Activity of the (R)-Enantiomers of 9-(2-phosphonylmethoxypropyl)-adenine and 9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine against human immunodeficiency virus in different human cell systems

J. Balzarini, S. Aquaro, C. F. Perno, M. Witvrouw, A. Holý, E. De Clercq

Research output: Contribution to journalArticle

Abstract

The (S)- and (R)-enantiomers of 9-(2-phosphonylmethoxypropyl) derivatives of adenine (PMPA) and 2,6-diaminopurine (PMPDAP) were evaluated for their inhibitory effect on HIV replication in several human cell systems, including natural peripheral blood lymphocytes (PBL) and freshly isolated monocyte/macrophages (M/M). The (R)-enantiomers of PMPDAP and PMPA were ~10- to 100-fold more effective against HIV than their (S)-enantiomeric counterparts. The antiviral efficacy of (R)-PMPA was comparable to that of the prototype acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine (PMEA). The most potent and selective HIV inhibitor was (R)-PMPDAP. Its 50% effective concentration ranged from 0.01 μM for HIV-1/Ba-L in M/M to 1-2.8 μM for HIV-1/III(B), and HIV-1/HE in C8166, GEM, Molt/4, MT-4 and PBL cells. Both (R)-PMPA and (R)-PMPDAP were not toxic to the host cells at 300 μM.

Original languageEnglish
Pages (from-to)337-341
Number of pages5
JournalBiochemical and Biophysical Research Communications
Volume219
Issue number2
DOIs
Publication statusPublished - Feb 15 1996

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

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