| Assay ID | Title | Year | Journal | Article |
|---|
| AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11
| 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500
| Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | | | |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
| Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | | | |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID717450 | Cytotoxicity against human CEM cells | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Synthesis, evaluation of anti-HIV-1 and anti-HCV activity of novel 2',3'-dideoxy-2',2'-difluoro-4'-azanucleosides. |
| AID211064 | In vitro percent of phosphorolysis after incubation with Escherichia coli thymidine phosphorylase for 10 min at 37 degree C | 1994 | Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
| Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT). |
| AID476929 | Human intestinal absorption in po dosed human | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
| Neural computational prediction of oral drug absorption based on CODES 2D descriptors. |
| AID1815386 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID259183 | Cytotoxicity in CEM cells | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
| Synthesis and antiviral evaluation of cyclic and acyclic 2-methyl-3-hydroxy-4-pyridinone nucleoside derivatives. |
| AID604020 | Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID542925 | Antiproliferative activity against human subcutaneous preadipocyte assessed as [3H]thymidine incorporation at 6 uM | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1275550 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID519866 | Antiviral activity against HIV1 subtype B-93US143 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID572780 | Ratio of IC50 for HIV1 harboring reverse transcriptase M184V mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID449349 | Inhibition of HIV1 wild type reverse transcriptase-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| The nucleoside analogue D-carba T blocks HIV-1 reverse transcription. |
| AID1391083 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID235441 | Selective index as the ratio of CC50 to that of IC50 value against MT-4 cells. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID458877 | Cytotoxicity against human MT4 cells by MTT assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| 5-Modified-2'-dU and 2'-dC as mutagenic anti HIV-1 proliferation agents: synthesis and activity. |
| AID1191971 | Antiviral activity against HIV1 3B infected infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
| AID1635809 | Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 8070-2 expressing integrase G140S/Q148H mutant to EC50 for HIV1 expressing wild-type integrase | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H. |
| AID1729153 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID78924 | Effective dose required to inhibit virus replication growth by 50% | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Antitumor agents. 166. Synthesis and biological evaluation of 5,6,7,8-substituted-2-phenylthiochromen-4-ones. |
| AID1737343 | Inhibition of recombinant HIV1 HXB2 reverse transcriptase RDDP activity assessed as reduction in biotin/digoxin-dU incorporation into polirA-oligodU template primer measured after 30 mins by ELISA | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis, in vitro and in silico studies of novel 4-oxoquinoline ribonucleoside derivatives as HIV-1 reverse transcriptase inhibitors. |
| AID198262 | Inhibitory concentration against human immunodeficiency virus type 1 (HIV-1 strain IIIB RT) reverse transcriptase was determined by triplicate assay at high (~1 pfu/cell) multiplicity of injection (moi) | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| (Z)- and (E)-2-((hydroxymethyl)cyclopropylidene)methyladenine and -guanine. New nucleoside analogues with a broad-spectrum antiviral activity. |
| AID21906 | Concentration in mouse blood 60 min post injection at a dose 240 mocromol/kg | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID46378 | Antiviral activity against site directed resistant isolate HIV-1 L100I in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID597659 | Cytotoxicity against human mock-infected MT4 cells after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT method. |
| AID81067 | Cytotoxicity against HIV-1 (human immunodeficiency virus type 1) | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
| Nucleosides and nucleotides. 183. Synthesis of 4'alpha-branched thymidines as a new type of antiviral agent. |
| AID310351 | Therapeutic index, ratio of IC50 for MT2 cells to EC50 for HIV1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Anti-AIDS agents 73: structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. |
| AID1199055 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for Human immunodeficiency virus type 2 ROD infected in human MT4 cells | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID1888700 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID548811 | Antiviral activity against HIV1 isolate 220 harboring reverse transcriptase K70E/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1064553 | Antiviral activity against HIV-1 infected in human CEM-TART cells assessed as protection against virus-induced cytopathicity after 96 hrs by MTT assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1
| 4-Quinolone alkaloids from Melochia odorata. |
| AID259181 | Antiviral activity against HIV1 IIIB in CEM cells | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
| Synthesis and antiviral evaluation of cyclic and acyclic 2-methyl-3-hydroxy-4-pyridinone nucleoside derivatives. |
| AID1368354 | Antiviral activity against HIV-1 3B infected in human TZM-bl cells at 10 uM treated 2 to 6 hrs post infection for 2 hrs followed by compound washout measured after 2 days by luciferase reporter assay | 2018 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
| Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41. |
| AID696750 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 | 2012 | Journal of natural products, Nov-26, Volume: 75, Issue:11
| Antiviral chromones from the stem of Cassia siamea. |
| AID291760 | Inhibition of HIV1 reverse transcriptase | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro. |
| AID29360 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
| QSAR model for drug human oral bioavailability. |
| AID701103 | Selectivity index, ratio of cytotoxic concentration for human MT4 cells to IC50 for HIV1 3B | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms. |
| AID576149 | Cytotoxicity against human PBMC assessed as cell viability at 10 uM by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID32074 | The compound was tested for anti HIV-activity (active) against ATH8 cell line | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14
| Correlation of anti-HIV activity with structure: use of electrostatic potential and conformational analysis. |
| AID1589125 | Selectivity index, ratio of IC50 for cytotoxicity in human NHDF cells to IC50 for cytotoxicity in human A549 cells | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID271060 | Antiviral activity against HIV1 FHR2 replication in MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID230269 | Ratio of TICD50 to that of IC50 of Rauscher-Murine leukemia virus (R-MuLv) | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia |
| AID81237 | Compound was evaluated for the antiviral activity against compound resistant virus isolate K103E with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID1546658 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells measured on day 3 post-infection by Nano-Glo luciferase assay | | | |
| AID350155 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as p24 antigen level after 4 days by ELISA | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. |
| AID718372 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
| AID104804 | Tested for the cytotoxic concentration required to reduce the number of viable mock infected MT-4 cells | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| 1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity. |
| AID235875 | Ratio of CD50 to ED50 rvaluated for inhibition of HIV replication in MT-4 cells | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
| Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides. |
| AID1410481 | Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
| AID1238317 | Antiviral activity against macrophage-tropic HIV1 NL(AD8) infected in human PM1 expressing CCR5 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID270072 | Antileishmanial activity against Leishmania donovani LV9 promastigotes by MTT method | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Structurally diverse 5-substituted pyrimidine nucleosides as inhibitors of Leishmania donovani promastigotes in vitro. |
| AID214085 | Effect against HIV-1 chronically infected promonocytic cell line U1 in the presence of PMA(phorbol 12-myristate 13-acetate) | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
| Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. |
| AID104967 | 50% effective concentration of compound which is required to protect human MT-4 cells against cytopathogenicity of HIV-1. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID1391084 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID548830 | Antiviral activity against HIV1 isolate 192 harboring reverse transcriptase M41L/T215Y mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1141965 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1316334 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID1457055 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID548839 | Antiviral activity against HIV1 isolate 215 harboring reverse transcriptase D67N/K70E mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID501755 | Cytotoxicity against human MT4 cells after 4 days | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
| Conjugates of betulin derivatives with AZT as potent anti-HIV agents. |
| AID1729151 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID231790 | Ratio of cytotoxic concentration (CC50) in test-I to that of EC50 of compound | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
| Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes. |
| AID1238311 | Cytotoxicity against human MT4 cells by MTT assay in presence of 5 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID79293 | Compound was evaluated for anti-HIV activity in acutely infected H9 Lymphocytes | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| Anti-AIDS agents. 33. Synthesis and anti-HIV activity of mono-methyl substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues. |
| AID81233 | Compound was evaluated for the antiviral activity against HIV-1 | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| Synthesis and antiviral activity of novel isodideoxy nucleosides with exocyclic methylene. |
| AID559940 | Antiviral activity against HIV1 R5 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID1610040 | Antiviral activity against HIV1 N119 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID47113 | In vitro inhibition of HIV-2 replication in human T-lymphocytic cells (CEM). | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID405345 | Toxicity against human HepG2/C3A cells assessed as effect on mitochondrial DNA copy numbers at 50 uM after 4 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID341365 | Drug level in human CD4+CEM cells per 10'9 cells at 0.1 uM | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID402093 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 3B | 1998 | Journal of natural products, Sep, Volume: 61, Issue:9
| Anti-AIDS agents. 30. Anti-HIV activity of oleanolic acid, pomolic acid, and structurally related triterpenoids. |
| AID706460 | Cytotoxicity against human MT4 cells after 2 days | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID373554 | Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication after 24 hrs by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID309233 | Reduction in cell viability of human H9 cells | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
| Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. |
| AID342548 | Antiviral activity against HIV1 infected human CEM-SS cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID1140742 | Antiviral activity against HIV1 HTLV-3B infected in human MT4 cells assessed as inhibition of virus proliferation by measuring host cell viability at 25 nM relative to control | 2014 | Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
| Synthesis and evaluation of phosphorus containing, specific CDK9/CycT1 inhibitors. |
| AID1737344 | Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by XTT assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Design, synthesis, in vitro and in silico studies of novel 4-oxoquinoline ribonucleoside derivatives as HIV-1 reverse transcriptase inhibitors. |
| AID1407645 | Cytotoxicity against human CEM-GFP cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
| AID1237701 | Antiviral activity against HIV2 ROD infected in human thymidine kinase deficient CEM/TK- cells assessed as reduction in virus-induced giant cell formation incubated for 4 to 5 days | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
| Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides. |
| AID1191401 | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID44664 | Ability to inhibit HIV-2 multiplication in acutely infected C8166 cells | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID735332 | Antiviral activity against deltaTat/rev deffective HIV-1 MC99 infected in human 1A2 cells assessed as inhibition of syncytia formation after 3 days | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4
| Cytotoxic, antitopoisomerase IIα, and anti-HIV-1 activities of triterpenoids isolated from leaves and twigs of Gardenia carinata. |
| AID405336 | Toxicity in human H9c2 cells assessed as induction of cell death at 50 uM after 12 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID1221968 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1220784 | Fraction unbound in mouse plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1391082 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID595595 | Cytotoxicity against human PBMC infected with Human immunodeficiency virus 1 LAV1 by MTS assay | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Broad-spectrum antiviral activity including human immunodeficiency and hepatitis C viruses mediated by a novel retinoid thiosemicarbazone derivative. |
| AID571592 | Half life in HIV-1 infected patient on day 10 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1391077 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID222690 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 48 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID291853 | Antiviral activity against HTLV1 in human PBMC at 5 uM | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID350157 | Cytotoxicity against human MT2 cells by XTT assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. |
| AID1757977 | Selectivity index, ratio of CC50 for human CEM-SS cells to EC50 for antiviral activity against HIV-1 infected in human CEM-SS cells | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID9852 | Effect against HIV-1 chronically infected promonocytic cell line ACH-2 cells in the presence of PMA(phorbol 12-myristate 13-acetate) | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
| Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. |
| AID257931 | Anti HIV activity against HIV1 NL4-3 in HeLa-CD4-LTR-beta-gal cells in MAGI-X4 assay | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent. |
| AID235220 | Therapeutic index of IC50 to EC50 | 1994 | Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
| Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT). |
| AID607873 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID105205 | Potency against non nucleoside reverse transcriptor was determined in MT-4 cells | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Threshold interaction energy of NRTI's (2'-deoxy 3'-substituted nucleosidic analogs of reverse transcriptase inhibitors) to undergo competitive inhibition. |
| AID780327 | Cytotoxicity against african green monkey Vero cells | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
| Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors. |
| AID198387 | Inhibitory effect on HIV-1 RT activity using template primer,poly (rA)-oligo (dT) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID83218 | Percent inhibition evaluated for anti-RT activity at 9 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID481802 | Activity of Ureaplasma parvum thymidine kinase by Michaelis-Menten plot | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID557279 | Ratio of EC50 for HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID548802 | Antiviral activity against HIV1 isolate 200 harboring reverse transcriptase M41L/L210W/T215Y mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID160452 | In vitro inhibitory activity against biotinylated human HIV-1 protease | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
| AID336314 | Cytotoxicity against human C8166 cells after 5 to 7 days by MTT-formazan method | 1992 | Journal of natural products, Aug, Volume: 55, Issue:8
| Constituents of Eriobotrya japonica. A study of their antiviral properties. |
| AID523483 | Antiviral activity against HIV1 with RT connection domain L100I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID154790 | Antiviral activity against subtype isolate G strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID157561 | Tested for the drug concentration required to decrease HIV-1D4 infected human peripheral blood mononuclear cell viability compared to uninfected controls | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID284448 | Antiviral activity against HIV1 LA1 in human PBM cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Enantioselective synthesis and antiviral activity of purine and pyrimidine cyclopentenyl C-nucleosides. |
| AID200172 | Compound is evaluated in vitro for the inhibition single mutant of HIV-1 RTS (K103 N) | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
| 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| AID46587 | Inhibitory concentration (cytotoxic activity) which results in a 50% survival of HIV-1-infected CEM cells relative to uninfected untreated control cells | 1994 | Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
| Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT). |
| AID718817 | Cytotoxicity against human C8166 cells after 3 days by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity. |
| AID646711 | Antiviral activity against HIV1 LAV1 infected in PHA-stimulated human PBMC assessed as reduction in RT activity after 6 days by micromethod-based beta scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl-7-deazapurine nucleosides, their phosphoramidate prodrugs and 5'-triphosphates. |
| AID493723 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of viral replication | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis of highly functionalized 2,4-diaminoquinazolines as anticancer and anti-HIV agents. |
| AID1377175 | Antiviral activity against NNRTI-resistant HIV1 isolate N119 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID13511 | AUC in brain | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine. |
| AID1289719 | Inhibition of human TERT-regulated Wnt/beta-catenin signalling in human MGC803 cells assessed as decrease in beta-catenin mRNA expression at 3 mmol/L after 48 hrs by RT-PCR method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID1221977 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1357785 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID693593 | Antiviral activity against HIV1 A17 harbouring RT K103N/Y181C mutant infected in human C8166 cells assessed as protection against virus-induced cytopathic effect after 3 days by syncytium reduction assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors. |
| AID600422 | Antiviral activity against HIV1 NL4-3 infected human C8166-CCR5 cells assessed as decrease in virus-induced cytopathicity after 72 hrs by cell associated dehydrogenase activity assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
| Novel 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2)-curcumin, kojic acid, quercetin, and baicalein conjugates as HIV agents. |
| AID1152127 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of p24 antigen production by measuring time delay in loss of compound activity at 50 to 100 times EC50 by ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors. |
| AID47640 | Concentration of the drug resulting in 50% reduction of the viral cytopathic effect against HIV-1 replication in CEM cells. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID21045 | Evaluated for Partition coefficient in n-octanol and phosphate buffer pH 7.4 | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Synthesis and biological evaluation of prodrugs of zidovudine. |
| AID105123 | Dose required to achieve 50% protection of MT-4 cells from the HIV-1 induced cytopathogenicity in mock-infected MT-4 cells | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID285189 | Inhibition of [3H]thymidine phosphorylation in isolated perfused Sprague-Dawley rat heart after 30 mins | 2007 | Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
| Zidovudine inhibits thymidine phosphorylation in the isolated perfused rat heart. |
| AID104766 | Compound was tested for reduction of the viability of mock infected MT-4 cell in test-I | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
| Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes. |
| AID267856 | Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
| AID680951 | TP_TRANSPORTER: inhibition of PGF2alpha uptake (PGF2alpha: 0.005 uM, AZT: 1000 uM) in OAT2-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID458192 | Activity at Drosophila melanogaster dNK by spectrophotometry | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
| Synthesis of fluorescent nucleoside analogs as probes for 2'-deoxyribonucleoside kinases. |
| AID106599 | Cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
| A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID198232 | Inhibitory activity of compound against purified recombinant HIV-1 reverse transcriptase; Not determined | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
| Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. |
| AID32214 | Concentration required to inhibit the cytopathic effect of HIV-2 on ATH8 cells; ND=Not determined | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5
| Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides. |
| AID247880 | Concentration required to inhibit 50% growth of uninfected H9 cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| Anti-AIDS agents. Part 62: anti-HIV activity of 2'-substituted 4-methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs. |
| AID82562 | The 50% inhibitory concentration expresses cellular toxicity measured against normal human granulocyte-monocyte cells | 1989 | Journal 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. |
| AID235800 | Selectivity index which is the ratio of IC50 to EC50 of R-MuLV. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Unsaturated and carbocyclic nucleoside analogues: synthesis, antitumor, and antiviral activity. |
| AID78783 | Toxic concentration on HIV-1 mock infected H9 lymphocyte cells | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
| AID409954 | Inhibition of mouse brain MAOA | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID611663 | Antiviral activity against HIV-2 ROD infected in human C8166 cells assessed as protection against viral cytopathogenicity after 3 days by measuring syncytia under inverted microscope | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID222394 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 1 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID417050 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine triphosphate level at 600 mg administered in two courses, first QD for 7 days followed by BID for 7 to 14 days and second course the subjects were switched to the other regimen measured per | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID229420 | Selectivity ratio CD50 to ED50 | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
| Synthesis and anti-HIV activity of various 2'- and 3'-substituted 2',3'-dideoxyadenosines: a structure-activity analysis. |
| AID398465 | Inhibition of HIV1 reverse transcriptase p66/p51 | 1995 | Journal of natural products, Jul, Volume: 58, Issue:7
| Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase. |
| AID1377170 | Antiviral activity against HIV1 isolate SF162 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID1238518 | Inhibition of HIV-1 reverse transcriptase in human Jurkat cells assessed as ratio MTT activity to reverse transcriptase activity with compound/reverse transcriptase activity with DMSO at 1 uM after 72 hrs (Rvb = 0.356 No_unit) | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
| Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase. |
| AID279934 | Decrease in fatty acid synthase activity in Wistar cafteria-fed rat inguinal adipose tissue at 70 mg/kg/day by DNA quantification assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID610677 | Therapeutic index, ratio of CC50 for C8166 cells to EC50 for Human immunodeficiency virus 1 | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Tigliane-type diterpenoid glycosides from Euphorbia fischeriana. |
| AID246139 | Effective concentration against HIV IIIB replication in H9 lymphocytes | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Anti-AIDS agents. 60. Substituted 3'R,4'R-di-O-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) analogues as potent anti-HIV agents. |
| AID83215 | Compounds were evaluated for anti-RT activity by MTT dose and % cell / viability was reported at 9 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID342011 | Ratio of kcat to Km for Staphylococcus aureus CCM 885 recombinant thymidine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID360656 | Cytotoxicity against uninfected human C8166 cells by XTT-formazan method | 2001 | Journal of natural products, May, Volume: 64, Issue:5
| Naphthopyranone glycosides from Paepalanthus microphyllus. |
| AID614143 | Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
| AID1077221 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID779529 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
