Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer was written by 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. And the article was included in Journal of Medicinal Chemistry in 2018.Formula: C9H8OS This article mentions the following:
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 experiment, the researchers used many compounds, for example, 6-Methoxybenzo[b]thiophene (cas: 90560-10-4Formula: C9H8OS).
6-Methoxybenzo[b]thiophene (cas: 90560-10-4) belongs to benzothiophene derivatives. Benzothiophene is used as starting material for the synthesis of bioactive molecules. The core structure is a part of various pharmaceutical substances and natural products. Its aromaticity makes it relatively stable, although as a heterocycle, it has reactive sites which allow for functionalization.Formula: C9H8OS
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem