Modelling, synthesis and biological evaluation of an ethidium-arginine conjugate linked to a ribonuclease mimic directed against TAR RNA of HIV-1.
Using molecular modelling studies, an active anti-HIV ethidium-arginine conjugate targeted against the viral TAR RNA sequence has been linked to an artificial ribonuclease, with the aim to obtain an irreversible inhibitor. The ribonuclease moiety consists of an N-[N-(3-aminopropyl)-3-aminopropyl] glycine and has been constructed via two successive N-alkylations following the Fukuyama procedure.
Laboratoire de Chimie Bio-organique, UNSA-CNRS UMR 6001, Université de Nice Sophia-Antipolis, 06108, Nice, France.
Nadia
N
Patino
Christophe
C
Di Giorgio
Cristina
C
Dan-Covalciuc
Valérie
V
Peytou
Raphaël
R
Terreux
Daniel
D
Cabrol-Bass
Christian
C
Bailly
Roger
R
Condom
D000478:Alkylation; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001120:Arginine / Q000737:chemistry; D004996:Ethidium / Q000031:analogs & derivatives* / Q000737:chemistry; D005998:Glycine / Q000737:chemistry; D016325:HIV Long Terminal Repeat / Q000187:drug effects*; D006801:Humans; D006868:Hydrolysis / Q000187:drug effects; D008024:Ligands; D008958:Models, Molecular; D018716:Molecular Mimicry; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D020871:RNA Stability / Q000187:drug effects; D012260:Ribonucleases / Q000737:chemistry*; D013696:Temperature
D019380:Anti-HIV Agents; D008024:Ligands; D001120:Arginine; D012260:Ribonucleases; D004996:Ethidium; D005998:Glycine