Xue, Ding published the artcileDiscovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors, Quality Control of 1178100-39-4, the publication is Journal of Medicinal Chemistry (2022), 65(1), 343-368, database is CAplus and MEDLINE.
Inhibition of oxidative phosphorylation (OXPHOS) is a promising therapeutic strategy for select cancers that are dependent on aerobic metabolism Here, we report the discovery, optimization, and structure-activity relationship (SAR) study of a series of novel OXPHOS inhibitors. The hit compound, benzene-1,4-disulfonamide 1 (I), was discovered in a phenotypic screen selective for cytotoxicity in a galactose-containing medium. Our multi-parameter optimization campaign led to the discovery of 65 (DX3-235)(II), showing nanomolar inhibition of complex I function and ATP production in a galactose-containing medium resulting in significant cytotoxicity. Importantly, 64 (DX3-234)(III), a close analog of 65, is well tolerated in mice and shows significant single agent efficacy in a Pan02 syngeneic pancreatic cancer model, suggesting that highly potent and selective OXPHOS inhibitors can be useful for the treatment of pancreatic cancer.
Journal of Medicinal Chemistry published new progress about 1178100-39-4. 1178100-39-4 belongs to bromides-buliding-blocks, auxiliary class Bromide,Sulfamide,Amine,Benzene, name is 4-Bromo-N,N-diethyl-3-methylbenzenesulfonamide, and the molecular formula is C9H9BrO2, Quality Control of 1178100-39-4.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary