114031-67-3Relevant articles and documents
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 (2006)
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
Rational design of ERα targeting hypoxia turn-on fluorescent probes with antiproliferative activity for breast cancer
Dong, Chune,Hu, Zhiye,Ma, Xiaoyu,Meng, Qiuyu,Xie, Baohua,Zhou, Fuling,Zhou, Hai-Bing
supporting information, p. 10493 - 10496 (2020/10/02)
The overexpression of estrogen receptor (ER) α is not only closely related to the development of ER+ breast cancer, but is also an important biomarker for clinical diagnosis and treatment. Herein, we report several ERα targeting hypoxia turn-on fluorescent probes with antitumor activity for breast cancer cells. Among them, probes 3 and 5 displayed good ERα targeting ability and favorable hypoxia turn-on response in MCF-7 cells. Moreover, the probes 3 and 5 exhibited good antiproliferative activity towards MCF-7 cells (IC50 = 8.5 μM, 10.3 μM) and a much lower cytotoxicity to normal cells compared with the positive control. It is expected that these novel fluorescent probes may provide useful tools for the theranostics of ER+ breast cancer.
ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS
-
Page/Page column 215, (2019/12/04)
The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.