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

doi:10.1016/S0968-0896(02)00305-X

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

Research output: Contribution to journal › Article › peer-review

16 Citations (Scopus)

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 language	English
Pages (from-to)	87-94
Number of pages	8
Journal	Bioorganic & Medicinal Chemistry
Volume	11
Issue number	1
DOIs	https://doi.org/10.1016/S0968-0896(02)00305-X
Publication status	Published - 2003

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

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.",

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AU - Klimkait, T.

AU - Gilbert, I. H.

AU - Simons, C.

PY - 2003

Y1 - 2003

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AB - 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.

U2 - 10.1016/S0968-0896(02)00305-X

DO - 10.1016/S0968-0896(02)00305-X

M3 - Article

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JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 1

ER -

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

Abstract

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