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A series of 1,1′-diazacrown compounds derivatized with phosphonate or sulfoxide moieties was synthesized as potential inhibitors of a Lys48-linked ubiquitin chain, which plays an important role in cell cycle regulation. Sulfoxide and phosphonate moieties are generally regarded as ionic or hydrogen bond acceptor groups, respectively, and are frequently included in molecules targeted to polypeptides. Most phosphonate crown ethers were relatively insoluble in aqueous media, whereas they were readily soluble in organic solvents and could be prepared in aqueous solution using a palladium-catalyzed reaction. Studies of these compounds with a model peptide and with a ubiquitin analogue suggested that they bind to a Lys48-linked ubiquitin chain by neutralizing the positive charge

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