In 2018,Tria, George S.; Abrams, Tinya; Baird, Jason; Burks, Heather E.; Firestone, Brant; Gaither, L. Alex; Hamann, Lawrence G.; He, Guo; Kirby, Christina A.; Kim, Sunkyu; Lombardo, Franco; Macchi, Kaitlin J.; McDonnell, Donald P.; Mishina, Yuji; Norris, John D.; Nunez, Jill; Springer, Clayton; Sun, Yingchuan; Thomsen, Noel M.; Wang, Chunrong; Wang, Jianling; Yu, Bing; Tiong-Yip, Choi-Lai; Peukert, Stefan published 《Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer》.Journal of Medicinal Chemistry published the findings.Reference of 1-Bromo-2-isopropylbenzene The information in the text is summarized as follows:
In breast cancer, estrogen receptor alpha (ERα) pos. cancer accounts for approx. 74% of all diagnoses, and in these settings, it is a primary driver of cell proliferation. Treatment of ERα pos. breast cancer has long relied on endocrine therapies such as selective estrogen receptor modulators, aromatase inhibitors, and selective estrogen receptor degraders (SERDs). The steroid-based anti-estrogen fulvestrant, the only approved SERD, is effective in patients who have not previously been treated with endocrine therapy as well as in patients who have progressed after receiving other endocrine therapies. Its efficacy, however, may be limited due to its poor physicochem. properties. THe authors describe the design and synthesis of a series of potent benzothiophene-containing compounds that exhibit oral bioavailability and preclin. activity as SERDs. This article culminates in the identification of LSZ102 (I), a compound in clin. development for the treatment of ERα pos. breast cancer. In the part of experimental materials, we found many familiar compounds, such as 1-Bromo-2-isopropylbenzene(cas: 7073-94-1Reference of 1-Bromo-2-isopropylbenzene)
1-Bromo-2-isopropylbenzene(cas: 7073-94-1) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Reference of 1-Bromo-2-isopropylbenzene
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary