534572-55-9Relevant academic research and scientific papers
Estradiol derivatives bearing sulfur-containing substituents at the 11β or 7α positions: Versatile reagents for the preparation of estrogen conjugates
Spera, Daniela,Cabrera, Gustavo,Fiaschi, Rita,Carlson, Kathryn E.,Katzenellenbogen, John A.,Napolitano, Elio
, p. 4393 - 4401 (2007/10/03)
Estradiol derivatives bearing HS-, HSCH2-, HSCH 2CH2-, MeS-, MeSCH2-, MeSCH2CH 2-, or PhCH2SCH2CH2-groups at the 11β position or an HS-group at the 7α position have been synthesized, and their binding affinity to the estrogen receptor (ER) determined. Nearly all of these substituted estrogens retain high binding affinity, and at the 11β position, the sulfur atom has an effect on ER binding that is similar to that of a carbon atom. These thiol derivatives are promising intermediates for the preparation of a variety of estradiol conjugates. The methyl sulfides, in particular, might potentially be developed as 11C-labeled agents for imaging ER-positive tumors by positron emission tomography.
11beta-short chain substituted estradiol analogs and their use in the treatment of menopausal symptoms and estrogen sensitive cancer
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Page/Page column 5, (2010/02/07)
The present invention relates to novel 11-β estradiol ester compounds and their use as locally active estrogens in the treatment of the symptomology of menopause and to treat estrogen sensitive cancers, including breast cancer.
Synthesis and evaluation of B-, C-, and D-ring-substituted estradiol carboxylic acid esters as locally active estrogens
Labaree, David C.,Zhang, Jing-Xin,Harris, Heather A.,O'Connor, Craig,Reynolds, Toni Y.,Hochberg, Richard B.
, p. 1886 - 1904 (2007/10/03)
We have synthesized derivatives of estradiol that are structurally modified to serve as "soft" estrogens and act within a geographically limited area of the body; estrogens without systemic action. We have previously shown with 16α-substituted analogues o
