177748-22-0Relevant academic research and scientific papers
New approach based on immunochemical techniques for monitoring of selective estrogen receptor modulators (SERMs) in human urine
Salvador, J.-Pablo,Vila-Roca, Ester,Monfort, Núria,Ventura, Rosa,Marco, M.-Pilar
, p. 147 - 152 (2018/05/04)
Antiestrogenic compounds such as tamoxifen, toremifen and chlomifen are used illegally by athletes to minimize physical impacts such as gynecomastia resulting from the secondary effects of anabolic androgenic steroids, used to increase athletic efficiency unlawfully. The use of these compounds is banned by the World Anti-Doping Agency (WADA) and controls are made through analytical methodologies such as HPLC–MS/MS, which do not fulfil the sample throughput requirements. Moreover, compounds such as tamoxifen are also used to treat hormone receptor-positive breast cancer (ER +).Therapeutic drug monitoring (TDM) of tamoxifen may also be clinically useful for guiding treatment decisions. An accurate determination of these drugs requires a solid phase extraction of patient serum followed by HPLC–MS/MS. In the context of an unmet need of high-throughput screening (HTS) and quantitative methods for antiestrogenic substances we have approached the development of antibodies and an immunochemical assay for the determination of these antiestrogenic compounds. The strategy applied has taken into consideration that these drugs are metabolized and excreted in urine as the corresponding 4-hydroxylated compounds. A microplate-based ELISA procedure has been developed for the analysis of these metabolites in urine with a LOD of 0.15, 0.16 and 0.63 μg/L for 4OH-tamoxifen, 4OH-toremifen and 4OH-clomifen, respectively, much lower than the MRPL established by WADA (20 μg/L).
Identification of novel inverse agonists of estrogen-related receptors ERRγ and ERRβ
Yu, Donna D.,Huss, Janice M.,Li, Hongzhi,Forman, Barry M.
, p. 1585 - 1599 (2017/02/26)
Estrogen-related receptors (ERRs, α, β, and γ) are orphan nuclear receptors most closely related in sequence to estrogen receptors (ERα and ERβ). Much attention has been paid recently to the functions of ERRs for their potential roles as new therapeutic t
USE OF A 4-HYDROXYTOREMIFENE PRODRUG FOR TREATMENT OF BREAST CANCER
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, (2011/11/01)
The present invention is directed to compounds, compositions thereof, and the use of the compounds and compositions for the treatment and prevention of breast cancer. In one embodiment, the present invention relates to the use of a prodrug of endoxifen or
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRγ
Chao, Esther Y.H.,Collins, Jon L.,Gaillard, Stephanie,Miller, Aaron B.,Wang, Liping,Orband-Miller, Lisa A.,Nolte, Robert T.,McDonnell, Donald P.,Willson, Timothy M.,Zuercher, William J.
, p. 821 - 824 (2007/10/03)
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor γ and the classical estrogen receptor α demonstrate that analogs bearing hydroxyalkyl g
Antioxidant compounds
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, (2008/06/13)
A new use of halogenated triphenylethylene derivatives for lowering levels of serum lipid perioxides and for the prevention or treatment of oxidative tissue damage induced by lipid peroxidation is disclosed. The new use includes the prevention or treatment of atherosclerosis, ischemic injury, psoriasis, inflammatory diseases, such as inflammatory bowel disease, or cardiovascular disorders, such as coronary heart disease, cardiac ischemic injury and post-ischemic cardiac arrhythmias, or the treatment of AIDS.
