Abstract:

Carbonic anhydrases (CAs) are zinc-containing enzymes that catalyze the decomposition of carbonic acid into carbon dioxide and water. There are various types of CAs isoforms that involved in different physiological and pathological process. Thus, many of these isozymes are important targets for the design of inhibitors with clinical applications. The most important inhibitors of CAs are used as anticancer. Alpha-class CAs in humans expressed 16 CA isoforms where CA IX and CA XII have been shown to be associated with tumors. Thus, CA IX and CA XII are involved in cancerogenesis in hypoxic tumors. These isoforms also are used as a potential target biomarker of tumor hypoxia and as a prognostic factor for cancer therapy. Inhibition the enzymatic activity of CA IX and CA XII by specific inhibitors, found to be effective in cancer therapy and imaging of various metastatic cancers.

To our knowledge, a small number of reviews covered the role of CA IX inhibitors as a target for cancer therapy however; no single review had covered the role of the other CA isoforms’ inhibitors such as those for CA I-XIV. The aim of this review is to give a comprehensive update on the reported discoveries in the field of CA IX inhibitors with an emphasis on the new families of compounds which reach in vivo/ preclinical studies for their potential in cancer therapy.