isomers are anti-oestrogenic whereas the cis isomers are oestrogenic (Harper and Walpole, 1966). Tamoxifen (Nolvadex) is the pure trans isomer but clomiphene is used as a mixture of cis (zuclomiphene) and trans (enclomiphene) isomers." @default.
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• W2464818884 date "1981-01-01" @default.
• W2464818884 modified "2023-09-23" @default.
• W2464818884 title "Biochemical and biological aspects of anti-oestrogen action" @default.
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• W2464818884 doi "https://doi.org/10.1007/978-1-349-81345-2_12" @default.
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