| AID154969 | Antiviral activity was evaluated in mitogen-stimulated human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| 1,3-dioxolanylpurine nucleosides (2R,4R) and (2R,4S) with selective anti-HIV-1 activity in human lymphocytes. |
| AID1884224 | Antiviral activity against HIV-1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID1265602 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 NL4-3 infected in MT4 cells | 2015 | Journal of natural products, Nov-25, Volume: 78, Issue:11
| Stelleralides D-J and Anti-HIV Daphnane Diterpenes from Stellera chamaejasme. |
| AID1483276 | Inhibition of HIV1 3B reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID456307 | Cytotoxicity against human CEM-SS cells by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands. |
| AID81099 | In vitro antiviral activity against HIV-1 IIIB in C8166 (human CD4) cells. | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
| 6-Aminoquinolones as new potential anti-HIV agents. |
| AID373867 | Hepatic clearance in human hepatocytes in absence of fetal calf serum | 2009 | European journal of medicinal chemistry, Apr, Volume: 44, Issue:4
| First-principle, structure-based prediction of hepatic metabolic clearance values in human. |
| AID198384 | Inhibitory concentration against human immunodeficiency virus type 1 (HIV-1 strain IIIB RT) reverse transcriptase was determined by triplicate assay at low (~0.1 pfu/cell) multiplicity of injection (moi) | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| (Z)- and (E)-2-((hydroxymethyl)cyclopropylidene)methyladenine and -guanine. New nucleoside analogues with a broad-spectrum antiviral activity. |
| AID222398 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 4 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID576195 | Antiviral activity against Human immunodeficiency virus 1 H10 harboring Tyr127His, Gly140Glu, Glu149Lys, Asp174Asn and Arg178Lys mutations in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporat | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID717260 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | | | |
| AID646709 | Cytotoxicity against human PBMC after 6 days by trypan blue exclusion method | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl-7-deazapurine nucleosides, their phosphoramidate prodrugs and 5'-triphosphates. |
| AID1653801 | Substrate activity at human mARC1 expressed in Escherichia coli assessed as turnover rates at 3 mM pre-incubated for 3 mins followed by NADH addition and measured after 15 mins by LC-MS analysis based assay | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| Drug Metabolism by the Mitochondrial Amidoxime Reducing Component (mARC): Rapid Assay and Identification of New Substrates. |
| AID235873 | Ratio of CD50 to ED50 based on MTT assay | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1383888 | Antiviral activity against HIV1 3B infected in human MT4 cells | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Polypharmacology in HIV inhibition: can a drug with simultaneous action against two relevant targets be an alternative to combination therapy? |
| AID1504697 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID106592 | Concentration to required to reduce viability of Mock infected MT-4 cells | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID309234 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 3B | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
| Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. |
| AID612669 | Antiviral activity against wild type HIV1 A17 harboring reverse transcriptase K103N and Y181C mutant infected in human C8166 cells assessed as inhibition of viral-induced cytopathogenicity after 3 days by syncytium formation assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
| Synthesis and biological evaluation of (±)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1377178 | Antiviral activity against HIV1/VSV-G pseudovirus infected in human A549 cells assessed as downregulation of R/U5 gene expression after 48 hrs by Taqman-based real-time PCR analysis | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID152642 | Cytotoxic effect in uninfected human peripheral blood mononuclear (PBM) cells | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
| Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells. |
| AID665548 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID574195 | Cytotoxicity against human skeletal muscle Myoblast assessed as change in Tfam mitochondrial RNA level on day 2 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID1238542 | Binding affinity to human serum albumin with excitation at 280 nm after 2 hrs by spectrofluorimetric analysis | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
| Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase. |
| AID47301 | Concentration required to kill 50% of CEM cells | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID157554 | Anti-HIV activity in Human peripheral blood mononuclear (PBM) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID198229 | Inhibition of recombinant reverse transcriptase (RT) in cell-free Quan-T-RT assay system | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
| N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. |
| AID46045 | Inhibitory activity against the cytopathic effect of HIV-1 RFstrain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID83267 | Effective concentration required for antiviral activity against HIV strain A17 (pyridinone-resistant strain) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID458874 | Antiviral activity against HIV1 LAI in human CEM-SS cells assessed as RT activity after 5 days by single passage assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| 5-Modified-2'-dU and 2'-dC as mutagenic anti HIV-1 proliferation agents: synthesis and activity. |
| AID698301 | Antiviral activity against HIV1 containing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1141970 | Ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID46848 | Concentration required to reduce 50% of the number of CEM/TK cells in the HIV-2 infected cell cultures. | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17
| Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3'-azido-3'-deoxythymidine. |
| AID3046 | Compound was evaluated for the inhibition of cell replication sheep choroid plexus (SCP) cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Novel acyclonucleotides: synthesis and antiviral activity of alkenylphosphonic acid derivatives of purines and a pyrimidine. |
| AID523350 | Antiviral activity against HIV1 with RT connection domain K103N/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID583848 | Antiviral activity against HIV1 NL4-3 infected in human SupT1 cells derived from 11 viral passages assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID583459 | Cytotoxicity against human HepG2 cells assessed as inhibition of mitochondrial respiratory chain complex IV activity at 50 uM after 15 days relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID1575287 | Cytotoxicity against human C8166 cells after 72 hrs by MTT assay | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1
| 3,4- seco-Norclerodane Diterpenoids from the Roots of Polyalthia laui. |
| AID556524 | Antiviral activity against Human immunodeficiency virus 1 clone pNL4-3-Q145M harboring K102Q, Q145M, S162C, K277R, I293V mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
| AID156335 | The compound was tested in vitro for anticancer activity against PC-3 cells; Not determined | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID253314 | Therapeutic index was determined | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Anti-AIDS agents. 60. Substituted 3'R,4'R-di-O-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) analogues as potent anti-HIV agents. |
| AID363858 | Ratio of CC50 for human Caco-2 cells to IC50 for rotavirus RF assessed by inhibition of infectivity following virus attachment | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
| Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities. |
| AID232753 | Selectivity index is the ratio of EC50 and CC50 in MT-4 cells | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
| New bicyclam-AZT conjugates: design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor. |
| AID1594865 | Inhibition of HIV1 3B reverse transcriptase infected in human PBMC cells after 4 days | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic. |
| AID83426 | Effective concentration required for antiviral activity against HIV strain VIHU (nonsyncytia inducing) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID698303 | Cytotoxicity against mock-infected human MT4 cells measured after 5 days by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1320864 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
| AID235486 | Selectivity index is the ratio of ED50 and CD50 values against inhibition of HIV-1 in MT-4 cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. |
| AID1815392 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID525113 | Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4
| Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID83393 | Antiviral activity against Human immunodeficiency virus type-1 | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| Nucleosides and nucleotides. 185. Synthesis and biological activities of 4'alpha-C-branched-chain sugar pyrimidine nucleosides. |
| AID519859 | Antiviral activity against HIV1 subtype B-RF infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1331268 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of viral-induced cytopathic effect by measuring syncytia formation after 72 hrs by inverted microscopic method | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
| Design, synthesis and anti-HIV-1 RT evaluation of 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives. |
| AID1815383 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID619632 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID1456306 | Inhibition of HIV-1 3B wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
| AID693590 | Cytotoxicity against human C8166 cells assessed as decrease in cell viability by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors. |
| AID46199 | Inhibitory effect against HIV-2 replication in CEM cells. | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
| Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase. |
| AID81246 | Compound was evaluated for the antiviral activity against compound resistant virus isolate Y188H with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID105764 | Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 125 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID512142 | Antiviral activity against HIV1 infected in human CEM cells assessed as protection against virus-induced cytopathic effect after 6 days by XTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents. |
| AID395818 | Cytotoxicity against human Bel7402 cells after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
| Simple and efficient synthesis of novel glycosyl thiourea derivatives as potential antitumor agents. |
| AID1743618 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID1815387 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID618866 | Cytotoxicity against human HepAD38 cells | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides. |
| AID548535 | Antiviral activity against HIV1 subtype G isolate RU132 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID235484 | Selectivity index is the ratio of CC50 to IC50 | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. |
| AID232765 | Selectivity index of HIV-1 and HIV-2 with respect to MT-4 cells | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID284320 | Growth inhibition of human Caco-2 cells after 72 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-2-keto-beta-D-glucopyranosyl derivatives of N4-benzoyl cytosine. |
| AID333022 | Cytotoxicity against human H9 cells after 3 days | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2
| Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. |
| AID1191974 | Selectivity index, ratio of CC50 for mock-infected human HeLa cells to EC50 for HIV2 ROD infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
| AID611664 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for HIV2 ROD infected in human C8166 cells | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID81245 | Compound was evaluated for the antiviral activity against compound resistant virus isolate Y181C/K103N with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID153136 | Effective concentration of required to inhibit the replication of HIV-1 BY 50% in PMBCs from donor 1 | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID308283 | Antiviral activity against HIV replication in H9 cells | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Anti-AIDS agents 72. Bioisosteres (7-carbon-DCKs) of the potent anti-HIV lead DCK. |
| AID563941 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S/M184V mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID648420 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID523346 | Antiviral activity against HIV1 with RT connection domain T369V mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID1064552 | Cytotoxicity against human CEM-TART cells assessed as cell viability after 72 hrs by MTT assay | 2014 | Journal of natural products, Jan-24, Volume: 77, Issue:1
| 4-Quinolone alkaloids from Melochia odorata. |
| AID1705185 | Selectivity ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID377703 | Antibacterial activity against methicillin-resistant Staphylococcus aureus | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7
| Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID426890 | Cytotoxicity against human PBMC by XTT assay | 2009 | Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
| Synthesis, antiviral activity and molecular modeling of oxoquinoline derivatives. |
| AID405333 | Toxicity in human HepG2/C3A cells assessed as induction of cell death at 50 uM after 4 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID154767 | Concentration required to reduce viability of Mock infected PBL (peripheral blood lymphocytes) cells. | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID26304 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
| QSAR model for drug human oral bioavailability. |
| AID389379 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID422693 | Antiviral activity against HIV1 with reverse transcriptase K70E M184V and K70G M184V mutation by antivirogram biological cutoffs assay relative to wild type HIV1 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
| Novel drug resistance pattern associated with the mutations K70G and M184V in human immunodeficiency virus type 1 reverse transcriptase. |
| AID1200846 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
| AID1357805 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID200148 | Ability to inhibit the HIV-1 reverse transcriptase in cord blood mononuclear cells. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID246175 | Effective concentration against HIV-induced cytopathogenicity in MT-4 cells | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
| Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. |
| AID154770 | Antiviral activity against Ba-L monocyte tropic isolate strain in monocyte | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID1752326 | Antiviral activity against HIV-1 NL4-3 infected in human MT4 cells assessed as reduction in p24 production treated at 48 hrs post-infection and measured on day 4 post-viral infection by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | New phorbol ester derivatives as potent anti-HIV agents. |
| AID378447 | Antiviral activity against HIV1 infected human H9 lymphocytes assessed as suppression of viral replication | 2006 | Journal of natural products, Sep, Volume: 69, Issue:9
| Tripfordines A-C, sesquiterpene pyridine alkaloids from Tripterygium wilfordii, and structure anti-HIV activity relationships of Tripterygium alkaloids. |
| AID46381 | Antiviral activity against site directed resistant isolate HIV-1 V179D in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6
| Structure-based identification of OATP1B1/3 inhibitors. |
| AID1226478 | Antiviral activity against West Nile virus infected in BHK-WII RepRen1B cells assessed as inhibition of viral replication at 10 uM after 3 days by luciferase reporter gene assay relative to control | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| 5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus. |
| AID22061 | Concentration in mouse blood 90 min post injection at a dose 240 mocromol/kg | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID1204142 | Cytotoxicity against human MCF7 cells after 48 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| PMA-SiO2 catalyzed synthesis of indolo[2,3-c]quinolines as potent anti cancer agents. |
| AID1635808 | Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 8070-1 expressing integrase G140S/Y143H/Q148H mutant to EC50 for HIV1 expressing wild-type integrase | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H. |
| AID232296 | Differential selectivity measured as the ratio of CEM-SS cell growth IC50 vs HIV plaque formation IC50. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| In vitro evaluation of phosphocholine and quaternary ammonium containing lipids as novel anti-HIV agents. |
| AID282658 | Inhibition of HIV1 LAI replication in MT2 by CPE assay | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
| (Z)- and (E)-[2-Fluoro-2-(hydroxymethyl)cyclopropylidene]methylpurines and -pyrimidines, a new class of methylenecyclopropane analogues of nucleosides: synthesis and antiviral activity. |
| AID342009 | Activity of Staphylococcus aureus CCM 885 recombinant thymidine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID597658 | Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT method. |
| AID15239 | Percentage of total protein recovered in P1 subregion in mouse brain that contains nuclei and cell debris, after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID142441 | Cytotoxicity was evaluated | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Unsaturated and carbocyclic nucleoside analogues: synthesis, antitumor, and antiviral activity. |
| AID563938 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID1228738 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2-ROD | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5
| Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID82919 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 15 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID568183 | Antiviral activity against multidrug-resistant R5 tropic HIV1 MM infected in human PBMC assessed as inhibition of HIN p24 antigen expression | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate. |
| AID267858 | Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
| AID233701 | Selectivity ratio to IC50 of MT4 cells and EC50, anti-HIV activity of MT-4 cells | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC). |
| AID47657 | Effective concentration that reduces HIV-induced cytopathic effect by 50% was determined by MTT assay. | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
| Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs. |
| AID104274 | Effective concentration required for 50% protection of MT-4 cells against the cytopathic effect of HIV-1 | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1705188 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID83401 | Tested for the determination of percentage toxicity at 100 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID155288 | Compound was evaluated for cytotoxic activity against peripheral blood mononuclear cells using microculture tetrazolium assay | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
| 5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series. |
| AID1565090 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID1743631 | Antiviral activity against HIV1 harboring RT F227L/V106Amutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID1410482 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
| AID393072 | Antiviral activity against HIV1 3a with reverse transcriptase K65R mutation in human MT2 cells assessed as inhibition of viral-induced cytopathic effect by XTT assay relative to wild type | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors. |
| AID45542 | Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| New bicyclam-GalCer analogue conjugates: synthesis and in vitro anti-HIV activity. |
| AID79295 | Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound able to suppress HIV replication by 50%. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID105521 | Anti-HIV activity was determined as dose required to protect 50% of the HIV-infected MT-4 cells against destruction | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
| Synthesis and anti-HIV activity of various 2'- and 3'-substituted 2',3'-dideoxyadenosines: a structure-activity analysis. |
| AID1743635 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID548588 | Antiviral activity against HIV1 isolate 180 harboring reverse transcriptase K65R mutant gene obtained as site-directed mutant of NL4-3 by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1884491 | Antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID481805 | Ratio of Vmax to Km for Ureaplasma parvum thymidine kinase relative to dThd | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID46049 | Inhibitory activity against the cytopathic effect of HIV-2 ROD strain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID1705184 | Cytotoxicity against human MT-4 cells assessed as reduction in cell viability by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID405339 | Toxicity against human HepG2/C3A cells assessed as elevation of lactate levels at 10 uM after 6 days by NAD+ reduction assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID717261 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID575958 | Antiviral activity against Human immunodeficiency virus 1 subtype D UG/92/046 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1565093 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | | | |
| AID1292012 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID319042 | Antiviral activity against HIV1 in C8166 cells after 72 hrs | 2008 | Journal of natural products, Jan, Volume: 71, Issue:1
| Octanorcucurbitane and cucurbitane triterpenoids from the tubers of Hemsleya endecaphylla with HIV-1 inhibitory activity. |
| AID1352317 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID246296 | Concentration required to inhibit 50% of HIV-1 (human immunodeficiency virus-1) replication | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents. |
| AID46996 | Antiviral activity was measured on HIV-2 in mutant thymidine kinase-deficient CEM/TK- cells | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| cycloSal-2',3'-dideoxy-2',3'-didehydrothymidine monophosphate (cycloSal-d4TMP): synthesis and antiviral evaluation of a new d4TMP delivery system. |
| AID398466 | Inhibition of DNA polymerase beta | 1995 | Journal of natural products, Jul, Volume: 58, Issue:7
| Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase. |
| AID540217 | Volume of distribution at steady state in dog after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID571605 | Ratio of AUC (0 to 12 hrs) in HIV-1 infected patient at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir to AUC (0 to 12 hrs) in HIV-1 infected patient at 300 mg, po bid on day 1 coadministered with 500 mg, po bid amdoxovir | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID581778 | Inhibition of human recombinant cyclophilin-associted cis-trans propyl isomerase activity | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
| AID155292 | Compound was evaluated for its cytotoxicity against peripheral blood mononuclear (PBM) cells. | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine. |
| AID557275 | Antiviral activity against HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1156485 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
| AID81100 | Antiviral activity against HIV-1 (human immunodeficiency virus type 1) | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
| Nucleosides and nucleotides. 183. Synthesis of 4'alpha-branched thymidines as a new type of antiviral agent. |
| AID377702 | Antibacterial activity against Staphylococcus aureus | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7
| Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID373360 | Drug metabolism in human CEM cells assessed as radioactive zidovudine monophosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID573982 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Simian immunodeficiency virus MAC 251 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID1304540 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2016 | Journal of natural products, Mar-25, Volume: 79, Issue:3
| Carolignans from the Aerial Parts of Euphorbia sikkimensis and Their Anti-HIV Activity. |
| AID1357798 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID1231848 | Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6
| Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID142320 | Reduced GM-CSF dependent colony formation in murine bone marrow progenitor cells at 0.5 uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID341358 | Drug uptake in human CD4+CEM cells assessed as 3'-azido-2',3'-dideoxythymidine monophosphate half life at 200 nM | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID548542 | Antiviral activity against HIV2 isolate CDC310342 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1743627 | Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID222681 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 8 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID548582 | Antiviral activity against HIV1 isolate 153 harboring reverse transcriptase L74V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID46988 | Cytotoxic concentration which is required to reduce CEM/TK- cell viability by 50%. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID83225 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID235739 | Therapeutic index determined by ratio of IC50 to EC50 | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
| Anti-AIDS agents 54. A potent anti-HIV chalcone and flavonoids from genus Desmos. |
| AID157556 | Cytotoxic concentration for inhibition of HIV-1 replication in human peripheral Blood mononuclear cells.(PBMCs) | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
| Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils. |
| AID519865 | Antiviral activity against HIV1 subtype B-NL4-3 infected in 3 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1316344 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID1763898 | Antiviral activity against HIV-1 IIIB harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID157418 | In vitro Cytotoxic concentration which reduced HIV-1 LAV infected peripheral blood lymphocytes by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID361401 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2002 | Journal of natural products, Nov, Volume: 65, Issue:11
| New saponins from the starfish Certonardoa semiregularis. |
| AID246263 | Concentration required to inhibit 50% of HIV (human immunodeficiency virus) replication | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| Anti-AIDS agents. Part 62: anti-HIV activity of 2'-substituted 4-methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs. |
| AID47009 | Concentration required to protect CEM/TK cells against the cytopathicity of HIV-2 by 50% | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID46837 | Cytotoxic concentration required to reduce the viability of HIV-1 by 50% in CEM/TK cells | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID198570 | antiviral activity in Human immunodeficiency virus-1 as reverse transcriptase activity in culture supernatant | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiproliferative and antiviral activity of 2'-deoxy-2'-fluoroarabinofuranosyl analogs of the nucleoside antibiotics toyocamycin and sangivamycin. |
| AID78958 | Compound was tested for the cytotoxicity in H-9 cells infected with HIV-IIIB over 7 days | 1996 | Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
| Synthesis and HIV inhibition activity of 2',3'-dideoxy-3'-C-hydroxymethyl nucleosides. |
| AID1888690 | Antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID235243 | Therapeutic index value was evaluated as the ratio of IC50/EC50 | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
| Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs. |
| AID1720645 | Selectivity index, ratio of CC50 for cytotoxicity in human TZM-bl assessed as reduction in cell viability incubated for 5 days by MTT to EC50 for inhibition of reverse transcriptase/nucleocapsid protein 7 in wild type HIV1 NL4-3 infected in human TZM-bl c | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID235801 | Selectivity index (CC50/EC50). | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID363848 | Ratio of CC50 for human Caco-2 cells to IC50 for rotavirus RF assessed by neutralization of virus before its attachment | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
| Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities. |
| AID235695 | Selectivity index is defined as CC25(A3.01 cells) / CC50(A3.01 cells) | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID45553 | Effective concentration required for antiviral activity against T cell line of CEM-SS cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID222688 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 24 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID154974 | Concentration required for antiviral activity in PBMC (human peripheral blood mononuclear cells) infected with HIV-1 strain LAV | 1993 | Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
| Structure-activity relationships of beta-D-(2S,5R)- and alpha-D-(2S,5S)-1,3-oxathiolanyl nucleosides as potential anti-HIV agents. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | | | |
| AID157581 | Effective concentration for inhibition of HIV-1 replication in human peripheral Blood mononuclear cells.(PBMCs) | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
| Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils. |
| AID99185 | Inhibitory effect of compound on the proliferation of murine leukemia cells L1210/TK- | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID46033 | Effective concentration in vitro against HIV-1-infected CEM cells relative to uninfected untreated controls | 1994 | Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
| Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT). |
| AID571603 | Apparent oral clearance in HIV-1 infected patient at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1316345 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID373364 | Drug metabolism in human CEM cells assessed as radioactive 2', 3'-didehydro-3'-deoxy-4'-ethynylthymidine diphosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID563939 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase M184V mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID45822 | The compound was evaluated for percent reduction of H2O2-induced H2DCFDA fluorescence in human CEM T-cells;No data | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
| Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity. |
| AID106767 | Cytotoxic dose required to reduce the proliferation of normal uninfected MT-4 cells by 50% | 1998 | Journal of medicinal chemistry, Jan-15, Volume: 41, Issue:2
| Synthesis and anti-HIV-1 activity of novel 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones. |
| AID548547 | Antiviral activity against HIV1 subtype B isolate ADA infected in human MDM after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID273054 | Inhibition of HIV1 LAI replication in MT2 cells by cytopathic effect assay | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| 9-{[3-fluoro-2-(hydroxymethyl)cyclopropylidene]methyl}adenines and -guanines. Synthesis and antiviral activity of all stereoisomers1. |
| AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID548311 | Antiviral activity against HIV1 subtype C isolate 92BR025 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID373366 | Drug metabolism in human CEM cells assessed as radioactive stavudine monophosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID288632 | Cytotoxicity against C8166 cells after 72 hrs by MTT method | 2007 | Journal of natural products, Jun, Volume: 70, Issue:6
| Triterpenoids from Schisandra rubriflora. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | | | |
| AID9851 | Effect against HIV-1 chronically infected promonocytic cell line ACH-2 cells | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
| Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. |
| AID1528486 | Inhibition of HIV1 3B reverse transcriptase infected in human MT4 cells assessed as reduction in p24 production at 12 uM incubated for 1 hr prior to viral infection followed by compound washout and measured up to 3 hrs by ELISA | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1
| Scaffold Simplification Strategy Leads to a Novel Generation of Dual Human Immunodeficiency Virus and Enterovirus-A71 Entry Inhibitors. |
| AID365484 | Antiviral activity against HIV1 3B in MT4 cells assessed as virus p24 antigen production administered at 16 hrs post infection by ELISA | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Structure-activity relationship study on anti-HIV 6-desfluoroquinolones. |
| AID83228 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID342551 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID1763901 | Antiviral activity against HIV-1 IIIB harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID542943 | Induction of adipocyte differentiation in mouse 3T3-F442A cells assessed as PPARgamma mRNA expression on day 6 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1610033 | Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID222691 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 4 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID658565 | Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
| AID1322997 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
| AID751135 | Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect after 3 days by Syncytia Assay | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6
| Bioactive dibenzocyclooctadiene lignans from the stems of Schisandra neglecta. |
| AID373387 | Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.18 uM after 24 hrs by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID222495 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 4 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID300150 | Antiviral activity against Rotavirus RF infected in rhesus monkey MA104 cells assessed as neutralization of virus in solution before its attachment after 72 hrs | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID235458 | Selectivity index (SI) is determined as the ratio of CC50/EC50 | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety. |
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
| Predicting phospholipidosis using machine learning. |
| AID357032 | Cytotoxicity against human H9 cells | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7
| Anti-AIDS agents. 46. Anti-HIV activity of harman, an anti-HIV principle from Symplocos setchuensis, and its derivatives. |
| AID1687680 | Antiviral activity against wild type HIV-1 strain 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID233700 | Selectivity ratio to IC50 of HL60 cells and EC50, anti-HIV activity of MT-4 cells | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC). |
| AID83212 | Compounds were evaluated for anti-RT activity at 9 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID46385 | Antiviral activity against site directed wild-type enzyme isolate HIV-1 NL4-3WT in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID104309 | Cytopathogenicity against HIV-2 induced replication in MT-4 cells was determined | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Synthesis, antiretrovirus effects, and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine. |
| AID222680 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 4 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID46613 | Inhibitory activity against HIV-1 IIIB in CEM-SS infected cells relative to AZT | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6
| A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | | | |
| AID493818 | Antiviral activity against HIV1 NL4.3 infected in human CEM-GFP cells assessed as inhibition p24 antigen production after 8 days by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus. |
| AID523351 | Antiviral activity against HIV1 with RT connection domain K103N/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID610675 | Antiviral activity against Human immunodeficiency virus 1 infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Tigliane-type diterpenoid glycosides from Euphorbia fischeriana. |
| AID559937 | Antiviral activity against HIV1 89.6 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID1446812 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID401234 | Antiviral activity against HIV1 | 2004 | Journal of natural products, Apr, Volume: 67, Issue:4
| Isolation of salicin derivatives from Homalium cochinchinensis and their antiviral activities. |
| AID584801 | Inhibition of electron transport protein complex 4 in human subcutaneous preadipocytes at 6 uM after 30 to 60 days by photometric analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1763897 | Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID287282 | Antiviral activity against HIV1 LAI replication in human PBMC after 5 days | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors. |
| AID106423 | Content of viable cells at 10e-4 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID373352 | Drug metabolism in human CEM cells assessed as radioactive zidovudine diphosphate accumulation at 2 uM after 2 hrs assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID523348 | Antiviral activity against HIV1 with RT connection domain T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID144633 | The compound was evaluated for percent reduction of H2O2-induced H2DCFDA fluorescence in NALM-6-B-cells;No data | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
| Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity. |
| AID47634 | Inhibitory effect against synthesis of p24 gag protein in CEM cells. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and anti-HIV activity of carbocyclic 2',3'-didehydro-2',3'-dideoxy 2,6-disubstituted purine nucleosides. |
| AID1406277 | Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells measured on day 3 post infection by Nano-Glo luciferase reporter gene assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Identification, structural modification, and dichotomous effects on human immunodeficiency virus type 1 (HIV-1) replication of ingenane esters from Euphorbia kansui. |
| AID82287 | Tested in vitro against HIV-1 MDR using MAGI assay | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity. |
| AID214422 | Inhibitory concentration against HIV-1 infected U937 cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID569566 | Antiviral activity against HIV1-3B infected in human C1866 cells assessed as inhibition of virus-induced cytopathic effect | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
| Compounds from Kadsura angustifolia with anti-HIV activity. |
| AID491832 | Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 6 days by p24 antigen based assay | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID104242 | In vitro Cytotoxic concentration which reduced HIV-1 LAV infected MT-2 cells by 25 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID154948 | Cytotoxic concentration of compound determined by the tyran blue exclusion staining method in PBMC by test II; Not tested | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. |
| AID232758 | Selectivity index measured as the ratio of CC50/IC50 values. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
| Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin- 2(1H)-one (TIBO) derivatives. |
| AID46561 | Cytotoxic concentration against CEM cells was determined on day 6 | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID525108 | Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID573979 | Antiretroviral activity against Simian immunodeficiency virus MAC 251 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID16367 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into cortex | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID152935 | Cytotoxic effect in human peripheral blood monocyte cells(PBMC) | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| HIV-1 neutralization and tumor cell proliferation inhibition in vitro by simplified analogues of pyrido[4,3,2-mn]thiazolo[5,4-b]acridine marine alkaloids. |
| AID154955 | Activity against Lamivudine-resistant virus (HIV-1XXBRU) in human PBM cells, expressed as EC50 | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance. |
| AID341371 | Ratio of EC50 for X4-HIV1MDR/C in human PHA-PBMC to EC50 for X4-HIV1NL4-3 in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID247769 | Inhibitory concentration against CEM cell line | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Synthesis, antiviral activity, and mechanism of drug resistance of D- and L-2',3'-didehydro-2',3'-dideoxy-2'-fluorocarbocyclic nucleosides. |
| AID104600 | The concentration required to cause a 50% inhibition of HIV reproduction was determined in MT-4 cell culture for free forms | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Carbocyclic dinucleoside polyphosphonates: interaction with HIV reverse transcriptase and antiviral activity. |
| AID1316338 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID538998 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
| Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds. |
| AID105578 | Concentration required to affect a 50% reduction in the cytopathic effect of HIV for MT-4 cells | 1992 | Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
| 3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine. |
| AID1238316 | Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 10 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID1572527 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID157559 | Cytotoxic concentration required to inhibit 50% of HIV-1 in peripheral blood mononuclear cells (PBMC) | 1997 | Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21
| Probing the mechanism of action and decomposition of amino acid phosphomonoester amidates of antiviral nucleoside prodrugs. |
| AID278018 | Selectivity index, CC50 against C8166 cell/ EC50 against HIV1 | 2007 | Journal of natural products, Feb, Volume: 70, Issue:2
| Tetranorclerodanes and clerodane-type diterpene glycosides from Dicranopteris dichotoma. |
| AID105399 | AntiHIV-1 activity measured in MT-4 cells at 5 to 6 different concentrations, using the P24 antigen enzyme-linked immunosorbent assay (ELISA). | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC). |
| AID473139 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication treated 1 day after infection measured on after 4 days postinfection by p24 antigen ELISA | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. |
| AID681232 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, AZT: 1000 uM) in OAT3-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID1572526 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID1368347 | Cytotoxicity against human TZM-bl cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
| Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41. |
| AID46656 | Concentration required to protect CEM/0 cells against the cytopathicity of HIV-1 by 50%. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID78947 | Inhibitory concentration required to inhibit uninfected growth of H9 lymphocytes by 50% | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Antitumor agents. 166. Synthesis and biological evaluation of 5,6,7,8-substituted-2-phenylthiochromen-4-ones. |
| AID104260 | In vitro Cytotoxic concentration which reduced G 910-6p2 (post-AZT) infected MT-2 cells by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID578849 | Cytotoxicity against human PBMC after 5 days by trypan blue assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors. |
| AID635346 | Cytotoxicity against human MT4 cells measured by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
| AID1761015 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID104297 | The compound was tested for effective concentration required to protect MT-4 cells against the cytopathicity of HIV-1(IIIB) | 2002 | Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
| New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation. |
| AID559942 | Antiviral activity against HIV1 A018G infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID1220783 | Drug metabolism in human assessed as glucuronide concentration in bile and urine | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID253092 | Mean phosphorylation rate of 100 uM compound by recombinant human thymidine kinase 2 (mitochondrial) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| Synthesis and biological evaluation of neutral and zwitterionic 3-carboranyl thymidine analogues for boron neutron capture therapy. |
| AID611572 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human C8166 cells assessed as numbers of syncytia after 3 days by MTT assay | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Sesquiterpene and norsesquiterpene derivatives from Sanicula lamelligera and their biological evaluation. |
| AID1565098 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID619637 | Antiviral activity against HIV-1 3B harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID222500 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 2 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID572777 | Antiviral activity against HIV1 harboring reverse transcriptase Q151M mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1141972 | Ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID141778 | Concentration inhibiting moloney murine leukemia retrovirus | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| Anti-HIV-I activity of linked lexitropsins. |
| AID647166 | Cytotoxicity in human TZM-bl cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Synthesis and antiviral activities of novel gossypol derivatives. |
| AID214084 | Effect against HIV-1 chronically infected promonocytic cell line U1 | 1995 | Journal of medicinal chemistry, Aug-04, Volume: 38, Issue:16
| Anti-AIDS (acquired immune deficiency syndrome) agents. 17. New brominated hexahydroxybiphenyl derivatives as potent anti-HIV agents. |
| AID630377 | Apparent permeability from apical to basolateral side of the human Caco2 cells at 100 uM after 30 mins by HPLC method | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Synthesis and anticancer activity of 5'-chloromethylphosphonates of 3'-azido-3'-deoxythymidine (AZT). |
| AID45198 | Compound was evaluated for the effect of Order of Addition on Cytoprotection against HIV-1RF at dilution 333, Add at infection | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID42399 | Inhibition of syncytia formation in infected C8166-cells | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. |
| AID79119 | Compound was evaluated for anti-HIV activity and the concentration that inhibits uninfected H9 cell growth by 50% | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| Anti-AIDS agents. 33. Synthesis and anti-HIV activity of mono-methyl substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues. |
| AID682180 | TP_TRANSPORTER: inhibition of benzylpenicillin uptake by 3'-Azido-3'-deoxythymidine at a concentration of 1000uM in Oat3-expressing oocyte cells | 2004 | The Journal of pharmacology and experimental therapeutics, Jun, Volume: 309, Issue:3
| Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. |
| AID79305 | Antiviral activity against HIV-1 in H9 lymphocytes. | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
| Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents. |
| AID157403 | Compound was evaluated for the inhibition of HIV-1 induced CPE (HTLV-III B strain ) replication in peripheral blood lymphocytes (PBL). | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID548566 | Selectivity ratio of EC50 for HIV1 7303-3 harboring reverse transcriptase 41L/44D/67N/69D/118I/210W/215Y mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID553578 | Antiviral activity against HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID16518 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into pons and medulla | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID575960 | Antiviral activity against Human immunodeficiency virus 1 subtype F BR/93/020 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1191972 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
| AID377704 | Antifungal activity against Cryptococcus neoformans | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7
| Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID551464 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as protection against virus-induced cytopathogenicity after 3 days | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents. |
| AID1141966 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID472672 | Cytotoxicity against human CEM cells expressing GFP after 48 to 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Synthesis and anti-HIV activity of alkylated quinoline 2,4-diols. |
| AID646707 | Cytotoxicity against african green monkey Vero cells after 3 days by hemocytometer analysis | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl-7-deazapurine nucleosides, their phosphoramidate prodrugs and 5'-triphosphates. |
| AID83081 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 7 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1157592 | Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID423280 | Antiviral activity against multinucleoside-resistant HIV1 NL4-3 harboring A62V, V75I, F77L, F116Y, Q151M mutation in viral reverse transcriptase infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro. |
| AID104616 | Ability to reduce 50% viability of MT-4 cells acutely infected with HIV-1 strain IIIB | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Decomposition pathways and in vitro HIV inhibitory effects of isoddA pronucleotides: toward a rational approach for intracellular delivery of nucleoside 5'-monophosphates. |
| AID1888697 | Antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID216718 | Compound was evaluated for anti-retrovirus activity against Visna virus (K184) strain in infected sheep choroid plexus cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Novel acyclonucleotides: synthesis and antiviral activity of alkenylphosphonic acid derivatives of purines and a pyrimidine. |
| AID382981 | Antiviral activity against gastrointestinal rotavirus in human Caco-2 cells assessed as neutralization of virus in the solution before attachment | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
| Unsaturated fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-4-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine and N(6)-benzoyl adenine. |
| AID571601 | Cmax in HIV-1 infected patient at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1460938 | Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 infected in MAGI-CCR5 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID693594 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for wild type HIV1 3B infected in human C8166 cells | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors. |
| AID104767 | Compound was tested for reduction of the viability of mock infected MT-4 cell in test-II | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
| Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes. |
| AID289141 | Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs. |
| AID523479 | Antiviral activity against HIV1 with RT connection domain G190S mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID718367 | Selectivity index, ratio of CC50 for HIV2 ROD infected in human MT4 cells to EC50 for HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
| AID81253 | Effective concentration required to inhibit HIV-1 replication in MT-4 cell line | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| S-acyl-2-thioethyl phosphoramidate diester derivatives as mononucleotide prodrugs. |
| AID1231488 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
| AID319043 | Cytotoxicity against human C8166 cells by MTT method | 2008 | Journal of natural products, Jan, Volume: 71, Issue:1
| Octanorcucurbitane and cucurbitane triterpenoids from the tubers of Hemsleya endecaphylla with HIV-1 inhibitory activity. |
