Anti-oestrogen

Johnson, L, Hetheridge, M., and Tyler, C.R. (2004). Assessment of the (Anti-) Oestrogenic and (Anti-) Androgenic Activity of Sewage Treatment Works Effluent. R D Technical Report, Environment Agency. [Pg.354]

Suggest how available oestrone ether (32) might be converted into potentially anti-oestrogenic (33). [Pg.345]

Powles TJ (2002) Anti-oestrogenic prevention of breast cancer - the make or break point. Nat Rev Cancer 2 787... [Pg.60]

Lipton A (1987) The anti-oestrogen tamoxifen is a calcium antagonist in perfused rat mesentery. Cancer Chemother Pharmacol 20 125-127... [Pg.112]

Sutherland RL, Murphy LC, San Foo M, Green MD, Whybourne AM, Krozowski ZS (1980) High-affinity anti-oestrogen binding site distinct from the oestrogen receptor. Nature 288(5788) 273-275... [Pg.114]

Geisler J, Haarstad H, Gundersen S, Raabe N, Kvinnsland S, Lonning PE (1995b) Influence of treatment with the anti-oestrogen 3-hydroxytamoxifen (droloxifene) on plasma sex hormone levels in postmenopausal breast cancer patients. J Endocrinol 146 359-363... [Pg.142]

Messinis IE, Templeton A (1990) Anti-oestrogen effect of clomiphene citrate in oestrogen-treated, hypogonadal women. Hum Reprod 5 150-152... [Pg.146]

Howell A, DeFriend DJ, Robertson JF, Blarney RW, Anderson L, Anderson E, Sutcliffe FA, Walton P (1996) Pharmacokinetics, pharmacological and anti-tumour effects of the specific anti-oestrogen ICI 182780 in women with advanced breast cancer. Br J Cancer 74 300-308... [Pg.166]

Thomas EJ, Walton PL, Thomas NM, Dowsett M (1994) The effects of ICI 182,780, a pure anti-oestrogen, on the hypothalamic- pituitary-gonadal axis and on endometrial proliferation in pre- menopausal women. Hum Reprod 9 1991-1996... [Pg.168]

Clark ER, Jordan VC (1976) Oestrogenic, anti-oestrogenic and fertility effects of some triphenylethanes and triphenylethylenes related to ethamoxytriphetol (MER 25). Br J Pharmacol 57(4) 487—493... [Pg.296]

Colletta AA, Wakefield LM, Howell FV, van Roozendaal KE, Danielpour D, Ebbs SR, Sporn MB, Baum M (1990) Anti-oestrogens induce the secretion of active transforming growth factor beta from human fetal fibroblasts. Br J Cancer 62(3) 405-409... [Pg.296]

Ugwumadu AH, Harding K (1994) Uterine leiomyomata and endometrial proliferation in postmenopausal women treated with the anti-oestrogen tamoxifen. Em J Obstet Gynecol Reprod Biol 54 153-156... [Pg.320]

Shilling V, Jenkins V, Fallowfield L, Howell A (2001) The effects of oestrogens and anti-oestrogens on cognition. Breast 10 484-491... [Pg.339]

Stevens HP, Ostlere LS, Black CM, Jacobs HS, Rustin MH (1993) Cyclical psoriatic arthritis responding to anti-oestrogen therapy. Br J Dermatol 129 458-460... [Pg.340]

Molecular targets Anti-oestrogens Aromatase inhibitors Androgens ... [Pg.506]

Hormone therapy Tamoxifen Anti-oestrogen, forms complex with oestrogen receptor... [Pg.506]

Figure 1.4. Structure of clomiphene and tamoxifen, two non-steroidal synthetic anti-oestrogens that have found medical application...

