BIOMAT Database Logo BIOMAT Database Logo

Antiretroviral activities of acyclic nucleoside phosphonates [9-(2-phosphonylmethoxyethyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, (R)-9-(2-phosphonylmethoxypropyl)adenine, and MDL 74,968] in cell cultures and murine sarcoma virus-infected newborn NMRI mice. 1997

J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium.

From a side-by-side comparative study, the acyclic nucleoside phosphonates (R)-9-(2-phosphonylmethoxypropyl)adenine [(R)-PMPA] and 9-(2-methylidene-3-phosphonomethoxypropyl)guanine (MDL 74,968) proved more selective in their inhibitory effect on human immunodeficiency virus types 1 and 2, feline immunodeficiency virus, and Moloney murine sarcoma virus (MSV) in cell cultures than the 9-(2-phosphonylmethoxyethyl) derivatives of adenine (PMEA) and guanine (PMEG). In particular, PMEG proved quite toxic. PMEA, (R)-PMPA, and MDL 74,968 afforded a marked delay in MSV-induced tumor initiation in MSV-infected newborn NMRI mice and substantially delayed associated animal death at doses as low as 4 to 10 mg/kg of body weight. Treatment of the NMRI mice with PMEA, (R)-PMPA, and MDL 74,968 at 25 or 50 mg/kg resulted in a high percentage of long-term survivors.

UI MeSH Term Description Entries
D008809 Mice, Inbred C3H An inbred strain of mouse that is used as a general purpose strain in a wide variety of RESEARCH areas including CANCER; INFECTIOUS DISEASES; sensorineural, and cardiovascular biology research. Mice, C3H,Mouse, C3H,Mouse, Inbred C3H,C3H Mice,C3H Mice, Inbred,C3H Mouse,C3H Mouse, Inbred,Inbred C3H Mice,Inbred C3H Mouse
D009053 Sarcoma Viruses, Murine A group of replication-defective viruses, in the genus GAMMARETROVIRUS, which are capable of transforming cells, but which replicate and produce tumors only in the presence of Murine leukemia viruses (LEUKEMIA VIRUS, MURINE). Finkel-Biskis-Jinkins murine sarcoma virus,Mouse Sarcoma Viruses,FBJ-MSV,FBR-MSV,Finkel-Biskis-Reilly murine sarcoma virus,Finkel Biskis Jinkins murine sarcoma virus,Finkel Biskis Reilly murine sarcoma virus,Murine Sarcoma Viruses,Sarcoma Viruses, Mouse
D009943 Organophosphorus Compounds Organic compounds that contain phosphorus as an integral part of the molecule. Included under this heading is broad array of synthetic compounds that are used as PESTICIDES and DRUGS. Organophosphorus Compound,Organopyrophosphorus Compound,Organopyrophosphorus Compounds,Compound, Organophosphorus,Compound, Organopyrophosphorus,Compounds, Organophosphorus,Compounds, Organopyrophosphorus
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D005347 Fibroblasts Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules. Fibroblast
D006147 Guanine
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000068698 Tenofovir An adenine analog REVERSE TRANSCRIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone. (R)-9-(2-phosphonylmethoxypropyl)adenine,9-(2-Phosphonomethoxypropyl)adenine,9-(2-Phosphonylmethoxypropyl)adenine,9-(2-Phosphonylmethoxypropyl)adenine, (+-)-isomer,9-(2-Phosphonylmethoxypropyl)adenine, (R)-isomer - T357098,9-(2-Phosphonylmethoxypropyl)adenine, (S)-isomer,9-PMPA (tenofovir),Tenofovir Disoproxil,Tenofovir Disoproxil Fumarate,Viread,Disoproxil Fumarate, Tenofovir,Disoproxil, Tenofovir,Fumarate, Tenofovir Disoproxil
D000225 Adenine A purine base and a fundamental unit of ADENINE NUCLEOTIDES. Vitamin B 4,4, Vitamin B,B 4, Vitamin
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Efficacy of the acyclic nucleoside phosphonates (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine (FPMPA) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against feline immunodeficiency virus.
February 1998, Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
5-Phosphoribosyl 1-pyrophosphate synthetase converts the acyclic nucleoside phosphonates 9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxyethyl)adenine directly to their antivirally active diphosphate derivatives.
May 1991, The Journal of biological chemistry,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Disposition of the acyclic nucleoside phosphonate (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine.
May 1998, Antimicrobial agents and chemotherapy,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Antimalarial and toxic effects of the acyclic nucleoside phosphonate (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine in Plasmodium berghei-infected mice.
July 1996, Antimicrobial agents and chemotherapy,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Inhibition of duck hepatitis B virus replication by 9-(2-phosphonylmethoxyethyl)adenine, an acyclic phosphonate nucleoside analogue.
December 1998, Antimicrobial agents and chemotherapy,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Prevention of murine AIDS development by (R)-9-(2-phosphonylmethoxypropyl)adenine.
August 1998, Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Treatment of visna virus infection in lambs with the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
May 1998, Antiviral chemistry & chemotherapy,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Potent antitumor activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine in choriocarcinoma-bearing rats.
May 1998, International journal of cancer,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
January 1996, Antimicrobial agents and chemotherapy,
J Balzarini, and T Vahlenkamp, and H Egberink, and K Hartmann, and M Witvrouw, and C Pannecouque, and P Casara, and J F Navé, and E De Clercq
Antiretroviral efficacy and pharmacokinetics of oral bis(isopropyloxycarbonyloxymethyl)-9-(2-phosphonylmethoxypropyl)adenine in mice.
July 1998, Antimicrobial agents and chemotherapy,
Copied contents to your clipboard!