| AID582311 | Antiviral activity against HIV1 Brazilian isolate 93BR021 infected in PHA-stimulated human PBMC assessed as inhibition of viral replication after 7 days | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Heterocyclic compounds that inhibit Rev-RRE function and human immunodeficiency virus type 1 replication. |
| AID105750 | Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.2 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID458876 | Antiviral activity against HIV1 3B in human MT4 cells assessed as RT activity after 5 days by single passage assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| 5-Modified-2'-dU and 2'-dC as mutagenic anti HIV-1 proliferation agents: synthesis and activity. |
| AID422694 | Antiviral activity against HIV1 with reverse transcriptase K70E M184V and K70G M184V mutation by vircotype clinical cutoffs assay relative to wild type HIV1 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
| Novel drug resistance pattern associated with the mutations K70G and M184V in human immunodeficiency virus type 1 reverse transcriptase. |
| AID222387 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 1 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID45836 | Tested for intracellular levels of AZT phosphate against CEM cell lines. | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Synthesis, in vitro anti-breast cancer activity, and intracellular decomposition of amino acid methyl ester and alkyl amide phosphoramidate monoesters of 3'-azido-3'-deoxythymidine (AZT). |
| AID1572524 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID624609 | Specific activity of expressed human recombinant UGT1A6 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID83068 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 10 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1391078 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID1687687 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopa | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID1391079 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID1377171 | Antiviral activity against HIV1 isolate BAL infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID28722 | Partition coefficient (logP) | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID85889 | Compound was evaluated for the antiviral activity against HSV-1; Not determined | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| Synthesis and antiviral activity of novel isodideoxy nucleosides with exocyclic methylene. |
| AID1060632 | Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID13512 | AUC in serum | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine. |
| AID540214 | Clearance in rat after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID1815395 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID257926 | Antiviral activity against HIV1 TEKI replication in PBMC at 1 uM | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent. |
| AID542928 | Induction of preadipocyte differentiation in mouse 3T3-F442A cells assessed as triglyceride accumulation at 0.1 uM after 9 days by oil red O staining relative to control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID357960 | Cytotoxicity against human H9 cells | 2001 | Journal of natural products, Oct, Volume: 64, Issue:10
| Anti-AIDS agents. 48.(1) Anti-HIV activity of moronic acid derivatives and the new melliferone-related triterpenoid isolated from Brazilian propolis. |
| AID590165 | Cytotoxicity against human CEM cells expressing green fluorescent protein after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
| Synthesis of 9-substituted derivatives of berberine as anti-HIV agents. |
| AID1172695 | Cytotoxicity against human KB cells | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
| Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates. |
| AID320326 | Inhibition of wild type HIV 3B reverse transcriptase in MT2 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor. |
| AID648422 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1165076 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
| AID1193107 | Cytotoxicity against IL2-independent cat FL-4 cells assessed as reduction in cell viability after 7 days by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Novel fused tetrathiocines as antivirals that target the nucleocapsid zinc finger containing protein of the feline immunodeficiency virus (FIV) as a model of HIV infection. |
| AID575955 | Antiviral activity against Human immunodeficiency virus 1 subtype A RW/92/016 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID257167 | Antiviral activity against HIV1 IRLL98 mutant strain infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
| AID157558 | Cytotoxic concentration was evaluated using microculture tetrazolium assay (MTA) | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
| N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. |
| AID1446811 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID1561722 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonam | | | |
| AID493817 | Cytotoxicity against human CEM cells expressing green fluorescent protein assessed as oncytotoxic concentration by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus. |
| AID152621 | The antiviral fold-increase activity of the compound (AZT-sensitive to AZT-resistant) | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID217737 | Inhibition of cell growth in vero cells | 1993 | Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
| Structure-activity relationships of beta-D-(2S,5R)- and alpha-D-(2S,5S)-1,3-oxathiolanyl nucleosides as potential anti-HIV agents. |
| AID154801 | Antiviral activity against subtype isolate C strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID23362 | Hydrolysis half life in glycine/HCl buffer at the specified pH; Not available | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID45017 | Concentration of compound required to inhibit 50% of host cell replication of human immunodeficiency virus in CEM-F cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia |
| AID83427 | Effective concentration required for antiviral activity against HIV strain WEJO (syncytia inducing) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID89309 | Inhibitory activity against HIV-2(LAV-2ROD strain) replication in MT-4 cells | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). |
| AID291849 | Cytotoxicity against PBMC after 1 week by trypan blue exclusion test | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID398468 | Inhibition of AMV reverse transcriptase | 1995 | Journal of natural products, Jul, Volume: 58, Issue:7
| Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase. |
| AID235876 | Ratio of CD50 value to that of ED50 value was determined and expressed as selectivity index | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Synthesis, antiretrovirus effects, and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine. |
| AID211648 | Compounds were evaluated for their potential toxic effect on uninfected PHA-stimulated human Peripheral blood mononuclear (PBM) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID392514 | Antiviral activity against HIV2 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks. |
| AID46205 | Tested for the inhibitory activity of virus induced giant cell formation in HIV-2 infected CEM cells | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| 1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity. |
| AID1174083 | Antiviral activity against HIV1 | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs. |
| AID646699 | Cytotoxicity against human HuH7 cells assessed as reduction of 50% rRNA level after 96 hrs | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl-7-deazapurine nucleosides, their phosphoramidate prodrugs and 5'-triphosphates. |
| AID384988 | Cytotoxicity against human C8166 cells after 72 hrs by MTT assay | 2008 | Journal of natural products, May, Volume: 71, Issue:5
| Periglaucines A-D, anti-HBV and -HIV-1 alkaloids from Pericampylus glaucus. |
| AID557280 | Ratio of EC50 for HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID279916 | Increase in triglyceride level in lean Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID82928 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 26 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | | | |
| AID1610038 | Antiviral activity against HIV1 92/BR/018 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4
| Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID104945 | Cytotoxic dose required to reduce the proliferation of normal uninfected MT-4 cells | 1996 | Journal of medicinal chemistry, Jun-07, Volume: 39, Issue:12
| Synthesis and potent anti-HIV-1 activity of novel 6-benzyluracil analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID473141 | Cytotoxicity against human MT2 cells by XTT assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. |
| AID82932 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 7 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1884538 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID105691 | Inhibitory activity against resistant HIV-1 strain MC639r was determined. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID1220792 | Ratio of drug level in blood to plasma in dog | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID235475 | Selectivity index is the ratio between CD50 and IC50 values of the compound | 1998 | Journal of medicinal chemistry, Jan-15, Volume: 41, Issue:2
| Synthesis and anti-HIV-1 activity of novel 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones. |
| AID611910 | Cytotoxicity against human C8166 cells by MTT assay | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus. |
| AID718370 | Cytotoxicity against HIV1 3B infected in human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
| AID154778 | Antiviral activity against subtype isolate A strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID559941 | Antiviral activity against HIV1 A018H infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID1172696 | Cytotoxicity against human HepG2 cells | 2014 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
| Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates. |
| AID125169 | In vitro Cytotoxic concentration in mock-infected A3.01 cells - 100% toxicity. | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID714356 | Inhibition of HIV1 reverse transcriptase incubated for 1 hr by colorimetric assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Synthetic bicyclic iminosugar derivatives fused thiazolidin-4-one as new potential HIV-RT inhibitors. |
| AID79129 | In vitro Cytotoxic concentration which reduced HIV-1 LAV infected H9 cells by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID79309 | Anti-HIV activity against acutely infected H9 lymphocytes. Activity expressed as concentration of compound toxic to 50% of mock-infected H9 cells. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID1237699 | Antiviral activity against HIV1 3B infected in human CEM/0 cells assessed as reduction in virus-induced giant cell formation incubated for 4 to 5 days | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
| Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides. |
| AID235487 | Selectivity index is the ratio of IC50 to EC50 of F-MuLV. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Unsaturated and carbocyclic nucleoside analogues: synthesis, antitumor, and antiviral activity. |
| AID1191402 | Cytotoxicity against human MT4 cells after 5 days MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID373351 | Drug metabolism in human CEM cells assessed as radioactive zidovudine monophosphate accumulation at 2 uM after 2 hrs assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID1261367 | Cytotoxicity against human CEM cells assessed as reduction in cell growth incubated for 5 days by CellTiter 96 AQueous One Solution cell proliferation assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of dihydropyrimidine α,γ-diketobutanoic acid derivatives targeting HIV integrase. |
| AID46801 | Concentration required to reduce 50% of the number of CEM/O cells in the HIV-2 infected cell cultures. | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17
| Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3'-azido-3'-deoxythymidine. |
| AID373388 | Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.22 uM after 24 hrs by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID417054 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine parent-drug level at 600 mg administered in two courses, first BID for 7 to 14 days followed by QD for 7 days and second course the subjects were switched to the other regimen measured per | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID79284 | Effective concentration against HIV-1 replication in H9 lymphocytic cells | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
| Anti-AIDS agents 54. A potent anti-HIV chalcone and flavonoids from genus Desmos. |
| AID83069 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 10 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1199053 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for Human immunodeficiency virus 1 3b infected in human MT4 cells | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID235472 | Selectivity index expressed as CC50/EC50 | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity. |
| AID83226 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID551466 | Selectivity index, ratio of CC50 for human C1866 cells to EC50 for HIV1 3B infected in human C8166 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents. |
| AID678793 | TP_TRANSPORTER: uptake in OCT2A-expressing HEK293 cells | 2002 | Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
| cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. |
| AID81438 | Dose required to inhibit cytopathic effect of human immunodeficiency virus replication in MT-4 cells. | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
| Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides. |
| AID83077 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 21 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID289146 | Antiviral activity against HIV with reverse transcriptase M184V mutation assessed as reduction of potency relative to wild type | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs. |
| AID32212 | Concentration required to inhibit the cytopathic effect of HIV-1 on ATH8 cells | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5
| Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides. |
| AID1235867 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 | 2015 | Journal of natural products, Aug-28, Volume: 78, Issue:8
| Kadcoccinic Acids A-J, Triterpene Acids from Kadsura coccinea. |
| AID574196 | Cytotoxicity against human skeletal muscle Myoblast assessed as change in POLG mitochondrial RNA level on day 5 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID284450 | Cytotoxicity against CEM cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Enantioselective synthesis and antiviral activity of purine and pyrimidine cyclopentenyl C-nucleosides. |
| AID154798 | Antiviral activity against multi drug resistant MDR 769 strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID548578 | Antiviral activity against HIV1 isolate 067 harboring reverse transcriptase A62V/D67G/T69SVG/V75I/T215I mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID717258 | Cytotoxicity against human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID79436 | Evaluated in vitro for the concentration required to produce 50% inhibition of proliferation of H9 lymphocytes | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Synthesis and biological evaluation of prodrugs of zidovudine. |
| AID678721 | Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID718816 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity. |
| AID235383 | Therapeutic index (IC50/EC50) was determined | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
| Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents. |
| AID493722 | Cytotoxicity against human C8166 cells after 3 days by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis of highly functionalized 2,4-diaminoquinazolines as anticancer and anti-HIV agents. |
| AID210882 | Inhibitory affect against rabbit thymus thymidine kinase | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID1546659 | Cytotoxicity against human MT4 cells incubated for 3 days by CellTiter-Glo luminescent assay | | | |
| AID1172375 | Cytotoxicity against human thymidine kinase-deficient 143B cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID417055 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine parent-drug level at 600 mg administered in two courses, first QD for 7 days followed by BID for 7 to 14 days and second course the subjects were switched to the other regimen measured per | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID46043 | Inhibitory activity against the cytopathic effect of HIV-1 IIIB strain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID133201 | Quantity of anylate in S3 which is the soluble fraction in mouse brain after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID279931 | Decrease in cytochrome c oxidase activity in lean Wistar rat inguinal adipose tissue at 70 mg/kg/day by DNA quantification assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID586320 | Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of gag gene expression after 5 days post infection by quantitative real time RT-PCR | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
| AID83266 | Effective concentration required for antiviral activity against HIV strain 214 by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID83417 | Effective concentration required for antiviral activity against HIV strain MCK by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID46649 | Activity against HIV-1 in CEM cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID668361 | Antiviral activity against HIV infected in human TZM-bl cells at 10 uM after 48 hrs by measuring luciferase activity by luminometer analysis | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Design, synthesis and antiviral activity of novel pyridazines. |
| AID341370 | Ratio of EC50 for R5-HIV1MDR/MM in human PHA-PBMC to EC50 for R5-HIV1Ba-L in human PHA-PBMC | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID572774 | Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID89028 | Antiviral activity against wild type HIV virus(xxBRU) in Human peripheral blood mononuclear (PBM) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID46447 | Cytotoxicity on CEM cells; Not tested | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
| (Z)- and (E)-2-((hydroxymethyl)cyclopropylidene)methyladenine and -guanine. New nucleoside analogues with a broad-spectrum antiviral activity. |
| AID540220 | Clearance in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID341184 | Cytotoxicity against human MT4 cells by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID342717 | Aqueous solubility of the compound | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID155105 | The anti-HIV-1 activity was assayed in activated human peripheral blood mononuclear (PBM) cells, relative to RVT | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
| 2('),3(')-didehydro-2('),3(')-dideoxynucleosides are degraded to furfuryl alcohol under acidic conditions. |
| AID341354 | Metabolic stability of the compound in human CEM cells assessed as 3'-azido-2',3'-dideoxythymidine triphosphate intracellular levels at 200 nM after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID222502 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 4 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID106929 | Inhibitory activity against the HIV-1-induced cytopathic effect in MT-2 cell line | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID675192 | Therapeutic index, ratio of TC50 for human PBMC to EC50 for HIV-1 subtype B US/92/727 infected in PBMC | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID46048 | Inhibitory activity against the cytopathic effect of HIV-2 MS strain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID1203619 | Toxicity in rat liver assessed as change in ALT release relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID43987 | Effect of compound against Moloney murine sarcoma virus (MSV)-induced transformation of C3H/3T3 embryo murine fibroblasts | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID525112 | Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID1157595 | Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID155632 | Inhibition of viral RNA in HIVD34-infected PBMC assay on day 4 at concentration of 40 nM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
| AID153137 | Effective concentration of required to inhibit the replication of HIV-1 BY 50% in PMBCs from donor 2 | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID234114 | Specific index of IC50 and CC50 on HIV-1 IIIB wild type | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors. |
| AID548798 | Antiviral activity against HIV1 isolate 185 harboring reverse transcriptase T215Y mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID557276 | Antiviral activity against HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID81413 | Inhibitory effect against HIV-1 in human peripheral blood monocyte cells(PBMC) (EC50 ->0.273 ug/mL) | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| HIV-1 neutralization and tumor cell proliferation inhibition in vitro by simplified analogues of pyrido[4,3,2-mn]thiazolo[5,4-b]acridine marine alkaloids. |
| AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4
| Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1457056 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID576143 | Antiviral activity against Human immunodeficiency virus 1 subtype O BCF02 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID235443 | Selective index as the ratio of CC50 to that of IC50 value. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID79450 | Ability to inhibit HIV-1 multiplication in chronically infected H9/IIIB cells | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID1884542 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID319044 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for HIV1 | 2008 | Journal of natural products, Jan, Volume: 71, Issue:1
| Octanorcucurbitane and cucurbitane triterpenoids from the tubers of Hemsleya endecaphylla with HIV-1 inhibitory activity. |
| AID153141 | Effective concentration required to inhibit the replication of HIV-1 by 50% in PMBCs in the presence of thymidine | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID542927 | Induction of preadipocyte differentiation in mouse 3T3-F442A cells assessed as triglyceride accumulation at 3 uM after 9 days by oil red O staining relative to control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID696751 | Cytotoxicity against human C8166 cells by MTT assay | 2012 | Journal of natural products, Nov-26, Volume: 75, Issue:11
| Antiviral chromones from the stem of Cassia siamea. |
| AID1368346 | Antiviral activity against HIV-1 3B infected in human TZM-bl cells treated for 2 hrs followed by compound washout measured after 2 days by luciferase reporter assay | 2018 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
| Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41. |
| AID46847 | Activity against HIV-1 in CEM/TK cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID1357795 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID405346 | Toxicity against human HepG2/C3A cells assessed as effect on mitochondrial DNA copy numbers at 50 uM after 10 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID519881 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1460945 | Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 harboring reverse transcriptase E138A mutant infected in MAGI-CCR5 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID235686 | Selectivity Index measured as the ratio of EC50(MT-4) to that of CC50(MT-4). | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID646708 | Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion method | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl-7-deazapurine nucleosides, their phosphoramidate prodrugs and 5'-triphosphates. |
| AID1231486 | Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
| AID216044 | Inhibitory activity was evaluated in Vero cells. | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
| Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2', 3'-unsaturated L-nucleosides. |
| AID257929 | Therapeutic index (TI=CC50/IC50) in HIV1 TEKI at 1 uM | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent. |
| AID373570 | Antiviral activity against 0.1 MOI HIV1 3B in 24 hrs pretreated human TZM-b1 cells infected 48 hrs post drug removal assessed as inhibition of viral replication at 0.04 to 0.22 uM measured 24 hrs postinfection by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID155118 | Compound was evaluated for its anti-HIV activity in vitro in peripheral blood mononuclear (PBM) cells; Not determined | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine. |
| AID1572528 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID1055512 | Antiviral activity against HIV1 3B infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis | 2013 | European journal of medicinal chemistry, , Volume: 70 | Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides. |
| AID571602 | AUC (0 to 12 hrs) in HIV-1 infected patient at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1460946 | Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 harboring reverse transcriptase Y181C mutant infected in MAGI-CCR5 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID142324 | Reduced IL-3 dependent colony formation in murine bone marrow progenitor cells at 0.05 uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID614141 | Antiviral activity against wild type Human immunodeficiency virus 1 3B bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
| AID1383890 | Antiviral activity against HIV1 | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Polypharmacology in HIV inhibition: can a drug with simultaneous action against two relevant targets be an alternative to combination therapy? |
| AID1757984 | Antiviral activity against HIV-1 infected in human MT4 cells assessed as reduction in virus-indued cytopathogenicity incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID406056 | Terminal phase half life in rhesus monkey | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID380205 | Cytotoxicity against human MT4 cells by MTT assay | 1999 | Journal of natural products, Jul, Volume: 62, Issue:7
