Targeted anticancer pre-vinylsulfone covalent inhibitors of carbonic anhydrase IX
Aivaras Vaškevičius,
Denis Baronas,
Janis Leitans
et al.
Abstract:The CA IX is a transmembrane protein, highly overexpressed in hypoxic solid tumors, important for cancer cell survival and proliferation because it acidifies tumor microenvironment helping invasion and metastases processes. We designed novel compounds that have several functionalities: 1) primary sulfonamide group recognizing carbonic anhydrases (CA), 2) high-affinity moieties specifically recognizing CA IX among all CA isozymes, and 3) forming a covalent bond with the His64 residue. Such targeted covalent com… Show more
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