RT Journal Article
T1 Structure-Activity relationship studies on a TPR dendrimer with dual activities against HIV and enterovirus A71. Modifications on the amino acid
A1 Martínez Gualda, Belén V.
A1 Sun, Liang
A1 Rivero Buceta, Eva María
A1 Flores Aguilar-Amat, Aída
A1 Quesada Del Sol, Ernesto
A1 Balzarini, Jan
A1 Noppen, Sam
A1 Liekens, Sandra
A1 Schols, Dominique
A1 Neyts, Johan
A1 Leyssen, Pieter
A1 Mirabelli, Carmen
A1 Camarasa Rius, María José
A1 San Félix García, Ana Rosa
AB We have recently described a new class of dendrimers with tryptophan (Trp) on the surface that show dual antiviral activities against HIV and EV71 enterovirus. The prototype compound of this family is a pentaerythritol derivative with 12 Trps on the periphery. Here we complete the structure-activity relationship studies of this family to identify key features that might be significant for the antiviral activity. With this aim, novel dendrimers containing different amino acids (aromatic and non-aromatic), tryptamine (a “decarboxylated” analogue of Trp) and N-methyl Trp on the periphery have been prepared. Dendrimer with N-Methyl Trp was the most active against HIV-1 and HIV-2 while dendrimer with tyrosine was endowed with the most potent antiviral activity against EV71. This tyrosine dendrimer proved to inhibit a large panel of EV71 clinical isolates (belonging to different clusters) in the low nanomolar/high picomolar range. In addition, a new synthetic procedure (convergent approach) has been developed for the synthesis of the prototype and some other dendrimers. This convergent approach proved more efficient (higher yields, easier purification) than the divergent approach previously reported.
PB Elsevier
SN 0166-3542
YR 2017
FD 2017-03
LK https://hdl.handle.net/20.500.14352/99617
UL https://hdl.handle.net/20.500.14352/99617
LA eng
NO Martínez-Gualda B, Sun L, Rivero-Buceta E, Flores A, Quesada E, Balzarini J, et al. Structure-activity relationship studies on a Trp dendrimer with dual activities against HIV and enterovirus A71. Modifications on the amino acid. Antiviral Research 2017;139:32–40. https://doi.org/10.1016/j.antiviral.2016.12.010
NO Ministerio de Economía, Comercio y Empresa (España)
NO KU Leuven
NO Belgian Interuniversity Attraction Poles
NO China Scholarship Council
DS Docta Complutense
RD 19 mar 2026