Boutard, Nicolas published the artcileDiscovery and structure-activity relationships of N-aryl 6-aminoquinoxalines as potent PFKFB3 kinase inhibitors, Recommanded Product: 4-Bromo-2-chloro-6-nitroaniline, the main research area is crystal structure neoplasm antitumor PFKFB3 kinase inhibitor aminoquinoxaline; cancer; enzymes; glycolysis; inhibitors; metabolism.
Energy and biomass production in cancer cells are largely supported by aerobic glycolysis in what is called the Warburg effect. The process is regulated by key enzymes, among which phosphofructokinase PFK-2 plays a significant role by producing fructose-2,6-biphosphate; the most potent activator of the glycolysis rate-limiting step performed by phosphofructokinase PFK-1. Herein, the synthesis, biol. evaluation and structure-activity relationship of novel inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3), which is the ubiquitous and hypoxia-induced isoform of PFK-2, are reported. X-ray crystallog. and docking were instrumental in the design and optimization of a series of N-aryl 6-aminoquinoxalines. The most potent representative, N-(4-methanesulfonylpyridin-3-yl)-8-(3-methyl-1-benzothiophen-5-yl)quinoxalin-6-amine, displayed an IC50 of 14 nM for the target and an IC50 of 0.49 μM for fructose-2,6-biphosphate production in human colon carcinoma HCT116 cells. This work provides a new entry in the field of PFKFB3 inhibitors with potential for development in oncol.
ChemMedChem published new progress about Antitumor agents. 34033-41-5 belongs to class bromides-buliding-blocks, name is 4-Bromo-2-chloro-6-nitroaniline, and the molecular formula is C6H4BrClN2O2, Recommanded Product: 4-Bromo-2-chloro-6-nitroaniline.
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Bromide – Wikipedia,
bromide – Wiktionary