Discovery of Novel Hydroxyimine-Tethered Benzenesulfonamides as Potential Human Carbonic Anhydrase IX/XII Inhibitors.

ABSTRACT: To discover novel carbonic anhydrase (CA, EC 4.2.1.1) inhibitors for cancer treatment, a series of 4-{4-[(hydroxyimino)methyl]piperazin-1-yl}benzenesulfonamides were designed and synthesized using SLC-0111 as the lead molecule. The developed novel compounds 27-34 were investigated for the inhibition of human (h) isoforms hCA I, hCA II, hCA IX, and hCA XII. The hCA I was inhibited by compound 29 with a K_i value of 3.0 nM, whereas hCA II was inhibited by compound 32 with a K_i value of 4.4 nM. The tumor-associated hCA IX isoform was inhibited by compound 30 effectively with an K_i value of 43 nM, whereas the activity of another cancer-related isoform, hCA XII, was significantly inhibited by 29 and <

SUBMITTER: Peerzada MN 

PROVIDER: S-EPMC10258898 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature