Page last updated: 2024-12-06

zidovudine triphosphate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Zidovudine triphosphate (AZTTP) is the active intracellular metabolite of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor (NRTI) used in the treatment of HIV infection. AZT is converted to AZTTP within cells by cellular kinases. AZTTP acts as a substrate for HIV reverse transcriptase, but it lacks a 3'-hydroxyl group, preventing the elongation of the growing viral DNA chain. This chain termination inhibits viral replication. AZTTP has been extensively studied due to its role in the treatment of HIV infection and its potential use in the development of new antiretroviral therapies. Its mechanism of action, pharmacokinetics, and clinical efficacy have been extensively investigated. AZTTP is a crucial component in the treatment of HIV, helping to slow the progression of the disease and improve the lives of individuals living with HIV.'

Cross-References

ID SourceID
PubMed CID455742
SCHEMBL ID21067527
MeSH IDM0149951
PubMed CID72187
CHEMBL ID193952
SCHEMBL ID19808965
MeSH IDM0149951

Synonyms (58)

Synonym
3'-azido-2',3'-dideoxythymidine-5'-diphosphate
{[3-(diazoazamvinyl)-5-(5-methyl-2,4-dioxo(1,3-dihydropyrimidinyl))oxolan-2-yl]methoxy}(hydroxyphosphoryl) dihydrogen phosphate
azt-diphosphate
azt-dp
[(2s,3s,5r)-3-azido-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)tetrahydrofuran-2-yl]methyl phosphono hydrogen phosphate
azddtdp
DB04542
aztdp
3'-azido-3'-deoxythymidine 5'-diphosphate
zidovudine diphosphate
[(2s,3s,5r)-3-azido-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methyl phosphono hydrogen phosphate
k7zg448v5m ,
106060-89-3
unii-k7zg448v5m
thymidine 5'-(trihydrogen diphosphate), 3'-azido-3'-deoxy-
azt diphosphate
3'-azido-3'-deoxythymidine 5'-(trihydrogen diphosphate)
3/'-azido-3/'-deoxythymidine 5/'-diphosphate
SCHEMBL21067527
Q27282068
combivir
zidovudine triphosphate
nsc742231
[[(2s,3s,5r)-3-azido-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)tetrahydrofuran-2-yl]methoxy-hydroxy-phosphoryl] phosphono hydrogen phosphate
thymidine 5'-(tetrahydrogen triphosphate), 3'-azido-3'-deoxy-
azt-triphospate
n3dttp
azddttp
3'-n3-dttp
azidothymidine triphosphate
3'-azido-2',3'-dideoxythymidine-5'- triphosphate
3'-azido-dttp
azttp ,
azt-tp
3'-azidothymidine triphosphate
zidovudine 5'-triphosphate
3'-azido-3'-deoxythymidine 5'-triphosphate
3'-azido-2',3'-dideoxythymidine-5'-triphosphate
erythro-azt-tp
dttp(3'n3)
1-(3'-azido-2',3'-dideoxy-beta-d-xylofuranosyl)thymine 5'-triphosphate
azt triphosphate
3'-deoxy-3'-azidothymidine triphosphate
[[(2s,3s,5r)-3-azido-5-(5-methyl-2,4-dioxopyrimidin-1-yl)oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate
CHEMBL193952
92586-35-1
6rgf96r053 ,
unii-6rgf96r053
bdbm50370476
3'-azido-3'-deoxythymidine triphosphate
DTXSID80239053
GLWHPRRGGYLLRV-XLPZGREQSA-N
SCHEMBL19808965
zidovudine-5'-triphosphate
azidothymidine-5'-triphosphate
Q27265380
HY-116364
CS-0065212

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Therapies including nucleoside analogs are associated with severe toxic side effects and acquirement of drug resistance."( Formulations of biodegradable Nanogel carriers with 5'-triphosphates of nucleoside analogs that display a reduced cytotoxicity and enhanced drug activity.
Han, HY; Kohli, E; Vinogradov, SV; Zeman, AD, 2007
)
0.34

Pharmacokinetics

ExcerptReferenceRelevance
" Intersubject pharmacokinetic variability for zidovudine is substantial, but intravenous therapy provides plasma concentrations and intracellular zidovudine triphosphate levels consistent with high antiviral activity."( Systemic pharmacokinetics and cellular pharmacology of zidovudine in human immunodeficiency virus type 1-infected women and newborn infants.
Bardeguez, AD; Blanchard, S; Flynn, PM; Fridland, A; Jimenez, E; Robbins, B; Rodman, JH; Rodriguez, JF, 1999
)
0.5
" A pharmacodynamic model that superimposes the pharmacokinetics of anti-HIV nucleoside reverse transcription (RT) and protease inhibitors over a previously published predator-prey model of HIV and CD4 dynamics was developed to address this need."( Development of a pharmacodynamic model for HIV treatment with nucleoside reverse transcriptase and protease inhibitors.
Hurwitz, SJ; Schinazi, RF, 2002
)
0.31
" Here, we use population pharmacokinetic (PK) modeling-based methods to simultaneously describe parent and intracellular metabolite PK in blood, semen, and PBMCs and SMCs."( Pharmacokinetic Modeling of Lamivudine and Zidovudine Triphosphates Predicts Differential Pharmacokinetics in Seminal Mononuclear Cells and Peripheral Blood Mononuclear Cells.
Bridges, AS; Cohen, MS; Dumond, JB; Fiscus, SA; Forrest, A; Kashuba, AD; Kendrick, R; Reddy, YS; Troiani, L; Yang, KH, 2015
)
0.68

Compound-Compound Interactions

ExcerptReferenceRelevance
"Didanosine (ddI) is used in the treatment of HIV-1 infection alone and in combination with azidothymidine (AZT)."( Pharmacodynamic studies (PD) of didanosine (ddI) alone and in combination with azidothymidine (AZT) in human T-cells; a stochastic biochemical approach to antiretroviral nucleoside drug combination in inhibiting HIV-reverse transcriptase (RT).
Avramis, VI; Nandy, P; Periclou, AP,
)
0.13

Dosage Studied

ExcerptRelevanceReference
"In vitro studies of zidovudine (ZDV) phosphorylation may not accurately reflect the in vivo dose-response relationship, which is crucial to determining the relationship between ZDV exposure, efficacy, and toxicity."( Intracellular zidovudine (ZDV) and ZDV phosphates as measured by a validated combined high-pressure liquid chromatography-radioimmunoassay procedure.
Hamzeh, FM; Kornhauser, DM; Kuwahara, SK; Lewis, LD; Lietman, PS; Slusher, JT, 1992
)
0.28
"The plasma and intracellular phosphorylated metabolite concentrations of ZDV were determined over a 12 h period following oral administration of 100 and 300 mg ZDV to 10 HIV-seropositive patients at steady state during two dosing regimens (i."( The effect of zidovudine dose on the formation of intracellular phosphorylated metabolites.
Back, DJ; Barry, MG; Breckenridge, AM; Gibbons, SE; Hoggard, PG; Khoo, SH; Veal, GJ; Wilkins, EG; Williams, O, 1996
)
0.29
"In vitro studies of zidovudine (ZDV) phosphorylation may not accurately reflect the in vivo dose-response relationship, which is crucial to determining the relationship between ZDV exposure, efficacy, and toxicity."( Intracellular zidovudine (ZDV) and ZDV phosphates as measured by a validated combined high-pressure liquid chromatography-radioimmunoassay procedure.
Hamzeh, FM; Kornhauser, DM; Kuwahara, SK; Lewis, LD; Lietman, PS; Slusher, JT, 1992
)
0.28
"The plasma and intracellular phosphorylated metabolite concentrations of ZDV were determined over a 12 h period following oral administration of 100 and 300 mg ZDV to 10 HIV-seropositive patients at steady state during two dosing regimens (i."( The effect of zidovudine dose on the formation of intracellular phosphorylated metabolites.
Back, DJ; Barry, MG; Breckenridge, AM; Gibbons, SE; Hoggard, PG; Khoo, SH; Veal, GJ; Wilkins, EG; Williams, O, 1996
)
0.29
" Data including demographic information, immunological markers (CD2+, CD3+, CD4+, CD5+/19+, CD8+, CD16+, CD19+, CD38+/8+ lymphocytes), hematologic function (absolute neutrophil count, white blood cell with differential, hemoglobin, and red blood cell count), concurrent medications, and dosage regimens were obtained."( Phosphorylated zidovudine concentrations in mononuclear cells in pediatric patients with human immunodeficiency virus infections.
Baker, RC; Brady, MT; Hunkler, JA; McOwen, NM; Nahata, MC; Sobol, BJ; Wintermeyer, SM, 1997
)
0.3
" Based on these findings this pharmacodynamic model can be applied to predict starting doses for a new agent based on simulated biological responses as a function of time for dosage regimens comprising one or two agents."( Development of a pharmacodynamic model for HIV treatment with nucleoside reverse transcriptase and protease inhibitors.
Hurwitz, SJ; Schinazi, RF, 2002
)
0.31
" In conclusion, with the persistence of 4'-Ed4TTP and persistent anti-HIV activity in cells, we anticipate less frequent dosing and fewer patient compliance issues than for D4T."( Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
Baba, M; Cheng, YC; Dutschman, GE; Grill, SP; Hu, R; Lam, W; Paintsil, E; Tanaka, H, 2007
)
0.34
"Phase 0 studies can provide initial pharmacokinetics (PKs) data in humans and help to facilitate early drug development, but their predictive value for standard dosing is controversial."( Biphasic elimination of tenofovir diphosphate and nonlinear pharmacokinetics of zidovudine triphosphate in a microdosing study.
Chen, J; Flexner, C; Fuchs, EJ; Hendrix, CW; Liberman, RG; Louissaint, NA; Skipper, PL; Tannenbaum, SR, 2012
)
0.61
" Blood samples were obtained from 14 infants on postdelivery days (PDD) 1, 7, 14, and 28 and from 17 infants at 0 and 4 hours after dosing on PDD-1."( High Plasma Concentrations of Zidovudine (AZT) Do Not Parallel Intracellular Concentrations of AZT-Triphosphates in Infants During Prevention of Mother-to-Child HIV-1 Transmission.
Gatanaga, H; Ha, do Q; Hosokawa, S; Kato, S; Kikuchi, Y; Kinai, E; Kinh, NV; Lam, NV; Liem, NT; Oka, S; Sadatsuki, M, 2016
)
0.43
" A safer dosage needs to be determined because high pAZT levels do not parallel those of icAZT-TP."( High Plasma Concentrations of Zidovudine (AZT) Do Not Parallel Intracellular Concentrations of AZT-Triphosphates in Infants During Prevention of Mother-to-Child HIV-1 Transmission.
Gatanaga, H; Ha, do Q; Hosokawa, S; Kato, S; Kikuchi, Y; Kinai, E; Kinh, NV; Lam, NV; Liem, NT; Oka, S; Sadatsuki, M, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pathways (1)

PathwayProteinsCompounds
Zidovudine Action Pathway05

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA polymerase catalytic subunitHuman alphaherpesvirus 1 strain KOSIC50 (µMol)3.30000.43801.86903.3000AID340465
DNA polymerase catalytic subunitHuman alphaherpesvirus 1 strain 17IC50 (µMol)3.30000.50001.46673.3000AID255129
DNA polymerase betaHomo sapiens (human)IC50 (µMol)16.00001.40006.56679.0000AID355062
DNA polymerase catalytic subunitHuman herpesvirus 5 strain AD169IC50 (µMol)22.10000.40001.31742.5000AID255119; AID307427
DNA polymerase catalytic subunitHuman herpesvirus 3 strain DumasIC50 (µMol)8.90000.28001.93005.8000AID255124
DNA polymerase alpha catalytic subunitHomo sapiens (human)IC50 (µMol)12.20001.00002.74294.3000AID255106; AID355060
DNA polymerase delta catalytic subunitHomo sapiens (human)IC50 (µMol)2.30002.30002.30002.3000AID255107
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.98350.00011.076810.0000AID1636131; AID198395; AID241929; AID323427; AID323429; AID323441; AID323443; AID355050; AID360704; AID360705; AID405417
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Ki0.05970.00031.552310.0000AID238445; AID341970; AID341972
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Kd18.07710.00062.40599.8000AID432585; AID432586; AID432587; AID432588; AID572771; AID618865; AID618875
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protease Human immunodeficiency virus 1ID5054.00000.00140.85491.7000AID162539
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (38)

Processvia Protein(s)Taxonomy
nucleotide-excision repair, DNA gap fillingDNA polymerase betaHomo sapiens (human)
in utero embryonic developmentDNA polymerase betaHomo sapiens (human)
DNA-templated DNA replicationDNA polymerase betaHomo sapiens (human)
DNA repairDNA polymerase betaHomo sapiens (human)
base-excision repairDNA polymerase betaHomo sapiens (human)
base-excision repair, gap-fillingDNA polymerase betaHomo sapiens (human)
pyrimidine dimer repairDNA polymerase betaHomo sapiens (human)
inflammatory responseDNA polymerase betaHomo sapiens (human)
DNA damage responseDNA polymerase betaHomo sapiens (human)
salivary gland morphogenesisDNA polymerase betaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageDNA polymerase betaHomo sapiens (human)
response to gamma radiationDNA polymerase betaHomo sapiens (human)
somatic hypermutation of immunoglobulin genesDNA polymerase betaHomo sapiens (human)
response to ethanolDNA polymerase betaHomo sapiens (human)
lymph node developmentDNA polymerase betaHomo sapiens (human)
spleen developmentDNA polymerase betaHomo sapiens (human)
homeostasis of number of cellsDNA polymerase betaHomo sapiens (human)
neuron apoptotic processDNA polymerase betaHomo sapiens (human)
response to hyperoxiaDNA polymerase betaHomo sapiens (human)
immunoglobulin heavy chain V-D-J recombinationDNA polymerase betaHomo sapiens (human)
DNA biosynthetic processDNA polymerase betaHomo sapiens (human)
double-strand break repair via nonhomologous end joiningDNA polymerase betaHomo sapiens (human)
DNA repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleotide-excision repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA synthesis involved in UV-damage excision repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA synthesis involved in DNA repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replicationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replication, synthesis of primerDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replication initiationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA strand elongation involved in DNA replicationDNA polymerase alpha catalytic subunitHomo sapiens (human)
leading strand elongationDNA polymerase alpha catalytic subunitHomo sapiens (human)
lagging strand elongationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
double-strand break repair via nonhomologous end joiningDNA polymerase alpha catalytic subunitHomo sapiens (human)
regulation of type I interferon productionDNA polymerase alpha catalytic subunitHomo sapiens (human)
mitotic DNA replication initiationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA synthesis involved in DNA repairDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA replicationDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA-templated DNA replicationDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA repairDNA polymerase delta catalytic subunitHomo sapiens (human)
base-excision repair, gap-fillingDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleotide-excision repair, DNA gap fillingDNA polymerase delta catalytic subunitHomo sapiens (human)
response to UVDNA polymerase delta catalytic subunitHomo sapiens (human)
cellular response to UVDNA polymerase delta catalytic subunitHomo sapiens (human)
fatty acid homeostasisDNA polymerase delta catalytic subunitHomo sapiens (human)
error-free translesion synthesisDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA biosynthetic processDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA replication proofreadingDNA polymerase delta catalytic subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
damaged DNA bindingDNA polymerase betaHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase betaHomo sapiens (human)
DNA-(apurinic or apyrimidinic site) endonuclease activityDNA polymerase betaHomo sapiens (human)
protein bindingDNA polymerase betaHomo sapiens (human)
microtubule bindingDNA polymerase betaHomo sapiens (human)
lyase activityDNA polymerase betaHomo sapiens (human)
enzyme bindingDNA polymerase betaHomo sapiens (human)
metal ion bindingDNA polymerase betaHomo sapiens (human)
5'-deoxyribose-5-phosphate lyase activityDNA polymerase betaHomo sapiens (human)
class I DNA-(apurinic or apyrimidinic site) endonuclease activityDNA polymerase betaHomo sapiens (human)
nucleotide bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
chromatin bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase alpha catalytic subunitHomo sapiens (human)
protein bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
zinc ion bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
protein kinase bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replication origin bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
single-stranded DNA bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleotide bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
chromatin bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
damaged DNA bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase delta catalytic subunitHomo sapiens (human)
protein bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
enzyme bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
metal ion bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
4 iron, 4 sulfur cluster bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
3'-5'-DNA exonuclease activityDNA polymerase delta catalytic subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (17)

Processvia Protein(s)Taxonomy
nucleusDNA polymerase betaHomo sapiens (human)
nucleoplasmDNA polymerase betaHomo sapiens (human)
cytoplasmDNA polymerase betaHomo sapiens (human)
microtubuleDNA polymerase betaHomo sapiens (human)
spindle microtubuleDNA polymerase betaHomo sapiens (human)
protein-containing complexDNA polymerase betaHomo sapiens (human)
nucleusDNA polymerase betaHomo sapiens (human)
nucleusDNA polymerase alpha catalytic subunitHomo sapiens (human)
nuclear envelopeDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleoplasmDNA polymerase alpha catalytic subunitHomo sapiens (human)
alpha DNA polymerase:primase complexDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleolusDNA polymerase alpha catalytic subunitHomo sapiens (human)
cytosolDNA polymerase alpha catalytic subunitHomo sapiens (human)
nuclear matrixDNA polymerase alpha catalytic subunitHomo sapiens (human)
chromatinDNA polymerase alpha catalytic subunitHomo sapiens (human)
chromosome, telomeric regionDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleusDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleoplasmDNA polymerase delta catalytic subunitHomo sapiens (human)
cytosolDNA polymerase delta catalytic subunitHomo sapiens (human)
membraneDNA polymerase delta catalytic subunitHomo sapiens (human)
aggresomeDNA polymerase delta catalytic subunitHomo sapiens (human)
delta DNA polymerase complexDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleotide-excision repair complexDNA polymerase delta catalytic subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (121)

Assay IDTitleYearJournalArticle
AID323417Inhibition of HIV1 reverse transcriptase wild type HXB2(a) in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323454Inhibition of HIV1 reverse transcriptase 41L/69S-SG/184V/210W/215Y mutant in presence of 5'-A12-(GACT)5-3' by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID282614Stability in CEM cell extract2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Synthesis of AZT 5'-triphosphate mimics and their inhibitory effects on HIV-1 reverse transcriptase.
AID323461Activity of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID481586Inhibition of VZV KOS DNA polymerase infected in HFF cells2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID241929Inhibitory concentration against human immunodeficiency virus type 1 reverse transcriptase2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase.
AID432621Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y mutant relative to wild type2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID307437Inhibition of human DNA polymerase delta by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID1636131Inhibition of HIV1 reverse transcriptase using T19-Cy5 labeled 23-mer DNA/T2-TAMRA labeled 63-mer DNA as primer/template assessed as inhibition of dNTP incorporation into primer/template2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID572771Binding affinity to HIV1 reverse transcriptase2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.
AID323434Inhibition of HIV1 reverse transcriptase 41L/67N/70R/184V/210W/215Y mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID355062Inhibition of DNA polymerase beta1996Journal of natural products, Sep, Volume: 59, Issue:9
Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii.
AID355050Inhibition of DNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p511996Journal of natural products, Sep, Volume: 59, Issue:9
Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii.
AID618876Ratio Kpol to Kd for wild type HIV 1 reverse transcriptase2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.
AID323440Inhibition of HIV1 LAI reverse transcriptase 41L/67N/70R/215Y/219Q mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID255106Inhibition of human alpha DNA polymerase (95 uL) activity in a solution containg 6.4 mM HEPES (pH 7.5) upon incubation for 12 minutes at 26 degrees C with the compound dissolved in DMSO2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID360704Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID238445Inhibitory constant against HIV-1 reverse transcriptase2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.
AID323429Inhibition of HIV1 pNL4-3 reverse transcriptase wild type pNL4-3 in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID432588Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID341975Ratio of Ki/Km for HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant to Ki/Km for wild-type reverse transcriptase2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
AID340468Inhibition of human polymerase delta by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID432622Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V mutant relative to wild type2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID432586Binding affinity to HIV1 LAI reverse transcriptase M184V mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID405416Inhibition of PERV reverse transcriptase from Kagoshima pig DRK4 cells2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
AID323423Inhibition of HIV1 reverse transcriptase 75I/77L/116Y/151M mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID1636135Inhibition of Escherichia coli RNA polymerase2016Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15
Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID323426Inhibition of HIV1 LAI reverse transcriptase 41L/67N/70R/215Y/219Q mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323437Inhibition of HIV1 reverse transcriptase 75I/77L/116Y/151M mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323450Inhibition of HIV1 reverse transcriptase wild type HXB2(a) in presence of 5'-A12-(GACT)5-3' by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323442Inhibition of HIV1 LAI reverse transcriptase 65R mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323433Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID432589Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V/G333D mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID83422The inhibition of compound was determined by reverse transcriptase assay using RNA as template1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
1-(2,3-Dideoxy-beta-D-glycero-pent-2-enofuranosyl)thymine. A highly potent and selective anti-HIV agent.
AID323449Inhibition of HIV1 reverse transcriptase wild type HXB2(a) in presence of 5'-A12-(GTCA)5-3' by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID432616Ratio of Kpol to Kd for HIV1 LAI reverse transcriptase M184V mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID255119Inhibition of human cytomegalovirus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID360705Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID323462Activity of HIV1 reverse transcriptase 41L/69S-SG/184V/210W/215Y mutant in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323430Inhibition of HIV1 pNL4-3 reverse transcriptase 115F mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID464099Inhibition of Varicella zoster virus recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase.
AID323424Inhibition of HIV1 reverse transcriptase 75I/77L/116Y/151M/184V mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID341973Ratio of Ki for HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant to Ki for wild-type reverse transcriptase2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
AID355060Inhibition of DNA polymerase alpha1996Journal of natural products, Sep, Volume: 59, Issue:9
Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii.
AID464096Inhibition of HCMV recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase.
AID405414Inhibition of PERV reverse transcriptase from pig PK15 cells2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
AID323463Activity of HIV1 reverse transcriptase wild type HXB2(b) in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323425Inhibition of HIV1 reverse transcriptase wild type HXB2(b) in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID282610Inhibition of HIV1 reverse transcriptase2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Synthesis of AZT 5'-triphosphate mimics and their inhibitory effects on HIV-1 reverse transcriptase.
AID618865Binding affinity to HIV1 reverse transcriptase assessed as L-3'-azido-NTP incorporation in nascent DNA2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.
AID341971Ratio of Ki to Km for HIV1 reverse transcriptase by steady state nucleotide incorporation assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
AID340466Inhibition of VZV DNA polymerase by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID340464Inhibition of HCMV DNA polymerase by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID323443Inhibition of HIV1 pNL4-3 reverse transcriptase wild type pNL4-3 by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323421Inhibition of HIV1 reverse transcriptase 41L/69S-SG/210W/215Y mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323418Inhibition of HIV1 reverse transcriptase 184V mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID1053517Binding affinity to HIV1 reverse transcriptase assessed as compound incorporation into DNA by primer extension assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus.
AID432620Binding affinity to HIV1 LAI reverse transcriptase M184V mutant relative to wild type2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID432618Ratio of Kpol to Kd for HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID341972Inhibition of HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant by steady state nucleotide incorporation assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
AID323420Inhibition of HIV1 reverse transcriptase 41L/67N/70R/184V/210W/215Y mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID299449Inhibition of human DNA polymerase delta2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID572772Ratio of Kpol to Kd for HIV1 reverse transcriptase2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.
AID323458Inhibition of HIV1 reverse transcriptase wild type HXB2(b) in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323428Inhibition of HIV1 LAI reverse transcriptase 65R mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323419Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID307427Inhibition of HCMV DNA polymerase by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID432617Ratio of Kpol to Kd for HIV1 LAI reverse transcriptase M41L/L210W/T215Y mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID572770Activity at HIV1 reverse transcriptase measured after 30 mins2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.
AID299437Inhibition of human cytomegalovirus DNA polymerase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID282613Stability in fetal calf serum at 500 uM at 37 degC2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Synthesis of AZT 5'-triphosphate mimics and their inhibitory effects on HIV-1 reverse transcriptase.
AID307428Inhibition of HSV1 DNA polymerase by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID323448Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 20 uM dNTP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323456Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323435Inhibition of HIV1 reverse transcriptase 41L/69S-SG/210W/215Y mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID307429Inhibition of VZV DNA polymerase by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID432623Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V/G333D mutant relative to wild type2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID299441Inhibition of VZV DNA polymerase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID323460Activity of HIV1 reverse transcriptase wild type HXB2(a) in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID432615Ratio of Kpol to Kd for wild type HIV1 LAI reverse transcriptase2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID255124Inhibition of Varicella-Zoster virus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID255129Inhibition of herpes simplex virus type 1 DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID432587Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID334986Inhibition of HIV reverse transcriptase assessed as incorporation of [3H]dTMP at 100 nM
AID323451Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 5'-A12-(GTCA)5-3' by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID198395Tested against HIV-1 reverse transcriptase (HIV-1 RT) with poly(rA)/(dT)12-18 as template and [methyl-3H]-dTTP as competing substrate1994Journal of medicinal chemistry, Oct-28, Volume: 37, Issue:22
The synthesis of nucleoside 5'-O-(1,1-dithiotriphosphates).
AID405415Inhibition of PERV reverse transcriptase from Kagoshima pig KK5 cells2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
AID432585Binding affinity to wild type HIV1 LAI reverse transcriptase2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID323422Inhibition of HIV1 reverse transcriptase 41L/69S-SG/184V/210W/215Y mutant in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323464Activity of HIV1 reverse transcriptase 41L/67N/70R/215Y/219Q mutant in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323457Inhibition of HIV1 reverse transcriptase 41L/69S-SG/184V/210W/215Y mutant in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID481584Inhibition of HSV1 KOS DNA polymerase infected in african green monkey Vero cells2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID323445Inhibition of HIV1 reverse transcriptase wild type HXB2(a) in presence of 1 uM dNTP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID405417Inhibition of HIV1 recombinant reverse transcriptase2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
AID323438Inhibition of HIV1 reverse transcriptase 75I/77L/116Y/151M/184V mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID340465Inhibition of HSV1 DNA polymerase by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID323444Inhibition of HIV1 pNL4-3 reverse transcriptase 115F mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323452Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 5'-A12-(GACT)5-3' by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323446Inhibition of HIV1 reverse transcriptase wild type HXB2(a) in presence of 20 uM dNTP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID162539Evaluated for the inhibition of HIV-1 Protease.1996Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching.
AID237107Half-life determined in fetal calf serum2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase.
AID323447Inhibition of HIV1 reverse transcriptase 41L/67N/70R/210W/215Y mutant in presence of 1 uM dNTP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323432Inhibition of HIV1 reverse transcriptase 184V mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323453Inhibition of HIV1 reverse transcriptase 41L/69S-SG/184V/210W/215Y mutant in presence of 5'-A12-(GTCA)5-3' by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323459Inhibition of HIV1 reverse transcriptase 41L/67N/70R/215Y/219Q mutant in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID341974Ratio of Ki to Km for HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant by steady state nucleotide incorporation assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
AID323427Inhibition of HIV1 LAI reverse transcriptase wild type in presence of 5 mM ATP by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323455Inhibition of HIV1 reverse transcriptase wild type HXB2(a) in presence of 3.2 mM ATP by prA/odT assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID618935Selectivity ratio of Kpol to Kd for TTP to Kpol to Kd for compound at HIV1 reverse transcriptase2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.
AID323431Inhibition of HIV1 reverse transcriptase wild type HXB2(a) by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID299440Inhibition of HSV1 DNA polymerase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID323436Inhibition of HIV1 reverse transcriptase 41L/69S-SG/184V/210W/215Y mutant by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID432619Ratio of Kpol to Kd for HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V/G333D mutant2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Mechanisms by which the G333D mutation in human immunodeficiency virus type 1 Reverse transcriptase facilitates dual resistance to zidovudine and lamivudine.
AID572764Selectivity, ratio of Kpol to Kd for TTP to Kpol to Kd for compound at HIV1 reverse transcriptase2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Anti-human immunodeficiency virus activity, cross-resistance, cytotoxicity, and intracellular pharmacology of the 3'-azido-2',3'-dideoxypurine nucleosides.
AID323439Inhibition of HIV1 reverse transcriptase wild type HXB2(b) by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID323441Inhibition of HIV1 LAI reverse transcriptase wild type LAI by heteropolymeric DNA polymerase assay2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Biochemical studies on the mechanism of human immunodeficiency virus type 1 reverse transcriptase resistance to 1-(beta-D-dioxolane)thymine triphosphate.
AID618875Binding affinity to HIV1 reverse transcriptase M184V mutant assessed as L-3'-azido-NTP incorporation in nascent DNA2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides.
AID255107Inhibition of human delta DNA polymerase (95 uL) activity in a solution containg 6.4 mM HEPES (pH 7.5) upon incubation for 12 minutes at 26 degrees C with the compound dissolved in DMSO2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID83421The inhibition of compound was determined by reverse transcriptase assay using DNA as template1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
1-(2,3-Dideoxy-beta-D-glycero-pent-2-enofuranosyl)thymine. A highly potent and selective anti-HIV agent.
AID481581Inhibition of HCMV DNA polymerase infected in HFF cells2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID341970Inhibition of HIV1 reverse transcriptase by steady state nucleotide incorporation assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of the translocation status of human immunodeficiency virus type 1 reverse transcriptase on the efficiency of excision of tenofovir.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (192)

TimeframeStudies, This Drug (%)All Drugs %
pre-199012 (6.25)18.7374
1990's89 (46.35)18.2507
2000's67 (34.90)29.6817
2010's22 (11.46)24.3611
2020's2 (1.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index17.50 (24.57)
Research Supply Index5.32 (2.92)
Research Growth Index5.18 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (9.09%)5.53%
Trials4 (2.01%)5.53%
Reviews0 (0.00%)6.00%
Reviews3 (1.51%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
Other192 (96.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]