Investigation of Carbonic Anhydrase Inhibitory Potency of (Z/E)-alkyl N‘-benzyl-N-(arylsulfonyl)-carbamimidothioates

Abstract

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 abstract

The 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.

Graphical abstract

Keywords:

• antitumor
• carbonic anhydrase
• inhibitors
• sulfonamides
• (Z/E)-alkyl N'-benzyl-N-(arylsulfonyl)-carbamimidothioates

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Financial & competing interests disclosure

This work was supported by the European Regional Development Fund (project no. 1.1.1.2/VIAA/3/19/398). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.