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Combined photochemical arylation, "nuisance effect" (SN Ar) reaction sequences have been employed in the design of small arrays for immediate deployment in medium-throughput X-ray protein-ligand structure determination. Reactions were deliberately allowed to run "out of control" in terms of selectivity; for example the ortho-arylation of 2-phenylpyridine gave five products resulting from mono- and bisarylations combined with SN Ar processes. As a result, a number of crystallographic hits against NUDT7, a key peroxisomal CoA ester hydrolase, have been identified.

Original publication

DOI

10.1002/cmdc.202000543

Type

Journal article

Journal

ChemMedChem

Publication Date

12/2020

Volume

15

Pages

2513 - 2520

Addresses

Chemistry Deparment, University of Sussex, Falmer, East Sussex, BN1 9QJ, UK.

Keywords

Humans, Palladium, Benzene Derivatives, Pyridines, Pyrrolidinones, Pyrophosphatases, Enzyme Inhibitors, Crystallography, X-Ray, Feasibility Studies, Protein Binding, Drug Design, Catalysis, Small Molecule Libraries, Coordination Complexes, Chemistry Techniques, Synthetic, Proof of Concept Study