Progestogens inhibit GnRH secretion and suppress LH release. They have anti-oestrogenic effects by reducing the number of oestrogen receptors and increasing oestradiol dehydrogenase. [Pg.401]

Clomiphene is a nonsteroidal agent with oestrogenic and anti-oestrogenic properties. The mechanism of action is not precisely clear, but it ultimately leads to the release of the pituitary gonadotropins FSH and LH. It stimulates ovulation in anovulatory or oligo-ovulatory women with adequate endogenous oestrogen activity and an intact hypothalamic-pituitary-ovarian axis. [Pg.403]

Women with anovulatory infertility should be offered full endocrinological evaluation, considering potential diagnoses such as hypothalamic-pituitary disease, polycystic ovary syndrome and primary gonadal disease. Hyperprolactinaemia must be sought as a potential cause, and its treatment is outlined below. The main treatments available include the anti-oestrogens clomiphene and tamoxifen, and gonadotrophin therapy. [Pg.771]

Phytoestrogens represent a family of plant compounds that have been shown to have both oestrogenic and anti-oestrogenic properties. Accumulating evidence from molecular and cellular biology experiments, animal studies and, to a limited extent, human clinical trials suggests that phytoestrogens may potentially confer health benefits related to... [Pg.302]

Powles TJ. Anti-oestrogenic chemoprevention of breast cancer—the need to progress. Eur J Cancer 2003 39 572-9. [Pg.161]

Afzal I, Cunningham P, Naftalin RJ. 2002. Interactions of ATP, oestradiol, genistein and the anti-oestrogens, faslodex (ICI 182780) and tamoxifen, with the human erythrocyte glucose transporter, GLUT1. Biochem J 365 707-719. [Pg.126]

Kirk, J., et al. 1994. Reversal of P-glycoprotein-mediated multidrug resistance by pure anti-oestrogens and novel tamoxifen derivatives. Biochem Pharmacol 48 277. [Pg.109]

BeckJI, Boothroyd C, Proctor M, et al. Oral anti-oestrogens and medical adjuncts for subfertility associated with anovulation. Cochrane Database Syst Rev. 2005 CD002249. [Pg.454]

Keywords Anti-androgen Anti-oestrogen/Anti-oestrogenic Breast cancer Cytoto x i c/Cytotox i c i ty. Electrochemistry/Electrochemical Oestradiol Ferricenium Ferrocene Ferrocenophane Hydroxyferrocifens Hydroxytamoxifen (OH-Tam) Oestrogen receptor (ER) Oestrogen/Oestrogenic Phenol Prostate cancer Quinone Raloxifen RBA ROS Steroid Tamoxifen Testosterone Vectorisation... [Pg.81]

In 1996, Jaouen et al. first coupled ferrocene to the active metabolite of tamoxifen, OH-Tam, Chart 2 [60, 61]. The resulting hydroxyferrocifens (with various lengths of the N, N-dimethylamino chain, n = 2-5, 8) were designed to combine the anti-oestrogenic properties of tamoxifen with potentially cytotoxic properties of ferrocene [62-64, 177]. In replacing the phenyl group of OH-Tam by the aromatic... [Pg.84]

Interestingly, the antiproliferative effects of the hydroxyferrocifens lb (n = 3) and Id (n = 5) are definitely superior to OH-Tam at 1 pM at this concentration, the contribution of a non-receptor-mediated and a dose-dependent cytotoxic component, which is not reversed upon the addition of oestradiol, begins to appear [64], On MDA-MB-231 cells, possessing undetectable amounts of ERa and low amounts of ERp, and thus classified as hormone-independent, these compounds have IC50 values as low as 0.5 pM (Table 1), while OH-Tam was completely inactive on these cells. Consequently, two kinds of behaviour can be observed one which is similar to the anti-oestrogenic role of OH-Tam on the ER, and a cytotoxic effect that involves the ferrocene moiety. [Pg.86]

The piperazinyl derivative showed the greatest in vitro activity, with a mean IC5o value of 1.64 pM over all cell lines, that is, tenfold lower than cisplatin. It was particularly active against the hormone-dependent breast, cervix and ovarian cells, implicating an oestrogenic/anti-oestrogenic effect. This compound also activates caspase-3 in ovarian cells, suggesting that the mechanism of cell death is apoptosis rather than necrosis. [Pg.91]

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