Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzeneOn September 9, 2021 ,《1,4,9-Triazaspiro[5.5]undecan-2-one Derivatives as Potent and Selective METTL3 Inhibitors》 was published in Journal of Medicinal Chemistry. The article was written by Dolbois, Aymeric; Bedi, Rajiv K.; Bochenkova, Elena; Muller, Anna; Moroz-Omori, Elena V.; Huang, Danzhi; Caflisch, Amedeo. The article contains the following contents:
N6-methyladenosine (m6A) is the most frequent of the 160 RNA modifications reported so far. Accumulating evidence suggests that the METTL3/METTL14 protein complex, part of the m6A regulation machinery, is a key player in a variety of diseases including several types of cancer, type 2 diabetes, and viral infections. Here we report on a protein crystallog.-based medicinal chem. optimization of a METTL3 hit compound that has resulted in a 1400-fold potency improvement (IC50 of 5 nM for the lead compound 22 (UZH2)(I) in a time-resolved Forster resonance energy transfer (TR-FRET) assay). The series has favorable ADME properties as physicochem. characteristics were taken into account during hit optimization. UZH2 shows target engagement in cells and is able to reduce the m6A/A level of polyadenylated RNA in MOLM-13 (acute myeloid leukemia) and PC-3 (prostate cancer) cell lines. In addition to this study using 4-Bromo-1-(bromomethyl)-2-fluorobenzene, there are many other studies that have used 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzene) was used in this study.
4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals.Name: 4-Bromo-1-(bromomethyl)-2-fluorobenzene Organobromine compounds have fallen under increased scrutiny for their environmental impact.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary