《Rational Design and Synthesis of Selective PRMT4 Inhibitors: A New Chemotype for Development of Cancer Therapeutics》 was written by Sutherland, Mathew; Li, Alice; Kaghad, Anissa; Panagopoulos, Dimitrios; Li, Fengling; Szewczyk, Magdalena; Smil, David; Scholten, Cora; Bouche, Lea; Stellfeld, Timo; Arrowsmith, Cheryl H.; Barsyte, Dalia; Vedadi, Masoud; Hartung, Ingo V.; Steuber, Holger; Britton, Robert; Santhakumar, Vijayaratnam. Category: bromides-buliding-blocks And the article was included in ChemMedChem on April 1 ,2021. The article conveys some information:
Protein arginine N-Me transferase 4 (PRMT4) asym. dimethylates the arginine residues of histone H3 and nonhistone proteins. The overexpression of PRMT4 in several cancers had stimulated interest in the discovery of inhibitors as biol. tools and, potentially, therapeutics. Although several PRMT4 inhibitors had reported, most display poor selectivity against other members of the PRMT family of Me transferases. Herein, the structure-based design of a new class of alanine-containing 3-arylindoles such as I [R = Me, i-Pr, NMe2, etc.] as potent and selective PRMT4 inhibitors was reported, and described key structure-activity relationships for this class of compounds In the experiment, the researchers used many compounds, for example, 1-Bromo-3-(isopropylsulfonyl)benzene(cas: 70399-01-8Category: bromides-buliding-blocks)
1-Bromo-3-(isopropylsulfonyl)benzene(cas: 70399-01-8) 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. Category: bromides-buliding-blocks In contrast, terrestrial plants account only for a few bromine-containing compounds.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary