Uslu, Azize Gizem published the artcileBenzimidazole derivatives as potent and isoform selective tumor-associated carbonic anhydrase IX/XII inhibitors, Recommanded Product: 4-Bromo-N-methyl-2-nitroaniline, the publication is Bioorganic Chemistry (2020), 103544, database is CAplus and MEDLINE.
We describe the synthesis of a series of 2-arylbenzimidazole derivatives bearing sulfonamide functionality (4a-d, 7a-c and 10) as well as hydroxamic acid (15a-b), carboxylic acid (16a-b), carboxamide (17a-b) and boronic acid (22a-b and 26) functionalities, which act as human carbonic anhydrase (hCA, EC 4.2.1.1) inhibitors. The newly synthesized benzimidazole derivatives were evaluated against 4 physiol. relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2-29.3 nM and 9.9-41.7 nM, resp. Notably, compound 4c was the most potent and selective CA IX (KI = 6.6 nM) and XII (KI = 9.9 nM) inhibitor with a significant selectivity ratio over cytosolic CA I and II isoforms in the range of 3.4-25.2. In addition, compounds having hydroxamic acid (15a-b) or carboxylic acid (16a-b) functionalities resulted in greater selectivity ratios for CA IX/XII over CAI/II in the range of 4.1-121.5 although with KI values in lower micromolar potency (KIs = 0.36-0.85μM for CA IX/XII).
Bioorganic Chemistry published new progress about 53484-26-7. 53484-26-7 belongs to bromides-buliding-blocks, auxiliary class Bromide,Nitro Compound,Amine,Benzene, name is 4-Bromo-N-methyl-2-nitroaniline, and the molecular formula is C7H6Cl2, Recommanded Product: 4-Bromo-N-methyl-2-nitroaniline.
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