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Synthesis and Activity of Analogues of the Isoleucyl tRNA Synthetase Inhibitor SB-203207

Crasto, Curtis; Forrest, Andrew; Karoli, Tomislav; March, Darren; Mensah, Lucy; O'Hanlon, Peter; Nairn, Michael; Oldham, Mark; Yue, Weimin; Banwell, Martin; Easton, Christopher


Twenty two analogues of SB-203207 have been prepared by total synthesis, and evaluated as inhibitors of a range of tRNA synthetases. Changes to the bicyclic core, removing either the terminal amino substituent or the sulfonyl group from the side chain, and altering either the carbon skeleton or stereochemistry of the isoleucine residue, decreases the potency of inhibition of isoleucyl tRNA synthetase. Substituting the isoleucine residue with other amino acids produces inhibitors of the...[Show more]

CollectionsANU Research Publications
Date published: 2003
Type: Journal article
Source: Bioorganic and Medicinal Chemistry
DOI: 10.1016/S0968-0896(03)00237-2


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