Structure activity study of carbonic anhydrase IX: Selective inhibition with ureido-substituted benzenesulfonamides.

Ureido-substituted benzenesulfonamides (USBs) show great promise as selective and potent inhibitors for human carbonic anhydrase hCA IX and XII, with one such compound (SLC-0111/U-F) currently in clinical trials (clinical trials.gov, NCT02215850). In this study, the crystal structures of both hCA II (off-target) and an hCA IX-mimic (target) in complex with selected USBs (U-CH, U-F, and U-NO), at resolutions of 1.