Product Details of 100-19-6. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article SLC-0111 enaminone analogs, 3/4-(3-aryl-3-oxopropenyl) aminobenzenesulfonamides, as novel selective subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform IX published in 2019.0, Reprint Addresses Eldehna, WM (corresponding author), Kafrelsheikh Univ, Dept Pharmaceut Chem, Fac Pharm, Kafrelsheikh, Egypt.; Supuran, CT (corresponding author), Univ Florence, Dept NEUROFARBA, Sect Pharmaceut & Nutraceut Sci, Via U Schiff 6, I-50019 Florence, Italy.. The CAS is 100-19-6. Through research, I have a further understanding and discovery of 1-(4-Nitrophenyl)ethanone.
SLC-0111, an ureido substituted benzenesulfonamide, is a selective carbonic anhydrase (CA, EC 4.2.1.1) IX inhibitor that is currently in Phase I/II clinical trials for the treatment of advanced hypoxic tumors complicated with metastases. Herein we report the synthesis of two series of 3/4-(3-aryl-3-oxopropenyl) aminobenzenesulfonamides 5a-i and 6a-j as SLC-0111 enaminone congeners. The prepared enaminones were in vitro investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I, II, IV and IX, using a stopped-flow CO2 hydrase assay. All these isoforms were inhibited by the enaminones reported here in variable degrees. The target tumor-associated isoform hCA IX was undeniably the most affected one (K i s: 0.21-7.1 nM), with 6- to 21-fold enhanced activity than SLC-0111 (K-I = 45 nM). All the prepared enaminones displayed interesting selectivity towards hCA IX over hCA I (SI: 32 – > 35714), hCA II (SI: 2 -1689) and hCA IV (SI: 11 – > 45454). Of particular interest, bioisosteric replacement of phenyl tail with the bulkier 2-naphthyl tail, sulfonamide 6h, achieved the higher II/IX selectivity herein reported with SI of 1689.
Product Details of 100-19-6. About 1-(4-Nitrophenyl)ethanone, If you have any questions, you can contact Eldehna, WM; Abo-Ashour, MF; Berrino, E; Vullo, D; Ghabbour, HA; Al-Rashood, ST; Hassan, GS; Alkahtani, HM; Almehizia, AA; Alharbi, A; Abdel-Aziz, HA; Supuran, CT or concate me.
Reference:
Benzodioxan,
,1,4-Benzodioxane | C8H8O2 – PubChem