Carbonic anhydrase (CA, EC 4.2.1.1) is a zinc enzyme responsible for the reversible hydration of carbon dioxide to bicarbonate with 16 isozyme described to date. Over the last decade a connection was established between cancer and the over-expression of membrane bound carbonic anhydrases CA IX and CA XII. Therefore, pharmaceutical agents that can selectively inhibit CA IX and CA XII may have therapeutic value for detection, imaging and treatment of a large variety of hypoxic tumors. Our team has a long-standing interest in the research on carbonic anhydrase activity modulation and has reported the first inhibition study of CA IX.<br/>Focusing on colon cancer, several studies have shown that membrane-bound CA IX and XII are present at very low levels in the normal colon, while being overexpressed in colon tumors. In this context we are presenting our synthetic efforts, supported by Xray crystallography [8,9], towards generation of several classes of nanomolar potent amphiphilic 1,3,4-thiadiazole-2-sulfonamides low molecular weight CA inhibitors and their transformation into theranostic systems for cancer detection and treatment via optimization of physicochemical and optical properties.

Amphiphilic heterocyclic sulfonamides as carbonic anhydrase inhibitors with selectivity for tumor-overexpressed isozymes – towards theranostic systems for cancer detection and treatment

255th National Meeting (2018)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.