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

GJ Bueno, T Klimkait, IH Gilbert, C Simons

Index: Bueno, G. Jimenez; Klimkait; Gilbert; Simons Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 1 p. 87 - 94

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Citation Number: 15

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.