Neamine derivatives having a nucleobase with a lysine or an arginine as a linker, their synthesis and evaluation as potential inhibitors for HIV TAR-Tat

Saki Yajima, Hirohito Shionoya, Takashi Akagi, Keita Hamasaki

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

Neamine derivatives bearing a nucleobase, adenine, cytosine, guanine or thymine with a lysine or an arginine as a linker have been synthesized and its potential as the inhibitor for HIV TAR-Tat interaction examined. Among them, modified neamine having an arginine-nucleobase showed a higher inhibition than that of the one having a lysine-nucleobase. The difference of the nucleobase anchor did not characterize inhibition specificity. Also, stereochemistry of the amino acid in the compounds causes no difference in the inhibition for TAR-Tat.

Original languageEnglish
Pages (from-to)2799-2809
Number of pages11
JournalBioorganic and Medicinal Chemistry
Volume14
Issue number8
DOIs
Publication statusPublished - 2006 Apr 15

Keywords

  • Aminoglycoside
  • Drug design
  • HIV TAR
  • HIV Tat
  • Inhibition
  • Neamine

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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