Xiong, Rui published the artcileNovel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer, Category: bromides-buliding-blocks, the main research area is estrogen receptor downregulator SERD antitumor breast cancer.
Resistance to the selective estrogen receptor modulator (SERM) tamoxifen and to aromatase inhibitors that lower circulating estradiol occurs in up to 50% of patients, generally leading to an endocrine-independent ER+ phenotype. Selective ER downregulators (SERDs) are able to ablate ER and thus theor. to prevent survival of both endocrine-dependent and independent ER+ tumors. The clin. SERD, fulvestrant, is hampered by i.m. administration and undesirable pharmacokinetics. Novel SERDs were designed using the 6-OH-benzothiophene (BT) scaffold common to arzoxifene and raloxifene. Treatment-resistant (TR) ER+ cell lines (MCF-7:5C and MCF-7:TAM1) were used for optimization, followed by validation in the parent endocrine-dependent cell line (MCF-7:WS8), in 2D and 3D cultures, using ERĪ± in-cell westerns, ERE-luciferase, and cell viability assays, with GDC-0810 (ARN-810) used for comparison. Two BT SERDs with superior in vitro activity to GDC-0810 were studied for bioavailability and shown to cause regression of a TR, endocrine-independent ER+ xenograft superior to GDC-0810.
Journal of Medicinal Chemistry published new progress about Antiestrogens. 452-63-1 belongs to class bromides-buliding-blocks, name is 1-Bromo-4-fluoro-2-methylbenzene, and the molecular formula is C7H6BrF, Category: bromides-buliding-blocks.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary