Using sulfuramidimidoyl fluorides that undergo sulfur(vi) fluoride exchange for inverse drug discovery

Fragment-based covalent ligand discovery

“…72% of the protein targets identified by SAFs have not been previously identified in previous SuFEx-based chemoproteomics. 73 Hsu et al have recently adapted sulfur-triazole exchange (SuTEx) chemistry (Fig. 4E) for fragment-based ligand discovery of Tyr-directed binders.…”

“…72% of the protein targets identified by SAFs have not been previously identified in previous SuFEx-based chemoproteomics. 73 …”

Development and biological applications of sulfur–triazole exchange (SuTEx) chemistry

“…Sulfuramidimidoyl fluorides have recently emerged as a more selective variant of SuFEx for developing protein ligands. 74 Applications of SuFEx probes include investigation of specific protein classes including kinases ( e.g. XO44 for selectivity profiling of dasatinib 29 ) as well as late-stage functionalization of phenol-containing drugs or drug candidates for developing new anticancer agents.…”

Modular Approaches to Synthesize Activity- and Affinity-Based Chemical Probes

“…They discovered that thionyl tetrafluoride (SOF 4 ) reacts selectively with primary amines to form iminosulfur oxydifluoride products and that a second fluoride can be substituted with secondary amines or aryl silyl ethers in follow-up steps to form sulfuramidimidoyl fluoride and sulfurofluoridoimidate products (Li et al, 2017 ). With this modular two-step approach, a structurally highly diverse library of 16 fully functional sulfuramidimidoyl fluoride probes was prepared (Brighty et al, 2020 ). Compound 10 depicts an example of a probe prepared via this method ( Figure 3D ).…”