| Biological evaluation of proanthocyanidin dimers and related polyphenols. |
| AID79116 | Evaluated for the anti-HIV activity against HIV-1 replication in H9 lymphocyte cells | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents. |
| AID481806 | Ratio of Vmax to Km for human TK1 | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID81244 | Compound was evaluated for the antiviral activity against compound resistant virus isolate Y181C with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID235202 | Therapeutic index for inhibition of uninfected H9 cell growth to that of inhibition of HIV-1 replication in H9 lymphocyte cells. | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues. |
| AID1304400 | Antiviral activity against HIV-1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID1714434 | Cytotoxicity in human PBMC cells | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Synthesis and Antiviral Evaluation of Octadecyloxyethyl Benzyl 9-[(2-Phosphonomethoxy)ethyl]guanine (ODE-Bn-PMEG), a Potent Inhibitor of Transient HPV DNA Amplification. |
| AID666971 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
| AID105749 | Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.008 uM concentration; Range is 40-60 | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID1267608 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID548583 | Antiviral activity against HIV1 isolate 157 harboring reverse transcriptase L74V/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1761007 | Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 1 day by CytoTox-Glo assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID288631 | Antiviral activity against HIV1 3B in C8166 cells | 2007 | Journal of natural products, Jun, Volume: 70, Issue:6
| Triterpenoids from Schisandra rubriflora. |
| AID559935 | Antiviral activity against HIV1 NL4-3 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID83419 | Effective concentration required for antiviral activity against HIV strain PM16 by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID548587 | Antiviral activity against HIV1 isolate 174 harboring reverse transcriptase M184V mutant gene obtained as site-directed mutant of NL4-3 by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID548548 | Antiviral activity against HIV1 isolate JR-CSF infected in human MDM after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID540215 | Volume of distribution at steady state in rat after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID1561721 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide to EC | | | |
| AID558374 | Drug level in HIV-infected pregnant woman cord blood plasma at 300 mg, po BID by LC/MS/MS analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
| Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID1203620 | Cytotoxicity against human 5637 cells assessed as growth inhibition at 50 uM after 48 hrs by MTT assay relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID197785 | Inhibition of recombinant HIV-1 reverse transcriptase | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
| Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID81251 | Effective concentration required to inhibit HIV-1 replication in CEM-SS cell line | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| S-acyl-2-thioethyl phosphoramidate diester derivatives as mononucleotide prodrugs. |
| AID717259 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID1714433 | Inhibition of HIV1 92US727 replication in PHA-P-stimulated human PBMCs incubated for 7 days by reverse transcriptase activity based assay | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Synthesis and Antiviral Evaluation of Octadecyloxyethyl Benzyl 9-[(2-Phosphonomethoxy)ethyl]guanine (ODE-Bn-PMEG), a Potent Inhibitor of Transient HPV DNA Amplification. |
| AID1410412 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
| AID45898 | Compound was tested for activity against HIV-1 by syncytial plaque assay performed in duplicate using CEM-SS cells | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole. |
| AID79437 | Inhibition of HIV replication was determined in H9 lymphocytes | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| Anti-AIDS agents. 42. Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone analogues. |
| AID1304402 | Cytotoxicity against mock-infected human CEM-SS cells | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID1180342 | Inhibition of HIV-1 reverse transcriptase after 1 hr by ELISA plate reader analysis | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
| Synthesis of bi-/tricyclic azasugars fused thiazinan-4-one and their HIV-RT inhibitory activity. |
| AID32208 | Concentration required to suppress the growth of target ATH8 cells | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5
| Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides. |
| AID523354 | Antiviral activity against HIV1 with RT connection domain Y181C/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID1292011 | Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID689101 | Antiviral activity against HIV1 pseudovirus by cell-based assay | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
| Phosphoramidate derivatives of acyclovir: synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro. |
| AID79283 | Concentration that inhibits HIV-1 replication in cell growth in H9 lymphocytes | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
| Anti-HIV agents. Part 55: 3'R,4'R-Di-(O)-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP), a novel anti-HIV agent. |
| AID1888699 | Antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID1483278 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID548581 | Antiviral activity against HIV1 isolate 071 harboring reverse transcriptase 65R/S68N/184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID645267 | Antiviral activity against HIV1 harboring VSV glycoprotein-G co-transfected with luciferase gene infected in human TZM-bl cells assessed as inhibition of viral replication at 10 uM after 48 hrs by microplate luminometer based luciferase assay | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Hydroxyl may not be indispensable for raltegravir: Design, synthesis and SAR Studies of raltegravir derivatives as HIV-1 inhibitors. |
| AID1275554 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV2 ROD infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID1888691 | Toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay | | | |
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
| A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| AID81247 | Compound was evaluated for the antiviral activity against resistant virus isolate IIIB with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID548307 | Antiviral activity against HIV1 subtype B isolate 92BR014 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID16519 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into rest of the brain | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID664471 | Antiviral activity against NNRTI-resistant HIV1 clade B A-17 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infecti | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID104773 | Concentration required to reduce the viability of mock-infected MT-4 cells by 50% (4 days) | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs. |
| AID1720087 | Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity measured after 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment. |
| AID357961 | Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral p24 antigen levels after 4 days by ELISA | 2001 | Journal of natural products, Oct, Volume: 64, Issue:10
| Anti-AIDS agents. 48.(1) Anti-HIV activity of moronic acid derivatives and the new melliferone-related triterpenoid isolated from Brazilian propolis. |
| AID295757 | Cytotoxicity against human HeLa cells at 100 uM after 48 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
| Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates. |
| AID81236 | Compound was evaluated for the antiviral activity against compound resistant virus isolate K101E with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID1141971 | Ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID611609 | Antiviral activity against HIV1 A17 expressing reverse transcriptase K103N/Y181C double mutant infected in human C8166 cells assessed as protection against virus-induced cytopathogenicity after 3 days by measuring syncytia under inverted microscope | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1056584 | Antiviral activity against wild-type HIV-1 infected in HEK293T cells co-transfected with VSVG protein assessed as time required for 50% failure of viral replication at 10 uM by luciferase reporter gene assay | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12
| Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
| AID235254 | Therapeutic index(TI) was measured as ratio of TD50 and MIC50 (Retrovirus) | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| Anti-HIV-I activity of linked lexitropsins. |
| AID583458 | Cytotoxicity against human HepG2 cells assessed as inhibition of mitochondrial respiratory chain complex III activity at 50 uM after 15 days relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID1543132 | Antiviral activity against HIV NL4-3 infected in human MT4 cells measured on day 3 post-infection by Nano-Glo luciferase assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6
| Potent Anti-HIV Ingenane Diterpenoids from Euphorbia ebracteolata. |
| AID417249 | Tmax in HIV-infected human assessed as zidovudine monophosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID573999 | Ratio of EC50 for Human immunodeficiency virus in presence of 10% FCS to EC50 for Human immunodeficiency virus in presence of 50% human serum | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID247698 | Inhibitory concentration against HIV-I RTMDR1 in MT-4 cells | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Anti-AIDS agents. 60. Substituted 3'R,4'R-di-O-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) analogues as potent anti-HIV agents. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | | | |
| AID45991 | Cytotoxic concentration required to reduce CEM cell viability by 50% | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents. |
| AID209370 | Effective concentration to inhibit HIV replication in TK CEM-SS cell line | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
| Rational design of a new series of pronucleotide. |
| AID548316 | Antiviral activity against HIV1 subtype D isolate 92UG046 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID222503 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 8 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID226670 | Compound was evaluated for its cytotoxicity. | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| Synthesis and antiviral activity of novel isodideoxy nucleosides with exocyclic methylene. |
| AID1231851 | Selectivity index, CC50 for african green monkey Vero cells to EC50 for HIV2 ROD | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6
| Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID18608 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
| QSAR model for drug human oral bioavailability. |
| AID1316806 | Selectivity index, ratio of CC50 for human MT-4 cells to IC50 for HIV-1 3B infected in human MT-4 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
| AID1298247 | Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
| AID1565094 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV RES056 | | | |
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Physicochemical determinants of human renal clearance. |
| AID1235865 | Antiviral activity against HIV1 assessed as inhibition of cytopathic effect by microtiter syncytium formation infectivity assay | 2015 | Journal of natural products, Aug-28, Volume: 78, Issue:8
| Kadcoccinic Acids A-J, Triterpene Acids from Kadsura coccinea. |
| AID83436 | Inhibitory activity against wild type strain,HIV104pre. | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
| AID1157585 | Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID1204139 | Antimycobacterial activity against Mycobacterium sp. | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| PMA-SiO2 catalyzed synthesis of indolo[2,3-c]quinolines as potent anti cancer agents. |
| AID1705186 | Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID104961 | Cytotoxic concentration for 50% death of MT-4 cell culture infected by HIV-1 | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID104256 | Compound was tested for its inhibitory activity against HIV replication in MT-2 cells. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID1316346 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID1710800 | Cytotoxicity against dog MDCK cells assessed as changes in cell morphology incubated for 3 to 6 days by light microscopy | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID1705187 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID291847 | Inhibition of HTLV1 reverse transcriptase | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID222491 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 1 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID346974 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV ROD | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Studies on anti-HIV quinolones: new insights on the C-6 position. |
| AID519877 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID152646 | Cytotoxicity against uninfected PHA-stimulated human peripheral blood mononuclear (PBM) cells was determined. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| 1,3-dioxolanylpurine nucleosides (2R,4R) and (2R,4S) with selective anti-HIV-1 activity in human lymphocytes. |
| AID1446813 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID1126508 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID542929 | Induction of preadipocyte differentiation in mouse 3T3L1 cells assessed as PPARgamma mRNA expression on day 6 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1705183 | Antiviral activity against HIV-1 NL4-3 infected in human MT-4 cells assessed as virus induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID1203629 | Induction of apoptosis in human 5637 cells assessed as ratio of Bax mRNA to Bcl2 mRNA level at 100 uM after 48 hrs by real-time PCR analysis (Rvb = 0.08 to 0.13 No_unit) | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID519963 | Antiviral activity against HIV1 3B infected in MOLT-4/3B cells assessed as inhibition of mature virus release measured after 4 days of infection by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID154776 | Antiviral activity against multi drug resistant MDR 769 strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID325392 | Activity of TMPK in human CEM cells assessed as level of triphosphate metabolites per 10^6 cells at 2 uM after 12 hrs | 2007 | Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
| Comparison of the phosphorylation of 4'-ethynyl 2',3'-dihydro-3'-deoxythymidine with that of other anti-human immunodeficiency virus thymidine analogs. |
| AID576193 | Antiviral activity against Human immunodeficiency virus 1 A7 harboring Tyr127His mutation in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID83211 | Compounds were evaluated for anti-RT activity at 7 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID460294 | Cytotoxicity against GFP expressing human CEM cells after 48 to 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols. |
| AID379883 | Antiviral activity against HIV1 3B in H9 cells after 4 days by p24-antigen ELISA | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12
| Rubrisandrins A and B, lignans and related anti-HIV compounds from Schisandra rubriflora. |
| AID45176 | Cytotoxic concentration required to reduce the viability of mock infected CEM-SS cells by 50%. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
| Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils. |
| AID104755 | Antiviral activity in MT-4 cell line infected with HIV-1 and cytotoxic concentration required to reduce the viability of uninfected cells by 50% | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID373564 | Antiviral activity against 0.1 MOI HIV1 3B in 24 hrs pretreated human TZM-b1 cells infected 24 hrs post drug removal assessed as inhibition of viral replication at 0.04 to 0.22 uM measured 24 hrs postinfection by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID106411 | Number of infected cells at 10e-5 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID155272 | Ability to inhibit the replication of HTLV IIIb strain of HIV-1 p24 antigen production in PBMC | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
| N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. |
| AID1561716 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in absence of test compound assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID681563 | TP_TRANSPORTER: Cytotoxicity in MT-4 and MT-4/DOX500 cells | 2003 | Molecular pharmacology, Jan, Volume: 63, Issue:1
| Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. |
| AID1267610 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID217433 | Antiviral activity against Vero cells, infected with HSV-1 | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID512143 | Cytotoxicity against african human CEM cells after 6 days by XTT assay | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents. |
| AID1561718 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against virus-indu | | | |
| AID595594 | Antiviral activity against Human immunodeficiency virus 1 LAV1 assessed as reduction in RT activity by [3H]-dTTP incorporation assay | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Broad-spectrum antiviral activity including human immunodeficiency and hepatitis C viruses mediated by a novel retinoid thiosemicarbazone derivative. |
| AID576392 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1410485 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
| AID106919 | Anti-HIV activity against HIV-I IIIB strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID1220790 | Ratio of drug level in blood to plasma in rat | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1729157 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID155119 | The anti-HIV-1 activity was assayed in activated human peripheral blood mononuclear (PBM) cells, relative to RVT | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
| 2('),3(')-didehydro-2('),3(')-dideoxynucleosides are degraded to furfuryl alcohol under acidic conditions. |
| AID1141964 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID658567 | Resistance factor, ratio of EC50 for multidrug-resistant HIV1 106-PR infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
| AID43981 | Compound was tested for anti-retroviral activity against moloney murine sarcoma virus (MSV) in murine C3H/3T3 embryo fibroblast cell culture | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
| Acyclic nucleotide analogs derived from 8-azapurines: synthesis and antiviral activity. |
| AID104399 | Total viral index (TAI) is the area between the cytotoxicity and the antiviral activity curve for MT-2 cell line. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID693592 | Antiviral activity against HIV2 ROD infected in human C8166 cells assessed as protection against virus-induced cytopathic effect after 3 days by syncytium reduction assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors. |
| AID757624 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID144029 | Inhibitory concentration against Mycobacterium intracellular; Not tested | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| New manzamine alkaloids from an Indo-Pacific sponge. Pharmacokinetics, oral availability, and the significant activity of several manzamines against HIV-I, AIDS opportunistic infections, and inflammatory diseases. |
| AID365483 | Antiviral activity against HIV1 3B in MT4 cells assessed as virus p24 antigen production administered at 5 hrs post infection by ELISA | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Structure-activity relationship study on anti-HIV 6-desfluoroquinolones. |
| AID1357801 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase K103N mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID160635 | Relative potency of compound to that of parent HIV Protease inhibitor, KNI-727 was determined | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
| 'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker. |
| AID671655 | Selectivity ratio of CC50 for human PBMC to EC50 for R5-tropic Human immunodeficiency virus 1 Ba-L subtype B | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Oxoquinoline acyclonucleoside phosphonate analogues as a new class of specific inhibitors of human immunodeficiency virus type 1. |
| AID548312 | Antiviral activity against HIV1 subtype C isolate 91IN101 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID226220 | Concentration of external nucleoside in mouse brain | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID576147 | Antiviral activity against simian immunodeficiency virus Mac251 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID106972 | Concentration required to inhibit the cytopathicity of HIV-1 strain IIIB by 50% in MT-4 cells (expressed in AZT equivalent) | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities. |
| AID370732 | Cytotoxicity against human C8166 cells by MTT method | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
| AID230271 | Ratio of TICD50 to that of IC50 of human immunodeficiency virus (HIV-1) | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia |
| AID569224 | Therapeutic index, ratio of CC50 for human CEM-GFP cells to EC50 for HIV1 NL4.3 | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
| Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5. |
| AID105513 | Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 virus. | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1267627 | Antiviral activity against AZT-resistant HIV1 ADP/141 harboring reverse transcriptase D67N/K70R/T215F/K219Q mutant infected in human MT4 cells | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID1060627 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID227258 | Ratio of CD50 to ID50 was determined | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| Uncharged AZT and D4T derivatives of phosphonoformic and phosphonoacetic acids as anti-HIV pronucleosides. |
| AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID449491 | Cytotoxicity against human MT4 cells as reduction in cell viability after 5 days by MTT assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID46384 | Antiviral activity against site directed resistant isolates in HIV-1 A98G CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID1410483 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
| AID553575 | Antiviral activity against HIV1 MOKW infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID449422 | Inhibition of HIV1 reverse transcriptase M41L/D67N/K70R/T215Y/K219Q mutant-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| The nucleoside analogue D-carba T blocks HIV-1 reverse transcription. |
| AID54867 | Inhibitory concentration against Cryptococcus neoformans; Not tested | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| New manzamine alkaloids from an Indo-Pacific sponge. Pharmacokinetics, oral availability, and the significant activity of several manzamines against HIV-I, AIDS opportunistic infections, and inflammatory diseases. |
| AID1203630 | Induction of apoptosis in human 5637 cells assessed as ratio of Bax mRNA to Bcl2 mRNA level at 50 uM after 48 hrs by real-time PCR analysis (Rvb = 0.08 to 0.13 No_unit) | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID235289 | CC50/EC50 was measured | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID1357803 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y181C mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID422695 | Ratio of IC50 for HIV1 with reverse transcriptase K70G mutation to IC50 for wild type HIV1 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
| Novel drug resistance pattern associated with the mutations K70G and M184V in human immunodeficiency virus type 1 reverse transcriptase. |
| AID155133 | Ability to inhibit the replication of A17 (Y181C) strain of HIV-1 p24 antigen production in PBMC | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
| N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. |
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1053517 | Binding affinity to HIV1 reverse transcriptase assessed as compound incorporation into DNA by primer extension assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID542941 | Induction of adipocyte differentiation in mouse 3T3-F442A cells assessed as triglyceride accumulation at 6 uM on day 9 by oil red O staining relative to control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID568182 | Antiviral activity against R5 tropic HIV1 Ba-L infected in human PBMC assessed as inhibition of HIN p24 antigen expression | 2011 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
| Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate. |
| AID1457788 | Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 6 days by XTT dye based assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs. |
| AID90921 | Bone marrow toxicity was measured against human colony forming units-granulocyte monocyte (CFU-GM), concentration is 1.0 uM | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID419085 | Inhibition of HIV1 replication in human 293T cells preincubated 15 mins prior to infection measured after 48 hrs postinfection by luciferase reporter gene assay | 2009 | Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
| Synthesis and biological evaluation of N4-(hetero)arylsulfonylquinoxalinones as HIV-1 reverse transcriptase inhibitors. |
| AID665549 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID53666 | Inhibitory activity against DNA polymerase-alpha derived from peripheral blood mononuclear cells | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID619511 | Cytotoxicity against human CEM-T4 cells assessed as cell viability after 7 days by MTT assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
| Aryl H-phosphonates 17: (N-aryl)phosphoramidates of pyrimidine nucleoside analogues and their synthesis, selected properties, and anti-HIV activity. |
