Isatin: a privileged scaffold for the design of carbonic anhydrase inhibitors

Abstract

The isatin scaffold is the constitutive fragment of several natural and synthetic bioactive molecules. Albeit several benzene sulphonamide-based carbonic anhydrase inhibitors (CAIs) have been reported, only recently isatin benzene sulphonamides have been studied and proposed as CAIs. In this study we have designed, synthesised, and evaluated the biological activity of a series of differently substituted isatin-based benzene sulphonamides which have been designed for the inhibition of carbonic anhydrase isoforms. The activity of all the synthesised compounds was evaluated towards human carbonic anhydrase I, II, IX, and XII isozymes. Our results indicate that the nature and position of substituents on the isatin ring can modulate both activity and isozyme selectivity.

Keywords:

• Antitumour agents
• carbonic anhydrase inhibitors
• isatin hybrid molecules

Acknowledgements

The authors wish to acknowledge the “Ufficio Valorizzazione dei Risultati della Ricerca” of Sardegna Ricerche Technological Park, Pula (CA) – Italy.

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.