Indolylchalcone benzenesulfonamides selectively inhibit tumor-associated carbonic anhydrase IX and XII

Novel indolylchalcone-benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase IX (Ki=8.9 nM) and XII (Ki=4.9 nM) with high selectivity over cytosolic isoforms, suggesting potential as anticancer leads (in vitro study).

• Design: Synthesis and in vitro enzymatic evaluation of 17 compounds against human carbonic anhydrase isoforms I, II, IX, and XII.
• Key secondary: Electron-withdrawing groups (cyano, bromo) on the indole scaffold enhance selectivity toward tumor-associated isoforms.
• Limitation: Preclinical in vitro and in silico study; no in vivo or clinical validation.

RadPigeon summaries are original and for information only. They are not clinical advice.