| AID1729161 | Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID519861 | Antiviral activity against HIV1 subtype B-3B infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID82565 | The 90% inhibitory concentration expresses cellular toxicity measured against normal human granulocyte-monocyte cells | 1989 | Journal 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. |
| AID572785 | Antiviral activity against HIV1 harboring reverse transcriptase M41L/D67N/K70R/L210W/T215Y/K219Q mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID79117 | Inhibitory concentration against HIV-1 replication in acutely infected H9 lymphocytes | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Anti-AIDS agents. Part 47: Synthesis and anti-HIV activity of 3-substituted 3',4'-Di-O-(S)-camphanoyl-(3'R,4'R)-(+)-cis-khellactone derivatives. |
| AID46374 | Antiviral activity against site directed 4X AZT resistant isolate HIV-1 L100I in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID222676 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 1 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1288069 | Inhibition of HIV1 reverse transcriptase using DIG-labeled dNTPs as substrate after 1 hr by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Synthesis of tetracyclic iminosugars fused benzo[e][1,3]thiazin-4-one and their HIV-RT inhibitory activity. |
| AID79125 | Concentration required to inhibit uninfected H9 cell growth | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues. |
| AID222392 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 8 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1545831 | Antiproliferative activity against human HepG2 cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
| AID84646 | Activity against HTLV-III/LAV/AAV, was determined in vitro. | 1987 | Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
| Synthesis and antiviral activity of various 3'-azido, 3'-amino, 2',3'-unsaturated, and 2',3'-dideoxy analogues of pyrimidine deoxyribonucleosides against retroviruses. |
| AID572781 | Ratio of IC50 for HIV1 harboring reverse transcriptase Q151M mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID1720085 | Antiviral activity against Human immunodeficiency virus 1 NLAD-8 infected in human PM1 cells expressing CCR5 assessed as reduction in virus-induced cytopathogenicity measured after 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment. |
| AID87598 | Tested in vitro against HIV-1 104pre from HeLa-CD4-LT4-beta gal-cells using MAGI assay | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity. |
| AID1754641 | Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID155299 | Cytotoxicity was determined in PBM cells, relative to RVT | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
| 2('),3(')-didehydro-2('),3(')-dideoxynucleosides are degraded to furfuryl alcohol under acidic conditions. |
| AID1357799 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID572769 | Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1231846 | Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6
| Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID1320867 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
| AID572776 | Antiviral activity against HIV1 harboring reverse transcriptase M184V mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1203621 | Cytotoxicity against human 5637 cells assessed as growth inhibition at 12.5 to 200 uM after 48 hrs by MTT assay relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID105136 | Concentration required to inhibit syncytia formation by 50% on HIV-1 infected MT-4 cells | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
| New bicyclam-AZT conjugates: design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor. |
| AID224946 | Compound was tested for anti-HIV activity in normal peripheral blood mononuclear cells infected with HIV-1(RTMDR-1) virus by inhibition of reverse transcriptase activity | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
| Enhancing effects of a mono-bromo substitution at the para position of the phenyl moiety on the metabolism and anti-HIV activity of d4T-phenyl methoxyalaninyl phosphate derivatives. |
| AID106768 | Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50% | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides. |
| AID45682 | Anti HIV-1 activity in human lymphocyte CEM/0 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | | | |
| AID222501 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 48 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1053503 | Binding affinity to HIV1 reverse transcriptase assessed as compound-terminated template/primer translocation from N-site to P-site of enzyme preincubated for 20 mins prior to TTP addition measured after 10 mins by gel electrophoretic analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID95276 | Cytotoxic concentration against HIV-1 infected Jurkat cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID1653796 | Substrate activity at human mARC2 expressed in Escherichia coli assessed as turnover rates at 3 mM pre-incubated for 3 mins followed by NADH addition and measured after 15 mins by UV-Visible spectroscopy based NADH assay | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| Drug Metabolism by the Mitochondrial Amidoxime Reducing Component (mARC): Rapid Assay and Identification of New Substrates. |
| AID548537 | Antiviral activity against HIV1 group O isolate BCF01 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID576192 | Antiviral activity against Human immunodeficiency virus 1 D1 harboring Tyr127His mutation in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID571597 | Apparent oral clearance in HIV-1 infected patient at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID222817 | In Vitro detection by Gray and Whittaker method for the total internal nucleoside | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID45027 | Effective concentration required to inhibit the replication of HIV-1 by 50% in CEM-SS cells | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID81243 | Compound was evaluated for the antiviral activity against compound resistant virus isolate V1081 with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | | | |
| AID222386 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 0.5 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID586326 | Cytotoxicity against PHA-stimutated human PBMC after 24 hrs by MTS assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
| AID519964 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1761008 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID548570 | Selectivity ratio of EC50 for HIV1 8415-2 harboring reverse transcriptase 65R/184V mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1267611 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID154804 | Antiviral activity against subtype isolate F strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID717452 | Antiviral activity against HIV1 LAI infected in human PBMC assessed as inhibition of viral replication | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Synthesis, evaluation of anti-HIV-1 and anti-HCV activity of novel 2',3'-dideoxy-2',2'-difluoro-4'-azanucleosides. |
| AID548835 | Antiviral activity against HIV1 isolate 204 harboring reverse transcriptase M41L/L210W/T215Y/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID647168 | Binding affinity to human serum albumin by fluorescence quenching assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Synthesis and antiviral activities of novel gossypol derivatives. |
| AID1056504 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of viral-induced cytopathogenicity by syncytium formation assay | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12
| Kadcotriones A-C: tricyclic triterpenoids from Kadsura coccinea. |
| AID342549 | Cytotoxicity against human CEM-SS cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID519867 | Antiviral activity against HIV1 subtype B-ASM 034 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID548314 | Antiviral activity against HIV1 subtype D isolate 92UG001 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID104429 | Effective concentration required to achieve 50% inhibition of HIV-1 IIIB multiplication in hT4 lymphoblastoid MT-4 cells using MTT assay | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID210881 | Inhibitory affect against rabbit thymus thymidine kinase and represented as molt/4F kinase. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID226233 | Fold increase ratio of HIV-1M184V to HIV-1XXBRU | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance. |
| AID617765 | Antiviral activity against HIV1 SF162 infected in human TZM-bl cells assessed as inhibition of virus neutralization after 48 hrs by luciferase assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Synthesis and biological evaluation of 2',4'- and 3',4'-bridged nucleoside analogues. |
| AID1456308 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
| AID279922 | Effect on LDL cholesterol level in lean Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID439740 | Inhibition of Vesicular stomatitis virus envelope glycoprotein-mediated viral entry into human A549 cells assessed as infectivity at 10 uM after 48 hrs postinfection by luciferase assay relative to control | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of the first series of small molecule H5N1 entry inhibitors. |
| AID1238314 | Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 2.5 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID83283 | Effective concentration required for antiviral activity against HIV strain G by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID341996 | Antimicrobial activity against Streptococcus sp. 07941-1 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID665553 | Fold resistance, ratio of EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant to EC50 for wild type HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID46200 | Tested for in vitro drug concentration which produces 50% survival of HIV-1 infected CEM cells relative to uninfected untreated controls | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine. |
| AID84930 | Compound was evaluated for the antiviral activity against HSV-2; Not determined | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| Synthesis and antiviral activity of novel isodideoxy nucleosides with exocyclic methylene. |
| AID449489 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus induced cytotoxicity after 5 days by MTT assay | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID46636 | Concentration required to reduce by 50% the viability of noninfected treated CEM-CL13 cells | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs. |
| AID573976 | Antiretroviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID1752327 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay | 2021 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 50 | New phorbol ester derivatives as potent anti-HIV agents. |
| AID257930 | Therapeutic index (TI=CC50/IC50) in HIV1 NL4-3 at uM | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent. |
| AID417254 | Cmin in HIV-infected human assessed as zidovudine diphosphate level in PBMC at 600 mg QD for 7 days measured per 10'6 cells in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID746746 | Cytotoxicity against human MT2 cells by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design, synthesis, and biological evaluation of new 2'-deoxy-2'-fluoro-4'-triazole cytidine nucleosides as potent antiviral agents. |
| AID154772 | Antiviral activity against SLKA virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID45013 | Concentration that reduced by 50% the HIV induced CPE (cytopathic effect) on day 7. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID706458 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as p24 antigen level after 4 days by ELISA | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID81242 | Compound was evaluated for the antiviral activity against compound resistant virus isolate T1391 with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID154771 | Antiviral activity against ROJO virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID548569 | Selectivity ratio of EC50 for HIV1 71361-1 harboring reverse transcriptase 65R mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1517733 | Antiviral activity against HIV-1 NL4-3 infected in human CEM-GFP cells assessed as suppression of viral replication by measuring reduction in p24 level measured at 72 hrs post-infection by ELISA | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-isoxazol-3-yl-acetamide analogues as heat shock protein 90 (HSP90) inhibitors with significant anti-HIV activity. |
| AID21904 | Concentration in mouse blood 15 min post injection at a dose 240 mocromol/kg | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID1223470 | Drug metabolism in non-diabetic human kidney microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID1231489 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
| AID341180 | Antiviral activity against R5-HIV1MDR/MM assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID89159 | Effective concentration against Wild Type HIV-1 virus in human peripheral blood mononuclear cells | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
| Synthesis, structure-activity relationships, and drug resistance of beta-d-3'-fluoro-2',3'-unsaturated nucleosides as anti-HIV Agents. |
| AID214214 | inhibition of infectious virus production in U1 cells | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID1888693 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID16517 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into hypothalamus | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID679515 | TP_TRANSPORTER: inhibition of PAH uptake (PAH: 5 uM, AZT: 1000 uM) in OAT1-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID548833 | Antiviral activity against HIV1 isolate 201 harboring reverse transcriptase M41L/L210W/T215Y mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID320330 | Antiviral activity against HIV with reverse transcriptase M184V mutation assessed as fold resistance relative to wild type | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor. |
| AID1157584 | Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID46651 | Activity against HIV-2 in CEM cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID153140 | Effective concentration required to inhibit the replication of HIV-1 by 50% in PMBCs in the absence of thymidine | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID612671 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for wild type HIV1 3B | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
| Synthesis and biological evaluation of (±)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID548819 | Antiviral activity against HIV1 isolate 070 harboring reverse transcriptase 65R/S68G mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID83268 | Effective concentration required for antiviral activity against HIV strain BAKI (syncytia inducing) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID82137 | Inhibition of HIV-1 (strain A17)-infected MT-4 cells | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. |
| AID607809 | Cytotoxicity against human C8166 cells by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1443667 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID32220 | Selectivity index expressed as ratio of compound concentration required to reduce the growth of normal uninfected ATH8 cells by 50% to the compound concentration (MIC) | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
| Chemotherapeutic approaches to the treatment of the acquired immune deficiency syndrome (AIDS). |
| AID405332 | Toxicity in human HepG2/C3A cells assessed as induction of cell death at 10 uM after 4 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID417058 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine triphosphate level at 600 mg administered in two courses, first BID for 7 to 14 days followed by QD for 7 days and second course the subjects were switched to the other regimen measured per | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID548557 | Antiviral activity against HIV1 7324-1 harboring reverse transcriptase 41L/67N/69N/70R/215F/219E mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID584603 | Toxicity in human subcutaneous preadipocytes assessed as decrease of mitochondrial DNA abundance at 6 uM after 30 days by RT-PCR analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1517732 | Cytotoxicity against human CEM-GFP cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-isoxazol-3-yl-acetamide analogues as heat shock protein 90 (HSP90) inhibitors with significant anti-HIV activity. |
| AID81966 | Protection of MT-4 lymphocytes by the compound against HIV-1 infectivity in vitro at a concentration of 0.032 ug/mL (0.0012 uM/mL) | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| HIV-1 neutralization and tumor cell proliferation inhibition in vitro by simplified analogues of pyrido[4,3,2-mn]thiazolo[5,4-b]acridine marine alkaloids. |
| AID1352318 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID106918 | Anti-HIV activity against HIV-I H112-2 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID499278 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
| Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
| AID142325 | Reduced IL-3 dependent colony formation in murine bone marrow progenitor cells at 0.5 uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID210904 | Inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis | 2003 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 13, Issue:18
| Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase. |
| AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4
| Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID630379 | Oral bioavailability in human | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Synthesis and anticancer activity of 5'-chloromethylphosphonates of 3'-azido-3'-deoxythymidine (AZT). |
| AID1410411 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
| AID1200844 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
| AID106948 | Anti-HIV activity based on the protection against HIV-induced cytopathogenicity in MT-4 cells using MTT method | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety. |
| AID46174 | Effective concentration against HIV-1-infected CEM cells in mice administered intraperitoneally | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
| Nucleoside conjugates. 15. Synthesis and biological activity of anti-HIV nucleoside conjugates of ether and thioether phospholipids. |
| AID576201 | Antiviral activity against Human immunodeficiency virus 1 3B infected in AA5 cells infected with 3.13 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1729149 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID1483281 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID47105 | compound tested for anti-HIV-1 activity by plaque reduction assay against HIV-1 in CEM cells | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Synthesis and antiviral activity of novel acyclic nucleosides: discovery of a cyclopropyl nucleoside with potent inhibitory activity against herpesviruses. |
| AID1060628 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID576387 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 25 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID104285 | Inhibition of HIV-1 (BRU) cytopathicity in MT-4 (human leukemia). | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID1220797 | Volume of distribution at steady state in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID152659 | Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17. | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
| Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. |
| AID1565097 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID1053507 | Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID732658 | Cytotoxicity against human C8166 cells assessed as inhibition of cell viability after 3 days by MTT assay | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Antiviral phenolic compounds from Arundina gramnifolia. |
| AID590167 | Therapeutic index, ratio of CC50 for human CEM cells expressing green fluorescent protein to EC50 for Human immunodeficiency virus 1 NL4.3 | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
| Synthesis of 9-substituted derivatives of berberine as anti-HIV agents. |
| AID79438 | Anti-HIV activity in H9 lymphocytes. | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
| Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents. |
| AID1285840 | Cytotoxicity against human C8166 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
| Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors. |
| AID1456311 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B wild type reverse transcriptase infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
| AID20867 | Concentration in 1-octanol / concentration in water | 1994 | Journal of medicinal chemistry, Dec-09, Volume: 37, Issue:25
| Synthesis, in vitro biological stability, and anti-HIV activity of 5-halo-6-alkoxy(or azido)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs to 3'-azido-3'-deoxythymidine (AZT). |
| AID539772 | Cytotoxicity against human CEM-SS cells assessed as cell viability by XTT assay | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
| 1-Benzyl derivatives of 5-(arylamino)uracils as anti-HIV-1 and anti-EBV agents. |
| AID233026 | Selective index was evaluated from inhibitory concentrations of compound | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| Structure-based design of N-[2-(1-piperidinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID1720088 | Cytotoxicity against Human immunodeficiency virus 1 NLAD8 infected in human PM1 cells expressing CCR5 assessed as cell viability measured after 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment. |
| AID81241 | Compound was evaluated for the antiviral activity against compound resistant virus isolate P236L with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID575954 | Antiviral activity against Human immunodeficiency virus 1 MDR 769 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4
| Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID83073 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 14 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID342005 | Antibacterial activity against deoxyribonucleotide kinase-deficient Escherichia coli KY895 expressing Streptococcus pyogenes recombinant thymidine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID766742 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against viral-induced cytopathogenicity after 4 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Synthesis and evaluation of novel 3-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents. |
| AID45706 | The compound was tested for anti HIV activity in CEM-SS cell lines | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
| Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents. |
| AID106758 | The compound was tested for cytotoxic concentration required to reduce the viability of MT-4 cells | 2002 | Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
| New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation. |
| AID379612 | Cytotoxicity against human H9 cells | 2000 | Journal of natural products, Mar, Volume: 63, Issue:3
| Sesquiterpene alkaloids from Tripterygium hypoglaucum and Tripterygium wilfordii: a new class of potent anti-HIV agents. |
| AID1504702 | Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID1572522 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | | | |
| AID523481 | Antiviral activity against HIV1 with RT connection domain G190S/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID32065 | Protection of ATH8 cells against the cytopathic effect of HIV. | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID322394 | Selectivity index, Ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs). |
| AID142328 | Reduced IL-3 dependent colony formation in murine bone marrow progenitor cells at 5uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1483273 | Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID679320 | TP_TRANSPORTER: uptake in OAT1-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID79435 | Concentration required to inhibit uninfected H9 cell growth by 50% | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| Anti-AIDS agents. Part 58: synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues. |
| AID573989 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID600420 | Cytotoxicity against HIV1 infected human C8166-CCR5 cells assessed as decrease in cell viability by cell associated dehydrogenase activity assay | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
| Novel 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2)-curcumin, kojic acid, quercetin, and baicalein conjugates as HIV agents. |
| AID1352315 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID548562 | Antiviral activity against HIV1 71361-1 harboring reverse transcriptase 65R mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID83108 | Concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1. | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
| Structure-activity relationships of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine analogues: effect of substitutions at the C-6 phenyl ring and at the C-5 position on anti-HIV-1 activity. |
| AID746747 | Antiviral activity against HIV1 expressing VSV glycoprotein plasmid infected in human 293T cells treated 15 mins before viral infection measured after 48 hrs by luciferase reporter gene assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design, synthesis, and biological evaluation of new 2'-deoxy-2'-fluoro-4'-triazole cytidine nucleosides as potent antiviral agents. |
| AID571620 | Drug level in HIV-1 infected patient urine at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID19209 | Partition coefficient (logP) | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
| New bicyclam-AZT conjugates: design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor. |
| AID548550 | Cytotoxicity against human MDM up to 1000 nM by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID548565 | Selectivity ratio of EC50 for HIV1 4755-5 harboring reverse transcriptase 41L/44D/67N/69D/118I/210W/215Y/184V mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID666134 | Cytotoxicity against human MOLT3 cells by MTS assay | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
| Truncated phosphonated C-1'-branched N,O-nucleosides: a new class of antiviral agents. |
