Safety of 4-Bromo-1-(bromomethyl)-2-fluorobenzeneOn September 15, 2019 ,《A fragment-like approach to PYCR1 inhibition》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Milne, Kirsty; Sun, Jianhui; Zaal, Esther A.; Mowat, Jenna; Celie, Patrick H. N.; Fish, Alexander; Berkers, Celia R.; Forlani, Giuseppe; Loayza-Puch, Fabricio; Jamieson, Craig; Agami, Reuven. The article contains the following contents:
Pyrroline-5-carboxylate reductase 1 (PYCR1) is the final enzyme involved in the biosynthesis of proline and has been found to be upregulated in various forms of cancer. Due to the role of proline in maintaining the redox balance of cells and preventing apoptosis, PYCR1 is emerging as an attractive oncol. target. Previous PYCR1 knockout studies led to a reduction in tumor growth. Accordingly, a small mol. inhibitor of PYCR1 could lead to new treatments for cancer, and a focused screening effort identified pargyline as a fragment-like hit. Herein the design and synthesis of the first tool compounds as PYCR1 inhibitors, derived from pargyline, which were assayed to assess their ability to attenuate the production of proline, are reported. Structural activity studies have revealed the key determinants of activity, with the most potent compound, 4-bromobenzyl(propargyl)methylamine, showing improved activity in vitro in enzyme (IC50 = 8.8μM) and pathway relevant effects in cell-based assays. The results came from multiple reactions, including the reaction of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Safety of 4-Bromo-1-(bromomethyl)-2-fluorobenzene)
4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds.The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. Safety of 4-Bromo-1-(bromomethyl)-2-fluorobenzene The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary