Application of 626-40-4In 2022 ,《Development of Sulfamoylated 4-(1-Phenyl-1H-1,2,3-triazol-4-yl)phenol Derivatives as Potent Steroid Sulfatase Inhibitors for Efficient Treatment of Breast Cancer》 was published in Journal of Medicinal Chemistry. The article was written by Biernacki, Karol; Ciupak, Olga; Dasko, Mateusz; Rachon, Janusz; Kozak, Witold; Rak, Janusz; Kubinski, Konrad; Maslyk, Maciej; Martyna, Aleksandra; Sliwka-Kaszynska, Magdalena; Wietrzyk, Joanna; Switalska, Marta; Nocentini, Alessio; Supuran, Claudiu T.; Demkowicz, Sebastian. The article contains the following contents:
Here development of new sulfamoylated 4-(1-phenyl-1H-1,2,3-triazol-4-yl)phenol derivatives I [R = 3-Cl, 3-Br, 3-Et, etc.; X = H, SO2NH2] via sulfamoylation reaction of 4-(1-phenyl1H-1,2,3-triazol-4-yl)phenol derivatives with sulfamoyl chloride as potent steroid sulfatase (STS) inhibitors for the treatment of breast cancer was presented. Prompted by promising biol. results and in silico anal., the initial series of similar compounds were extended, appending a variety of m-substituents at the outer Ph ring. The inhibition profiles of the newly synthesized compounds were evaluated using a radioisotope enzymic assay and, together with the preceding reported derivatives, using a radioisotope assay in MCF-7 cells. The most active compound, I [R = 3,5-di-F, X = SO2NH2], demonstrated an extraordinary STS inhibitory potency in MCF-7 cells with an IC50 value improved 5-fold compared to that of the reference Irosustat (0.21 vs 1.06 nM). The five most potent compounds were assessed in vivo in a 67NR mouse mammary gland cancer model, with I [R = 3,5-di-Cl, X = SO2NH2] measured to induce up to 51% tumor growth inhibition at 50 mg/kg with no evidence of side effects and toxicity. In addition to this study using 3,5-Dibromoaniline, there are many other studies that have used 3,5-Dibromoaniline(cas: 626-40-4Application of 626-40-4) was used in this study.
3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Application of 626-40-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary