Antiestrogens properties

Other compounds of this general class which have been found to have antiestrogenic properties include the cytochrome P-450 inhibitor, SKF 525A P02-33-0](Sl) (24) JV, JV-diethyl-2-[(4-phenylmethyl)phenoxy]ethanamine [98774-23-3] (DPPE)(58) (42) /-Butylphenoxyethyl diethylamine [57586-10-4] (BPEA)(59) (43) and cyclofenil [110042-18-7] (60, R = C H ) (24) analogues. 

Megestrol is a synthetic progestin with antiestrogen properties that is used for breast cancer and in higher doses for weight... 

Tamoxifen has been the gold standard for adjuvant endocrine therapy. It has both estrogenic and antiestrogenic properties, depending on the tissue and gene in question. 

Poulin R, Merand Y, Poirier D et al. (1989) Antiestrogenic properties of keoxifene, trans-4-hydroxytamoxifen, and ICI 164384, a new steroidal antiestrogen, in ZR-75-1 human breast cancer cells. Breast cancer Res Treat 14 65-76... 

Crystallographic studies have confirmed that a critical difference in the antiestrogenic action of raloxifene lies in the interaction of the alkylaminoethoxy side chain with the amino acid aspartate at position 351. The peculiar orientation of this side chain of the raloxifene molecule, an essential determinant of the antiestrogenic properties of the drug, is believed to account for its lack of endometrial activity (Clark et al. 1976 Grese et al. 1997 Bryant et al. 1998). 

The first 1,6-addition reactions of thiolates to steroid dienones were examined well before the discovery of the antiestrogenic properties of 7o -substituted steroids. Ralls and coworkers129 and Djerassi and coworkers130 studied thiol additions to A3,5-steroids for example, the reaction of 3,5-cholestadien-7-one with ethanethiol was reported to proceed with high 1,6-regioselectivity and -stereoselectivity (equation 47)129. In a series of papers, Brueggemeier and coworkers131-137 described the synthesis and biochemical evaluation of numerous 7at-sul fur-substituted steroids which were prepared by Michael addition to steroid dienones. Thus, 4,6-androsta-3,17-dienone was treated with various... 

Metabolism in the rat has been found to transform the steroid drug furazol (74) into a /3-lactone derivative (75) (72CPB1243). A spiro-oxetane analog of estrone (76) has been synthesized for possible antiestrogenic properties (67JMC546). 

Bhat KP, Lantvit D, Christov K, Mehta RG, Moon RC, Pezzuto JM. 2001. Estrogenic and antiestrogenic properties of resveratrol in mammary tumor models. Cancer Res 61 7456-7463. 

Tennant, M.K., D.S. Hill, J.C. Eldridge, L.T. Wetzel, C.B. Breckenridge, and J.T. Stevens (1994a). Possible antiestrogenic properties of chloro-i-triazincs in rat uterus. J. Toxicol. Environ. Health, 43 183-196. 

The bis-Cp titanium molecules shown in Scheme 765 have been synthesized and used as potential antiestrogenic vectors to the estradiol receptor and a recognized cytotoxic molecule. They also proved to be particularly easy to exchange with Re in order to prepare organometallic radiopharmaceutical compounds with antiestrogenic properties.2020 These processes have been used as a source for Re(CO)3 through thermal ligand-transfer reaction between Cp titanium complexes and Re2(CO)i0. 

Synthetic progestin with antiestrogen properties interferes with normal estrogen cycle may also have direct effects on the endometrium... 

Bhat, K.P. and Pezzuto, J.M., Resveratrol exhibits cytostatic and antiestrogenic properties with human endometrial adenocarcinoma (Ishikawa) cells. Cancer Res., 61 (16), 6137-6144, 2001. 

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