Diversely Substituted Sulfamides for Fragment-based Drug Discovery of Carbonic Anhydrase Inhibitors: Synthesis and Inhibitory Profile

Overview

Journal J Enzyme Inhib Med Chem

Specialty Biochemistry

Date 2022 Mar 17

PMID 35296197

Authors

Tatiana Sharonova

Petr Zhmurov

Stanislav Kalinin

Alessio Nocentini

Andrea Angeli

Marta Ferraroni

Mikhail Korsakov

Claudiu T Supuran

Mikhail Krasavin

Affiliations

Soon will be listed here.

Abstract

A series of sulfamide fragments has been synthesised and investigated for human carbonic anhydrase inhibition. One of the fragments showing greater selectivity for cancer-related isoforms CA IX and XII was co-crystalized with CA II showing significant potential for fragment periphery evolution fragment growth and linking. These opportunities will be identified in the future the screening of this fragment structure for co-operative carbonic anhydrase binding with other structurally diverse fragments.[Figure: see text].

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Valtari A, Kalinin S, Jantti J, Vanhanen P, Martina H, Hanzlikova M Mol Pharm. 2025; 22(2):721-732.

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