Investigation of carbonic anhydrase inhibitory potency of (Z/E)-alkyl N'-benzyl-N-(arylsulfonyl)-carbamimidothioates

Aim: Among 15 human (h) carbonic anhydrase (CA; EC 4.2.1.1) isoforms, two (hCA IX and XII) play important roles in the growth and survival of tumor cells, making them therapeutic targets for cancer treatment. This study aimed to develop novel sulfonamide-based compounds as selective hCA IX and XII inhibitors. Materials & methods: A library of novel N-sulfonyl carbamimidothioates was obtained for CA inhibitory activity studies against four hCA isoforms. Results: None of the developed compounds displayed inhibitory potential against off-target isoforms hCA I and II. However, they effectively inhibited tumor-associated hCA IX and XII. Conclusion: The present study suggests potent lead compounds as selective hCA IX and XII inhibitors with anticancer activity.

Tweetable abstractThe importance of targeting hCA IX and XII as a therapeutic approach in cancer treatment has been well documented. The present study suggests novel sulfonamide-based potent lead compounds as selective hCA IX and XII inhibitors.