In vitro activity of acyclic nucleoside phosphonate derivatives against feline immunodeficiency virus in Crandell feline kidney cell s and feline peripheral blood lymphocytes

K. Hartmann, J. Balzarini, J. Higgins, E. De Clercq, Niels C Pedersen

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16 Citations (Scopus)

Abstract

Several novel fluorinated acyclic nucleoside phosphonates [i.e. 9-(3-fluoro-2-phosphonylmethoxy propyl)adenine (FPMPA) and 9-(3-fluoro-2-phosphonylmethoxypropyl)-2,6-diaminopurine (FPMP-DAP)] were evaluated for their inhibitory effect against feline immunodeficiency virus (FIV) replication in Crandell feline kidney (CrFK) cells and feline peripheral blood lymphocytes (PBL) in vitro. Whereas 3'-azido-3'deoxythymidine (AZT) was not able to achieve complete suppression of viral antigen expression and reverse transcriptase activity in the FIV-infected cell culture supernatants at 25 μM, FPMPA, FPMPDAP, and the 9-(2-phosphonylmethoxyethyl)purine derivatives PMEA and PMEDAP fully protected FIV-infected cells at 5 μM. Both FPMPA and FPMPDAP were endowed with a higher antiviral potency and/or therapeutic selectivity than PMEA and PMEDAP in inhibiting FIV infection, mainly due to a markedly lower toxicity for the cell cultures.

Original languageEnglish (US)
Pages (from-to)13-19
Number of pages7
JournalAntiviral Chemistry and Chemotherapy
Volume5
Issue number1
StatePublished - 1994
Externally publishedYes

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Feline Immunodeficiency Virus
Organophosphonates
Felidae
Nucleosides
Lymphocytes
Kidney
Cell Culture Techniques
Zidovudine
Viral Antigens
RNA-Directed DNA Polymerase
Adenine
Virus Diseases
Virus Replication
Antiviral Agents
In Vitro Techniques
9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine

ASJC Scopus subject areas

  • Virology
  • Pharmacology

Cite this

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title = "In vitro activity of acyclic nucleoside phosphonate derivatives against feline immunodeficiency virus in Crandell feline kidney cell s and feline peripheral blood lymphocytes",
abstract = "Several novel fluorinated acyclic nucleoside phosphonates [i.e. 9-(3-fluoro-2-phosphonylmethoxy propyl)adenine (FPMPA) and 9-(3-fluoro-2-phosphonylmethoxypropyl)-2,6-diaminopurine (FPMP-DAP)] were evaluated for their inhibitory effect against feline immunodeficiency virus (FIV) replication in Crandell feline kidney (CrFK) cells and feline peripheral blood lymphocytes (PBL) in vitro. Whereas 3'-azido-3'deoxythymidine (AZT) was not able to achieve complete suppression of viral antigen expression and reverse transcriptase activity in the FIV-infected cell culture supernatants at 25 μM, FPMPA, FPMPDAP, and the 9-(2-phosphonylmethoxyethyl)purine derivatives PMEA and PMEDAP fully protected FIV-infected cells at 5 μM. Both FPMPA and FPMPDAP were endowed with a higher antiviral potency and/or therapeutic selectivity than PMEA and PMEDAP in inhibiting FIV infection, mainly due to a markedly lower toxicity for the cell cultures.",
author = "K. Hartmann and J. Balzarini and J. Higgins and {De Clercq}, E. and Pedersen, {Niels C}",
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AU - Hartmann, K.

AU - Balzarini, J.

AU - Higgins, J.

AU - De Clercq, E.

AU - Pedersen, Niels C

PY - 1994

Y1 - 1994

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AB - Several novel fluorinated acyclic nucleoside phosphonates [i.e. 9-(3-fluoro-2-phosphonylmethoxy propyl)adenine (FPMPA) and 9-(3-fluoro-2-phosphonylmethoxypropyl)-2,6-diaminopurine (FPMP-DAP)] were evaluated for their inhibitory effect against feline immunodeficiency virus (FIV) replication in Crandell feline kidney (CrFK) cells and feline peripheral blood lymphocytes (PBL) in vitro. Whereas 3'-azido-3'deoxythymidine (AZT) was not able to achieve complete suppression of viral antigen expression and reverse transcriptase activity in the FIV-infected cell culture supernatants at 25 μM, FPMPA, FPMPDAP, and the 9-(2-phosphonylmethoxyethyl)purine derivatives PMEA and PMEDAP fully protected FIV-infected cells at 5 μM. Both FPMPA and FPMPDAP were endowed with a higher antiviral potency and/or therapeutic selectivity than PMEA and PMEDAP in inhibiting FIV infection, mainly due to a markedly lower toxicity for the cell cultures.

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