Nonsteroidal Estrogens

Estrogen therapy Estrogens, nonsteroidal Estrogens, steroidal Ethylene oxide... 

Estrogen therapy, postmenopausal Estrogen-progesterone postmenopausal therapy Estrogen-progesterone oral contraceptives Estrogens, nonsteroidal... 

Estrogens, nonsteroidal Cervix/vagina, breast, testis (endometrium) ... 

Chromium(VI] compounds -Solar radiation Nickel compounds Radon and its decay products -Mustard gas (Sulfur mustard) -N -Bis(2-chloroethyl)-2-naphthylamine Analgesic mixtures containing phenacetin -Diethylstilbestrol Estrogens, nonsteroidal Betel quid with tobacco Arsenic and arsenic compounds Azathioprine... 

Diethylstlbestrol [56-53-1] (DES)(7), which was first synthesized in the 1930s, is the most widely studied nonsteroidal estrogen and has been extensively reviewed. It is an extremely potent estrogen, possessing four times the oral potency of estradiol (3), but carcinogenicity problems have limited its use. 

For the purposes of this article, antiestrogens are compounds that counteract the biological activity of estrogens at the receptor level. In the late 1970s, there were no steroidal antiestrogens in widespread clinical use. Clomiphene [911 -45-5]( ) and tamoxifen/7(954(9-25 -/7(9) were nonsteroidal antiestrogens that had been employed for the treatment of female infertility and breast cancer, respectively. 

Steroidal and Nonsteroidal Estrogens. Modification of the basic steroid skeleton and the nature of the functional groups in the B, C, and D rings while maintaining the phenoHc A-ring has continued to be a primary approach in the development of new estrogens with unique biological profiles. 

WS-7528 [132147-69-4][VI] a nonsteroidal estrogen, is an isoflavone which has been isolated from Streptomjces sp. No. 7528 and is an estrogen agonist. It inhibits [3ff]-estradiol binding to its receptor in rat uterine cytosol at an inhibitor for 50% of the rats tested (IC q) concentration of 5.7 nM. It also induces the growth of estrogen-dependent human breast cancer cell line MCE-7 (7). 

Synthetic Estrogens" under "Hormones" in ECT 1st ed., Vol. 7, pp. 536—547, by P. E. Dreisbach, Calco Chemical Division, American Cyanamid Company "Nonsteroidal Estrogens" under "Hormones" in ECT 2nd ed., VoL 11, pp. 127—141, by R. 1. Dorfman, Syntex Research Division of Syntex Corporation "Nonsteroidal Estrogens" under "Hormones" in ECT 3rd ed., Vol. 12, pp. 658—691, by G. C. Crawley, Imperial Chemical Industries Limited. 

Comparative QSAR analysis of derivatives of heterocycles as nonsteroid ligands of estrogen receptors 99CRV723. 

Cells from tissues associated with primary and secondary sexual characteristics are under particular endocrine control. Sex hormones determinethe growth, differentiation, and proliferation of such cells. When a tumor develops in such tissues, it is sometimes hormone dependent and the use of anti hormones removes the impetus for the tumor s headlong growth. Many nonsteroidal compounds have estrogenic activity diethylstilbest-jrol (81) may be taken as an example. Certain more bulky an-... 

Anastrazole is a nonsteroidal, type H, aromatase inhibitor that is 200 times more potent than aminoglutethimide. It is eliminated primarily via hqDatic metabolism, has a terminal half life of 50 h with steady state concentrations achieved approximately 10 days with once daily dosing regimens. It is administered orally at a dose of 1 mg/day that achieves near maximal aromatase inhibition and hence estrogen suppression in breast cancer patients. No effect on adrenal steroidogenesis has been observed at up to ten times the daily recommended dose. When used in the metastatic setting, anastrozole has been shown... 

Clomiphene (Clomid) is a synthetic nonsteroidal compound that binds to estrogen receptors, decreasing the amount of available estrogen receptors and causing the anterior pituitary to increase secretion of FSH and LH. It is used to induce ovulation in anovulatory (nonovulating) women. 

Anastrozole is a selective nonsteroidal aromatase inhibitor that lowers estrogen levels. The pharmacokinetics of anastrozole demonstrate good absorption, with hepatic metabolism the primary route of elimination and only 10% excreted unchanged by the kidney. The elimination half-life is approximately 50 hours. Anastrozole is used for the adjuvant treatment of postmenopausal women with hormone-positive breast cancer and in breast cancer patients who have had disease progression following tamoxifen. Side effects include hot flashes, arthralgias, osteoporosis/bone fractures, and thrombophlebitis. 

Ke HZ, Paralkar VM, Grasser WA, Crawford DT, Qi H, Simmons H, et al. (1998) Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus, and body composition in rat models. Endocrinology 139 2068-2076... 

Tamoxifen, a first-generation SERM, is a nonsteroidal triphenylethylene derivate routinely used in clinical practice for the treatment and prevention of breast cancer in high-risk populations (Robertson 2004). This drug produces an estrogen antagonist effect on the breast and an estrogen agonist effect... 

Raloxifene hydrochloride is a synthetic nonsteroidal drug derived from the benzothiophene and afferent to SERMs. It is known that raloxifene acts on metabolism, the skeleton, and the cardiovascular system as an estrogenic agonist (Khovidhunkit et al. 1999 Ettinger et al. 1999 Walsh et al. 1998), whereas it shows an estrogenic antagonist effect on reproductive organs such as the... 

Lasofoxifene is a new potent nonsteroidal SERM that binds with high affinity to ERs acting as a tissue-selective estrogen antagonist or agonist (Maeda et al. 2004). 

Pung, O.J., Luster, M.L, Hayes, H.T. and Rader, J. (1984). Influence of steroidal and nonsteroidal sex hormones on host resistance in the mouse Increased susceptibility to Listeria monocytogenes following exposure to estrogenic hormones. Infect. Immun. 46 301-307. 

Equol [7-hydroxy-3-(4 -hydroxyphenyl)-chroman] is a nonsteroidal estrogen of the isoflavone class. It is exclusively a product of intestinal bacterial... 

Watanabe N, Ikeno A, Minato H, et al. Discovery and preclinical characterisation of (-l-)-3-[4-(l-piperidinoethoxy)phenyl]spiro[indene-l,l -indane]-5,5 -diol hydrochloride a promising nonsteroidal estrogen receptor agonist for hot flush. / Med Chem 2003 46 3961-4. 

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