Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 Tat-TAR binding inhibitors

G. Jimenez Bueno, T. Klimkait, I. H. Gilbert, C. Simons

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    Abstract

    A series of diamine and polyamine derivatives, either free amines or salts (HCl or TFA), of aspartic and glutamic acid were prepared in excellent yields using Rink Amide solid-phase synthesis. The asparagine and glutamine derivatives were all evaluated for their ability to inhibit Tat-TAR binding using a FIGS cellular assay, with the polyamine derivatives exhibiting the most promising binding activity. (C) 2002 Published by Elsevier Science Ltd.

    Original languageEnglish
    Pages (from-to)87-94
    Number of pages8
    JournalBioorganic & Medicinal Chemistry
    Volume11
    Issue number1
    DOIs
    Publication statusPublished - 2003

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