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Synthesis of deuterated-BCX-1777, a potent inhibitor of purine nucleoside phosphorylase

TitleSynthesis of deuterated-BCX-1777, a potent inhibitor of purine nucleoside phosphorylase
Publication TypeJournal Article
Year of Publication2002
AuthorsKezar III, H. S., Hutchison T. L., Tyler P. C., and Morris Jr. P. E.
IRL TeamCarbohydrate Chemistry
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume45
Pagination71-78
Keywordsarticle, Catalysis, chemical bond, Deuterium, drug structure, drug synthesis, immucillin h, mass spectrometry, purine nucleoside phosphorylase inhibitor, unclassified drug
Abstract BCX-1777, a novel inhibitor of the enzyme purine nucleoside phosphorylase, mimics the charged ribosyl oxocarbenium ion formed during the transition state of the enzyme-catalyzed C-N bond cleavage of nucleosides. BCX-1777 is a slow-onset, tight-binding inhibitor with a K1* of 23 pM and is one of the most potent inhibitors known for the enzyme. In support of our BCX-1777 program, a mass spectrometric assay has been developed utilizing 5′-[2H]-BCX-1777 as an internal standard. The synthesis of 5′-[2H]-BCX-1777 is described in this report. Copyright © 2002 John Wiley & Sons, Ltd.
URLhttp://www.scopus.com/inward/record.url?eid=2-s2.0-0036157739&partnerID=40&md5=e6d060500e35c01106b223f0a196b901
DOI10.1002/jlcr.533

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