| AID1653791 | Substrate activity at human mARC1 expressed in Escherichia coli assessed as turnover rates at 3 mM pre-incubated for 3 mins followed by NADH addition and measured after 15 mins by UV-Visible spectroscopy based NADH assay | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| Drug Metabolism by the Mitochondrial Amidoxime Reducing Component (mARC): Rapid Assay and Identification of New Substrates. |
| AID1060631 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID229224 | Cytotoxicity in vero cells. | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID104769 | Concentration required to cause 50% death of uninfected MT-4 cells | 1999 | Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2
| New bicyclam-AZT conjugates: design, synthesis, anti-HIV evaluation, and their interaction with CXCR-4 coreceptor. |
| AID612004 | Antiviral activity against R5 tropic multidrug-resistant HIV1 MM infected PBMC assessed as inhibition of viral p24 antigen expression | 2011 | Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
| Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist. |
| AID81606 | Compound was tested for antiviral activity against matched pairs of HIV-1 sensitive to AZT | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole. |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID235557 | Ratio of the EC50 against HIV-1 infected MT-4 cells and CC50 against mock infected MT-4 cells. | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID308284 | Therapeutic index, IC50 for H9 cells to EC50 for HIV | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Anti-AIDS agents 72. Bioisosteres (7-carbon-DCKs) of the potent anti-HIV lead DCK. |
| AID1141961 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4.3 infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1761009 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID1504698 | Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID1754637 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID45683 | Anti HIV-2 activity in human lymphocyte CEM/0 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID89139 | Anti-HIV-1 activity against syncytial plaque formation at a conc. of 0.0015 uM | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID83541 | Tested for the determination of percentage toxicity at 5 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID1220793 | Ratio of drug level in blood to plasma in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID624640 | Drug glucuronidation reaction catalyzed by human recombinant UGT2B7 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
| UDP-glucuronosyltransferases and clinical drug-drug interactions. |
| AID515989 | Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 6 hrs by p24 antigen based assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
| Anti-AIDS agents 84. Synthesis and anti-human immunodeficiency virus (HIV) activity of 2'-monomethyl-4-methyl- and 1'-thia-4-methyl-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) analogs. |
| AID548828 | Antiviral activity against HIV1 isolate 185 harboring reverse transcriptase T215Y mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1743630 | Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID275065 | Antiviral activity against HIV1 in MAGI-CCR5 cells | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Synthesis, in vitro antiviral evaluation, and stability studies of novel alpha-borano-nucleotide analogues of 9-[2-(phosphonomethoxy)ethyl]adenine and (R)-9-[2-(phosphonomethoxy)propyl]adenine. |
| AID43986 | Concentration of compound required to inhibit HIV-1 induced cytopathogenicity of MSV-induced transformation of C3H/3T3 cells by 50%. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine. |
| AID47300 | Compound was tested for its inhibitory activity against HIV replication in CEM cells. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID81605 | Compound was tested for antiviral activity against matched pairs of HIV-1 resistant to AZT | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole. |
| AID1126509 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID466209 | Cytotoxicity against human C8166 cells by MTT assay | 2010 | Journal of natural products, Feb-26, Volume: 73, Issue:2
| Chemical constituents from the leaves and stems of Schisandra rubriflora. |
| AID152629 | The antiviral fold-increase activity of the compound (AZT-sensitive to AZT-resistant) | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID384987 | Antiviral activity against HIV1 in human C8166 cells assessed as protection against viral-induced cytopathic effect by syncytium reduction assay | 2008 | Journal of natural products, May, Volume: 71, Issue:5
| Periglaucines A-D, anti-HBV and -HIV-1 alkaloids from Pericampylus glaucus. |
| AID519869 | Antiviral activity against HIV1 subtype B-ASM 044 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID548825 | Antiviral activity against HIV1 isolate 166 harboring reverse transcriptase L74V mutant gene obtained as site-directed mutant of NL4-3 by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1565099 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID574186 | Cytotoxicity against human skeletal muscle Myoblast assessed as increase in mitochondrial DNA on day 2 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID540221 | Volume of distribution at steady state in human after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID81964 | Protection of MT-4 lymphocytes by the compound against HIV-1 infectivity in vitro at a concentration of 0.008 ug/mL (0.00003 uM/mL) | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| HIV-1 neutralization and tumor cell proliferation inhibition in vitro by simplified analogues of pyrido[4,3,2-mn]thiazolo[5,4-b]acridine marine alkaloids. |
| AID460291 | Cytotoxicity against GFP expressing human CEM cells assessed as maximal non-toxic concentration after 48 to 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols. |
| AID83416 | Effective concentration required for antiviral activity against HIV strain LAV by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID612668 | Antiviral activity against wild type HIV1 3B infected in human C8166 cells assessed as inhibition of viral-induced cytopathogenicity after 3 days by syncytium formation assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
| Synthesis and biological evaluation of (±)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID341181 | Antiviral activity against X4-HIV1 NL4-3 assessed as inhibition of p24 Gag protein production in human MT4 cells by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID1610041 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 N119 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID581777 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
| AID155280 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain RT-MDR(V106A) in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
| N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. |
| AID1589126 | Selectivity index, ratio of IC50 for cytotoxicity in human NHDF cells to IC50 for cytotoxicity in human U87 cells | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1700255 | Binding affinity to two PBDs of N36 trimer of gp41 in HIV1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral fusion incubated for 48 hrs by Steady-Glo luciferase assay | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
| Bivalent HIV-1 fusion inhibitors based on peptidomimetics. |
| AID393071 | Cytotoxicity against human MT2 cells after 5 days | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors. |
| AID675190 | Therapeutic index, ratio of TC50 for human CEM-SS cells to EC50 for HIV-1 subtype 3B infected in CEM-SS cells | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID1506739 | Antiproliferative activity in human 5637 cells assessed as inhibition of cell growth incubated for 24 hrs by MTT assay | 2017 | MedChemComm, Feb-01, Volume: 8, Issue:2
| Synthesis, antioxidant and antitumoral activities of 5'-arylchalcogeno-3-aminothymidine (ACAT) derivatives. |
| AID618859 | Cytotoxicity against human CEM cells after 6 days by trypan blue exclusion assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides. |
| AID154802 | Antiviral activity against subtype isolate D strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID45035 | Tested for anti-HIV -1 Activity in CEM-SS cell culture | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID1220795 | Plasma clearance in po dosed human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1597908 | Chronic cytotoxicity against cat FL-4 cells assessed as decrease in cell viability measured after 7 days by MTT assay | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID15238 | Percentage of radioactivity in S3 which is the soluble fraction in mouse brain after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID300152 | Antiviral activity against Rotavirus RF in rhesus monkey MA104 cells assessed as inhibition of infectivity following virus attachment after 72 hrs | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Physicochemical determinants of human renal clearance. |
| AID210597 | Therapeutic Index is the average of the IC50 to that of EC50 | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID341182 | Antiviral activity against R5-HIV1MDR/C assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID318738 | Inhibition of HIV1 in sup T1 cells assessed as total reverse transcribed viral DNA at 2 uM by PCR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, May-15, Volume: 104, Issue:20
| Inhibiting HIV-1 integrase by shifting its oligomerization equilibrium. |
| AID46399 | Inhibition of human immunodeficiency virus-2 (HIV-2) induced cytopathicity in CEM cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
| Acyclic nucleotide analogs derived from 8-azapurines: synthesis and antiviral activity. |
| AID417056 | Half life in HIV-infected human at 300 mg, po bid | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID751136 | Cytotoxicity against human C8166 cells after 3 days by MTT assay | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6
| Bioactive dibenzocyclooctadiene lignans from the stems of Schisandra neglecta. |
| AID253093 | Mean phosphorylation rate of 10 uM compound by recombinant human thymidine kinase 1 (cytosolic) expressing wild type L929 tumor cells | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| Synthesis and biological evaluation of neutral and zwitterionic 3-carboranyl thymidine analogues for boron neutron capture therapy. |
| AID45681 | cytotoxic activity in CEM/0 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID257928 | Antiviral activity against HIV1 NL4-3 replication in PBMC at 1 uM | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent. |
| AID222679 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 48 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID155631 | Inhibition of viral RNA in HIVD34-infected PBMC assay on day 4 at concentration of 4 nM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
| AID679673 | TP_TRANSPORTER: uptake in OAT3-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID279927 | Increase in plasma insulin level in cafteria-fed Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1377180 | Antiviral activity against HIV1/VSV-G pseudovirus infected in human A549 cells assessed as downregulation of U5/gag gene expression after 48 hrs by Taqman-based real-time PCR analysis | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID1757986 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID489452 | Antiviral activity against HIV1 bearing VSV glycoprotein infected in human MT2 cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Synthesis and anti-HIV activity of 2'-deoxy-2'-fluoro-4'-C-ethynyl nucleoside analogs. |
| AID1743628 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID563937 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID46250 | Concentration which produces a 50% survival of HIV-1 infected cells relative to uninfected control CEM-SS cells (in vitro anti-HIV activity) | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
| AID45552 | Effective concentration required for antiviral activity against HIV strain IIIB in CEM-SS cells by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID548815 | Antiviral activity against HIV1 isolate 063 harboring reverse transcriptase M41L/D67N/K70R/M184V/L210W/T215Y/K219E mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID226232 | Fold increase of EC50 HIV M184v to that of EC90 HIV-1xxBRU was determined | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID382982 | Ratio of CC50 for Caco-2 cells to IC50 for rotavirus infected human Caco2 cells assessed as neutralization of virus in the solution before attachment | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
| Unsaturated fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-4-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine and N(6)-benzoyl adenine. |
| AID235238 | Therapeutic index was evaluated as ratio of IC50 to that of EC50 | 1998 | Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
| Anti-AIDS agents. 32. Synthesis and anti-HIV activity of betulin derivatives. |
| AID157417 | In vitro Cytotoxic concentration which reduced HIV-1 LAV infected peripheral blood lymphocytes (PBL) by 25 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID1053508 | Ratio of EC50 for AZT-resistant Human immunodeficiency virus 1 to EC50 for wild type Human immunodeficiency virus 1 expressing p24 | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID481808 | Inhibition of Ureaplasma parvum thymidine kinase by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID279918 | Increase in total cholesterol level in lean Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1379962 | Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
| AID154784 | Antiviral activity against subtype isolate D strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID572977 | Ratio of IC50 for HIV1 harboring reverse transcriptase diserine insert between residues 69 and 70 infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID393070 | Antiviral activity against HIV1 3a infected human MT2 cells assessed as inhibition of viral-induced cytopathic effect after 3 days by XTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors. |
| AID1068975 | Antiviral activity against HIV-2 ROD infected in thymidine kinase-deficient human CEM cells | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents. |
| AID154803 | Antiviral activity against subtype isolate E strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID565571 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production at 10 uM after 8 hrs by ELISA | 2009 | Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
| ADS-J1 inhibits human immunodeficiency virus type 1 entry by interacting with the gp41 pocket region and blocking fusion-active gp41 core formation. |
| AID83210 | Compounds were evaluated for anti-RT activity at 13 days of culture; Not determined | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1304408 | Antiviral activity against HIV-1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID1815384 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID42390 | Antiviral activity against HIV-1 (RF strain) in C8166 cells | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1). |
| AID1687685 | Antiviral activity against HIV-2 ROD strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID80086 | Compound was evaluated for the antiviral activity against HCMV; Not determined | 1998 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7
| Synthesis and antiviral activity of novel isodideoxy nucleosides with exocyclic methylene. |
| AID1610034 | Antiviral activity against HIV1 VB59 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID416386 | Cytotoxicity against human MT4 cells by MTS method | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Synthesis and antiviral evaluation of thieno[3,4-d]pyrimidine C-nucleoside analogues of 2',3'-dideoxy- and 2',3'-dideoxy-2',3'-didehydro-adenosine and -inosine. |
| AID1261366 | Cytotoxicity against human PBMC assessed as reduction in cell growth incubated for 5 days by CellTiter 96 AQueous One Solution cell proliferation assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of dihydropyrimidine α,γ-diketobutanoic acid derivatives targeting HIV integrase. |
| AID519882 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID1203614 | Antioxidant activity in Wistar rat brain assessed as inhibition of TBARS formation at 200 uM after 60 mins by spectrophotometric method relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID153143 | Effective concentration required to inhibit the replication of HIV-1 with 2 hr pretreatment of activated PBMCs | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID46990 | 50% effective concentration of compound which is required to protect Thymidine kinase deficient human CEM (CEM/TK-) cells against HIV-2. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID779525 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
| AID83217 | Percent inhibition evaluated for anti-RT activity at 7 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID540219 | Volume of distribution at steady state in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID105132 | Activity against HIV-2 in MT-4 cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID1720641 | Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT to EC50 for inhibition of reverse transcriptase K103N/Y181C double mutant/nucleocapsid protein 7 in HIV1 | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID222692 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 8 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID573978 | Antiretroviral activity against Human immunodeficiency virus 2 EHO infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID105153 | Dose required to achieve 50% protection of MT-4 cells from HIV-1(IIIB) induced cytopathogenicity, determined by MIT method. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
| Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication. |
| AID163315 | Concentration of compound required to inhibit 50% of viral replication of Rauscher-Murine leukemia virus | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia |
| AID154943 | The compound was tested for anti HIV-activity (active) against PBM cell line | 1999 | Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14
| Correlation of anti-HIV activity with structure: use of electrostatic potential and conformational analysis. |
| AID648421 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
| AID235253 | Therapeutic index(TI) was evaluated (IC50/EC50) | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2
| Substituted 7H-pyrido[4,3-c]carbazoles with potent anti-HIV activity. |
| AID46379 | Antiviral activity against site directed resistant isolate HIV-1 L74V in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID244677 | Therapeutic index expressed as ratio of IC50 for 50% growth inhibition to EC50 for 50% replication inhibition | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| Anti-AIDS agents. Part 62: anti-HIV activity of 2'-substituted 4-methyl-3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (4-methyl DCK) analogs. |
| AID105009 | Anti HIV-2 activity in human lymphocyte MT-4 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID685331 | Antiviral activity against HIV-1 3B infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
| AID142326 | Reduced IL-3 dependent colony formation in murine bone marrow progenitor cells at 50 uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID548560 | Antiviral activity against HIV1 1617-1 harboring reverse transcriptase 69K/70G/75I/77L/116Y/151M/184V mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID738314 | Inhibition of HIV1 reverse transcriptase at 50 uM relative to control | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors. |
| AID571622 | Drug level in HIV-1 infected patient urine on day 10 assessed as zidovudine-5-O-glucoronide level by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1572523 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID46370 | Ability to reduce viable cell number on HIV-1-infected CEM cells in mice after intraperitoneal administration | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
| Nucleoside conjugates. 15. Synthesis and biological activity of anti-HIV nucleoside conjugates of ether and thioether phospholipids. |
| AID618793 | Antiviral activity against HIV1 LAV1 infected in phytohemagglutininin-stimulated human PBMC assessed as RT level after 6 days by microdilution plate assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides. |
| AID154942 | Cytotoxic concentration against PBM cells was determined on day 6 | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID104244 | Cytotoxic concentration against MT-2 cells | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi |
| AID1053511 | Antiviral activity against wild type Human immunodeficiency virus 1 expressing p24 infected in human HeLa P4/R5 cells preincubated for 16 hrs prior to virus infection measured after 48 hrs by beta-galactosidase-based single replication cycle assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID89158 | Effective concentration against M184V HIV-1 virus in human peripheral blood mononuclear cells | 2004 | Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
| Synthesis, structure-activity relationships, and drug resistance of beta-d-3'-fluoro-2',3'-unsaturated nucleosides as anti-HIV Agents. |
| AID665547 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID572982 | Cytotoxicity against human MT2 cells after 2 to 4 days by MTT assay | 2009 | Antimicrobial 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. |
| AID619631 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID1761012 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID1152374 | Selectivity index, ratio CC50 for human MT4 cells to EC50 for HIV 1 3B | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1289703 | Inhibition of human TERT protein expression in human MGC803 cells at 3 mmol/L after 48 hrs by Western blotting method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID405412 | Antiviral activity against PERV infected in human 293T cells assessed as inhibition of proximal DNA synthesis after 24 hrs by RT-PCR | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates. |
| AID584080 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K, F227F/L mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sen | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID523353 | Antiviral activity against HIV1 with RT connection domain Y181C mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID689102 | Antiviral activity against HIV1 pseudovirus infected in Jurkat cells coexpressing GFP assessed as viral growth inhibition incubated for 2 to 8 hrs prior to infection measured after 48 hrs by flow cytofluorimetric analysis | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19
| Phosphoramidate derivatives of acyclovir: synthesis and antiviral activity in HIV-1 and HSV-1 models in vitro. |
| AID548302 | Antiviral activity against HIV1 subtype A isolate 92RW009 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1377172 | Antiviral activity against HIV1 isolate LAV0.04 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID1193052 | Cytotoxicity against human PBMC cells assessed as reduction in cell viability after 5 days by Cell Titer 96 Aqueous One Solution cell proliferation assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Molecular docking and antiviral activity of N-substituted benzyl/phenyl-2-(3,4-dimethyl-5,5-dioxidopyrazolo[4,3-c][1,2]benzothiazin-2(4H)-yl)acetamides. |
| AID1357790 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID222493 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 2 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID24309 | Time taken to decrease plasma concentration to half of its initial concentration after ip administration | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
| Nucleoside conjugates. 15. Synthesis and biological activity of anti-HIV nucleoside conjugates of ether and thioether phospholipids. |
| AID1761017 | Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID618794 | Antiviral activity against Hepatitis B virus infected in human HepAD38 assessed as reduction of viral DNA level on day 7 by quantitative-PCR assay analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides. |
| AID658564 | Antiviral activity against multidrug-resistant HIV1 695-RT infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
| AID519886 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID718520 | Cytotoxicity against mock-infected human MT4 cells assessed as decrease in cell viability by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| POMA analyses as new efficient bioinformatics' platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues. |
| AID576194 | Antiviral activity against Human immunodeficiency virus 1 A12 harboring Tyr127His, Asp174Asn and Arg178Lys mutations in nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1763906 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID548322 | Antiviral activity against HIV1 subtype F isolate 93BR029 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID154931 | Anti-HIV activity against human peripheral blood mononuclear (PBM) cell lines infected with XxBRU Pitt (FTC sensitive isolate) | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents. |
| AID540235 | Phospholipidosis-negative literature compound | | | |
| AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16
| FDA-approved drug labeling for the study of drug-induced liver injury. |
| AID1267609 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID1126510 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to IC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID235699 | Selectivity index is defined as CC25(PBLcells) / CC50(PBL cells) | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID47460 | Evaluated for the anticellular activity against CEM cells by dye-exclusion method | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
| Acyclic purine phosphonate analogues as antiviral agents. Synthesis and structure-activity relationships. |
| AID1304403 | Cytotoxicity against mock-infected human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID1391080 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID548561 | Antiviral activity against HIV1 52534-2 harboring reverse transcriptase 41L//74V/210W/215Y/184V/69SSS mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1815390 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 of Anti-HIV activity against HIV-1 IIIB infected in human MT4 | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID588964 | Substrates of transporters of clinical importance in the absorption and disposition of drugs, OAT1 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
