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

TY - JOUR

T1 - Solid-phase synthesis of diamine and polyamine amino acid derivatives as HIV-1 Tat-TAR binding inhibitors

AU - Jimenez Bueno, G.

AU - Klimkait, T.

AU - Gilbert, I. H.

AU - Simons, C.

PY - 2003

Y1 - 2003

N2 - 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.

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

SN - 0968-0896

VL - 11

SP - 87

EP - 94

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 1

ER -