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
Full Text: HTML
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.
Related Articles:
Direct force measurement between cucurbit [6] uril and spermine using atomic force microscopy
[Kim, Jeonghan; Kim, Youngkook; Baek, Kangkyun; Ko, Young Ho; Kim, Dongwoo; Kim, Kimoon Tetrahedron, 2008 , vol. 64, # 36 p. 8389 - 8393]
[Jasys, V. John; Kelbaugh, Paul B.; Nason, Deane M.; Phillips, Douglas; Rosnack, Kenneth J.; Saccomano, Nicholas A.; Stroh, Justin G.; Volkmann, Robert A. Journal of the American Chemical Society, 1990 , vol. 112, # 18 p. 6696 - 6704]