Estrogen antiestrogens

Toremifene is a recently marketed antiestrogen whose primary advantage is a lower estrogenic antiestrogenic ratio than tamoxifen (based on laboratory data).41 Toremifene (60 mg orally daily) has been found to have efficacy similar to that of tamoxifen in metastatic disease and a generally similar side-effect profile.42 Currently, toremifene is indicated as an alternative to tamoxifen in patients with metastatic breast cancer, but studies are ongoing that evaluate its safety and efficacy in the adjuvant setting. 

From a synthetic standpoint, the most interesting silylated steroids are those having silicon substituted for one of the carbon atoms of a ring. Only one such system has been reported, that of the 6-silasteroids. A number of these compounds, for example 7, have been screened for estrogenic, antiestrogenic, and postcoital antifertility effects but no significant activity was noted (29). 

The tissue specificity of an estrogenic, antiestrogenic, or mixed estrogenic-antiestrogenic response can thus be explained by two different sites of DNA action of ERa and ERp. The classical ERE (Fig. 5A) binds both ER0C-E2 and ERP-E2, with a positive response in both cases (Fig. 6). With ERa or ER 3 and a reporter gene under the transcriptional control of an ERE, tamoxifen and raloxifene as well as ICI 164,384 inhibit the stimulatory effect ofE2 (Paech et al., 1997). 

Jordan, V.C. (1986) Estrogen/Antiestrogen Action and Breast Cancer Therapy. University of Wisconsin Press, Madison. 

Watts, C.K.W., Murphy, L.C. and Sutherland, R.L. (1986) In Estrogen/Antiestrogen Action and Breast Cancer Therapy (Jordan, V.C. ed.) pp. 93-114, University of Wisconsin Press, Madison. 

PAHs ER agonists - estrogenic, antiestrogenic -various mechanisms... 

Some cucurbitacins have been reported to be antifertility agents. The enriched cucurbitacin extract obtained from Wilbrandia sp. was tested for its potential antifertility effects with different experimental protocols including those involving estrus cycle, implantation, abortifacient, and estrogenic/antiestrogenic activities. The extract suppressed the number of... 

Basly JP, Mane-Foumier F, Le Bail JC, Habrioux G, Chulia AJ (2000) Estrogenic/ antiestrogenic and scavenging properties of (E)- and (Z)-resveratrol. Life Sci 66 769-777... 

Other recently reported activities of ginkgo include estrogenic/antiestrogenic, immu-nostimulatory, larvicidal, and modulation of certain cytochrome enzyme subtypes. Many reviews about the pharmacology and therapeutic potential of ginkgo have been published. " "- ... 

Thrae are a variety of isoflavones present in raw soy, specifically known as graiistdn, daidzin, and glycitin. These isoflavones can have numerous elfects in the body, including mimicking estrogen, antiestrogen effects, as well as some effects unrelated to estrograi. These chemicals remain in soy products that arc not washed with alcohol to remove these isoflavones. 

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