| AID152775 | Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain RT-MDR. | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
| Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID106959 | Compound was tested for antiviral activity indicative of 50% cytopathic concentration in virus (HIV-1) infected MT-4 cells. | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Synthesis and biological evaluation of novel D-2'-azido-2',3'-dideoxyarabinofuranosyl-4'-thiopyrimidines and purines. |
| AID1632123 | Cytotoxicity against human KB cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID208555 | In vitro effective concentration against HIV-1 cytopathic effect in T4 cells | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
| Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents. |
| AID154788 | Antiviral activity against subtype isolate F strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID612003 | Antiviral activity against R5 tropic HIV1 Ba-L infected PBMC assessed as inhibition of viral p24 antigen expression | 2011 | Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
| Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist. |
| AID1357796 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID572976 | Ratio of IC50 for HIV1 harboring reverse transcriptase M41L/D67N/K70R/L210W/T215Y/K219Q mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID548319 | Antiviral activity against HIV1 subtype E isolate CMU08 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID153134 | Intracellular of AZT-TP concentrations in LAI/HIV-1 infected PMBCs was determined at a conc of 10 uM) | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID1610037 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 UG070 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID235442 | Selective index as the ratio of CC50 to that of IC50 value against U937 cells. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID346973 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 3B | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Studies on anti-HIV quinolones: new insights on the C-6 position. |
| AID142319 | Reduced GM-CSF dependent colony formation in murine bone marrow progenitor cells at 0.05 uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID234204 | Therapeutic index (Ratio = ID50/ED50). | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID1223448 | Drug metabolism in diabetic human kidney microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID46042 | Inhibitory activity against the HIV-1-induced cytopathic effect in CEM-SS cell line | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID46446 | Concentration which results in 50% survival of uninfected untreated control CEM-SS cells (cytotoxicity of the compound) | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
| AID83397 | Evaluated for minimum inhibitory concentration (MIC) against MT-4 cells of human immunodeficiency virus type-1 (HIV-1) | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Stereospecific synthesis and antiviral properties of different enantiomerically pure carbocyclic 2'-deoxyribonucleoside analogues derived from common chiral pools: (+)-(1R,5S)- and (-)-(1S,5R)-2-oxabicyclo[3.3.0]oct-6-en-3-one. |
| AID89166 | Cytotoxic concentration of compound required to reduce the viability of mock infected MT-4 cells against the HIV-1 (HTLV-IIIB)induced cytopathic effect | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). |
| AID378448 | Therapeutic index, ratio of IC50 for human H9 lymphocytes to EC50 for HIV1 | 2006 | Journal of natural products, Sep, Volume: 69, Issue:9
| Tripfordines A-C, sesquiterpene pyridine alkaloids from Tripterygium wilfordii, and structure anti-HIV activity relationships of Tripterygium alkaloids. |
| AID575951 | Antiviral activity against Human immunodeficiency virus 1 SLKA infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID47658 | Antiviral activity measured in lymphocytic cell line (CEM-C113) infected with HIV-1 cell free supernatants | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
| Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs. |
| AID214559 | In vitro antiviral activity against U937 cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID501756 | Therapeutic index, ratio of IC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
| Conjugates of betulin derivatives with AZT as potent anti-HIV agents. |
| AID1172372 | Cytotoxicity against human KB-3-1 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID1126507 | Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID402091 | Antiviral activity against HIV1 3B in human H9 cells after 4 days by p24 antigen ELISA | 1998 | Journal of natural products, Sep, Volume: 61, Issue:9
| Anti-AIDS agents. 30. Anti-HIV activity of oleanolic acid, pomolic acid, and structurally related triterpenoids. |
| AID214558 | In vitro antiviral activity against U937 cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID103548 | Cytotoxic activity against MCF-7 cell lines. | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Synthesis, in vitro anti-breast cancer activity, and intracellular decomposition of amino acid methyl ester and alkyl amide phosphoramidate monoesters of 3'-azido-3'-deoxythymidine (AZT). |
| AID83082 | Compounds were evaluated for anti-RT activity at 0 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID472671 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected human CEM cells expressing GFP at 4.98 uM measured up to 8 days postinfection by p24 antigen capture ELISA | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Synthesis and anti-HIV activity of alkylated quinoline 2,4-diols. |
| AID473142 | Therapeutic index, IC50 for human MT2 cells to EC50 for HIV1 3B | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors. |
| AID1653806 | Substrate activity at human mARC2 expressed in Escherichia coli assessed as turnover rates at 3 mM pre-incubated for 3 mins followed by NADH addition and measured after 15 mins by LC-MS analysis based assay | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
| Drug Metabolism by the Mitochondrial Amidoxime Reducing Component (mARC): Rapid Assay and Identification of New Substrates. |
| AID1152373 | Cytotoxicity against human MT4 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1743620 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID1320868 | Solubility of the compound | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
| AID79444 | Inhibitory concentration required to inhibit uninfected H9 lymphocytic cell growth by 50% | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2
| Substituted 7H-pyrido[4,3-c]carbazoles with potent anti-HIV activity. |
| AID1292013 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID519875 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID523345 | Antiviral activity against HIV1 with RT connection domain T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID104765 | Cytotoxic concentration required to reduce viability of uninfected cells in MT-4 cell line | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| S-acyl-2-thioethyl phosphoramidate diester derivatives as mononucleotide prodrugs. |
| AID519883 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1174088 | Cytotoxicity against human HepG2 cells | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs. |
| AID558381 | Drug level in HIV-infected pregnant woman amniotic fluid at 300 mg, po BID by LC/MS/MS analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID373386 | Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.13 uM after 24 hrs by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID222687 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 1 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1743634 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID47305 | Cytotoxicity against CEM cells | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents. |
| AID42384 | Effective dose which reduces the HIV-1 yield in C8166 cells by 90% | 1992 | Journal of medicinal chemistry, Mar-06, Volume: 35, Issue:5
| Pyrazole-related nucleosides. Synthesis and antiviral/antitumor activity of some substituted pyrazole and pyrazolo[4,3-d]-1,2,3-triazin-4-one nucleosides. |
| AID1238520 | Inhibition of HIV-1 reverse transcriptase in human Jurkat cells assessed as ratio MTT activity to reverse transcriptase activity with compound/reverse transcriptase activity with DMSO at 10 uM after 72 hrs (Rvb = 0.795 No_unit) | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16
| Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase. |
| AID28964 | Partition coefficient (logP) | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID1357788 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID584616 | Toxicity in human subcutaneous preadipocytes assessed as triacylglyceride droplets at 6 uM after 30 days using oil red O fluorescence staining by conventional fluorescence microscopy | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID584802 | Inhibition of electron transport protein complex 5 in human subcutaneous preadipocytes at 6 uM after 30 to 60 days by photometric analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID584641 | Inhibition of electron transport protein complex 2/3 in human subcutaneous preadipocytes at 6 uM after 30 to 60 days by photometric analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID525105 | Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID45188 | Compound was evaluated for the effect of Order of Addition on Cytoprotection against HIV-1RF at dilution 100, Add at infection | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID1174087 | Cytotoxicity against african green monkey Vero cells | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs. |
| AID155278 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain HTLV IIIB in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
| N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. |
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID1757975 | Antiviral activity against HIV-1 infected in human CEM-SS cells assessed as reduction in viral multiplication by measuring decrease in reverse transcriptase activity incubated for 5 days | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID382980 | Antiviral activity against gastrointestinal rotavirus in human Caco-2 cells assessed as inhibition of infectivity following virus attachment | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
| Unsaturated fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-4-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine and N(6)-benzoyl adenine. |
| AID571623 | Drug level in HIV-1 infected patient urine assessed as zidovudine-5-O-glucoronide level at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID83061 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID152626 | Activity against Lamivudine-resistant virus (HIV-1M184V) in human PBM cells, expressed as EC90 | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance. |
| AID576202 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 3.13 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID671654 | Cytotoxicity against human PBMC after 7 days by XTT assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Oxoquinoline acyclonucleoside phosphonate analogues as a new class of specific inhibitors of human immunodeficiency virus type 1. |
| AID1316343 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID1720638 | Inhibition of nucleocapsid protein 7/reverse transcriptase K103N/Y181C double mutant in HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID573975 | Antiretroviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID105514 | The effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 virus A012D strain | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1077222 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID104432 | In vitro anti viral activity against HIV-1(IIIB) in MT-4 T-lymphoid cell culture by p-24-ELISA assay | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design. |
| AID701105 | Antiviral activity against HIV1 3B infected in MT4 cells | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms. |
| AID1575288 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B infected in human MT4 cells | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1
| 3,4- seco-Norclerodane Diterpenoids from the Roots of Polyalthia laui. |
| AID87480 | Compound was tested for antiviral activity against HSV-1 | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Synthesis and biological evaluation of novel D-2'-azido-2',3'-dideoxyarabinofuranosyl-4'-thiopyrimidines and purines. |
| AID106424 | Content of viable cells at 10e-5 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID392513 | Antiviral activity against HIV1 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks. |
| AID1068976 | Cytotoxicity against human CEM/0 cells | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents. |
| AID1888696 | Antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID573998 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for CHI/1043-resistant Human immunodeficiency virus harboring T66I and Q146K mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID572768 | Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1589127 | Selectivity index, ratio of IC50 for cytotoxicity in human NHDF cells to IC50 for cytotoxicity in human HepG2 cells | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID235014 | In vitro therapeutic index was measured from IC50 to EC50 towards HIV-1 replication in cell growth in H9 lymphocytes | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
| Anti-HIV agents. Part 55: 3'R,4'R-Di-(O)-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP), a novel anti-HIV agent. |
| AID523358 | Antiviral activity against HIV1 with RT connection domain G190A/N348Ib mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID106886 | Tested for the drug concentration required to decrease HIV-1IIIb infected MT-2 cell viability compared to uninfected controls | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID584613 | Toxicity in human subcutaneous preadipocytes assessed as cell death at 6 uM after 30 days using oil red O fluorescence staining by conventional fluorescence microscopy | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1632129 | Selectivity index, ratio of IC50 for HDF to IC50 for human KB cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID152792 | In vitro cytotoxicity in PBM cells. | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
| Enantiomeric synthesis of D- and L-cyclopentenyl nucleosides and their antiviral activity against HIV and West Nile virus. |
| AID89143 | Anti-HIV-1 activity against syncytial plaque formation at a conc. of 0.003 uM | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID105345 | Protection of MT-4 cells against the cytopathic effect of HIV-2 (8 days) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiviral activity of 8-aza analogs of chiral [2-(phosphonomethoxy) propyl]guanines. |
| AID586319 | Antiviral activity against Human T-cell leukemia/lymphoma virus type 1 infected in human PBMC assessed as inhibition of tax/rex gene expression after 3 weeks post infection by quantitative real time RT-PCR | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
| AID210286 | In vitro antiviral activity against T-cells | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID45201 | Compound was evaluated for the effect of Order of Addition on Cytoprotection against HIV-1RF at dilution 333, Pretreat with 100 uM | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID519870 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID222397 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 48 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID56582 | Inhibitory activity against deoxycytidine kinase from L1210 cells | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
| Synthesis and biological activity of various 3'-azido and 3'-amino analogues of 5-substituted pyrimidine deoxyribonucleosides. |
| AID82929 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 26 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1316335 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID154795 | Antiviral activity against SLKA virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID105347 | Tested for in vitro cytopathic effect of HIV for MT-4 cells | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine. |
| AID548308 | Antiviral activity against HIV1 subtype B isolate 96USHIPS7 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID590166 | Antiviral activity against 0.05 MOI Human immunodeficiency virus 1 NL4.3 infected in human CEM cells expressing green fluorescent protein assessed as p24 antigen production measured 7 days post infection by ELISA | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
| Synthesis of 9-substituted derivatives of berberine as anti-HIV agents. |
| AID1443662 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID540218 | Clearance in monkey after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID105165 | Effective concentration required for antiviral activity against T (HTLV-1+)cell line of MT-4 cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID370733 | Therapeutic index, ratio of IC50 for HIV1 3B to TC50 for human C8166 cells | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
| AID452269 | Antiviral activity against HIV1 LAI infected in human PBM cells after 5 days | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus. |
| AID1483285 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase F227L/V106A double mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID261444 | Cytotoxicity against human CEM cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
| Synthesis and anti-HIV activity of D- and L-thietanose nucleosides. |
| AID581774 | Antiviral activity against HIV-1 SF2 infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
| AID1483280 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID1710793 | Antiviral activity against Human immunodeficiency virus 1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 3 to 6 days by light microscopic analysis | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4
| Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1815380 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID1888702 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID681231 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, AZT: 5 uM) in Xenopus laevis oocytes | 2001 | Molecular pharmacology, May, Volume: 59, Issue:5
| Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. |
| AID105155 | Effective concentration against HIV-1 induced cytopathogenicity in MT-4 cells | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
| 2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. |
| AID1223445 | Drug metabolism in diabetic human liver microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID291761 | Cytotoxicity in human C8166 cells | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro. |
| AID72042 | Inhibitory effect of compound on the proliferation of murine mammary carcinoma cells FM3A/0 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID1193109 | Therapeutic index, ratio of CC50 for cat FL-4 cells to EC50 for Feline immunodeficiency virus infected in cat FL-4 cells | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Novel fused tetrathiocines as antivirals that target the nucleocapsid zinc finger containing protein of the feline immunodeficiency virus (FIV) as a model of HIV infection. |
| AID232356 | Ratio of CC50 value that of EC50 value(HIV-2) | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs. |
| AID727265 | Mitochondrial toxicity in human HepG2 cells assessed as lactate dehydrogenase release up to 200 uM | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| 2'-Fluoro-6'-methylene-carbocyclic adenosine phosphoramidate (FMCAP) prodrug: in vitro anti-HBV activity against the lamivudine-entecavir resistant triple mutant and its mechanism of action. |
| AID1265600 | Antiviral activity against HIV-1 NL4-3 infected in MT4 cells assessed as viral replication measured on day 4 post infection by ELISA | 2015 | Journal of natural products, Nov-25, Volume: 78, Issue:11
| Stelleralides D-J and Anti-HIV Daphnane Diterpenes from Stellera chamaejasme. |
| AID46051 | Tested for inhibitory concentration on HIV-I Lai wild type in CEM-SS cell line | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. |
| AID671653 | Antiviral activity against R5-tropic Human immunodeficiency virus 1 Ba-L subtype B infected in human PBMC assessed as inhibition of viral replication after 7 days by ELISA | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| Oxoquinoline acyclonucleoside phosphonate analogues as a new class of specific inhibitors of human immunodeficiency virus type 1. |
| AID106607 | Cytotoxic concentration required to reduce the viability of normal uninfected MT-4 cells by 50% | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
| 5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity. |
| AID382983 | Ratio of CC50 for Caco-2 cells to IC50 for rotavirus infected human Caco2 cells assessed as inhibition of infectivity following virus attachment | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
| Unsaturated fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-4-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine and N(6)-benzoyl adenine. |
| AID106240 | 50% inhibition of HIV replication in MT-4 cells | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| Uncharged AZT and D4T derivatives of phosphonoformic and phosphonoacetic acids as anti-HIV pronucleosides. |
| AID153132 | Conc. required to inhibit HIV-1 replication on PBMCs by 50% | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID211485 | Compounds were evaluated for their potential toxic effect on uninfected PHA-stimulated Vero cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID235439 | Selective index as the ratio of CC50 to that of IC50 value against H9 cells. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID1275548 | Antiviral activity against HIV1 3B expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID563942 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase T165A/M184V mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | | | |
| AID611662 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID619630 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID574189 | Cytotoxicity against human skeletal muscle Myoblast assessed as change in MTCYB mitochondrial RNA level on day 2 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID1457062 | Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y1881C double mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID341185 | Cytotoxicity against human PHA-PBMC cells by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID1652587 | Antiviral activity against HIV2 ROD infected in human TK-deficient CEM/TK(-) cells assessed as inhibition of viral-induced giant cell formation incubated for 4 to 5 days by microscopy | | | |
| AID548579 | Antiviral activity against HIV1 isolate 069 harboring reverse transcriptase D67E/T69SSG/V75M/M184V/L210W/T215Y mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID572784 | Antiviral activity against HIV1 harboring reverse transcriptase D67N/K70R/T215F/K219Q mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID417242 | AUC in HIV-infected human assessed as zidovudine diphosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID397592 | Therapeutic index, ratio of cytotoxicity against human H9 cells to EC50 for HIV1 RF | 2001 | Journal of natural products, Feb, Volume: 64, Issue:2
| Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program. |
| AID519871 | Antiviral activity against 0.01 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1457053 | Antiviral activity against HIV1 NL4-3 infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID79108 | In vitro Cytotoxic concentration which reduced HIV-1 LAV infected H9 cells by 25 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID484742 | Antiviral activity against HIV1 3B infected in C8166 cells assessed as inhibition of syncytia formation | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
| Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro. |
| AID422692 | Ratio of IC50 for HIV1 with reverse transcriptase K70G/M184V mutation to IC50 for wild type HIV1 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
| Novel drug resistance pattern associated with the mutations K70G and M184V in human immunodeficiency virus type 1 reverse transcriptase. |
| AID44591 | Effective concentration required for antiviral activity against BxT cell line of 174xCEM cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID1456307 | Inhibition of HIV-1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
| AID44830 | Inhibitory effects on HIV-1 induced syncytium formation in C8166 cells | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
| A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships. |
| AID548572 | Antiviral activity against HIV1 isolate 057 expressing wild type reverse transcriptase gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID607807 | Antiviral activity against 0.06 MOI Human immunodeficiency virus 1 IIIB A17 harboring reverse transcriptase K103N and Y181C double mutant infected in C8166 cells assessed as reduction in virus-induced cytopathic effect after 3 days by syncytium reduction | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1193053 | Cytotoxicity against human CEM cells assessed as reduction in cell viability after 5 days by Cell Titer 96 Aqueous One Solution cell proliferation assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Molecular docking and antiviral activity of N-substituted benzyl/phenyl-2-(3,4-dimethyl-5,5-dioxidopyrazolo[4,3-c][1,2]benzothiazin-2(4H)-yl)acetamides. |
| AID569229 | Inhibition of HIV1 reverse transcriptase | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
| Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5. |
| AID152655 | In vitro cytotoxicity against human peripheral blood mononuclear (PBM) cells | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
| Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID523349 | Antiviral activity against HIV1 with RT connection domain K103N mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID206707 | Inhibitory concentration against Staphylococcus aureus; Not tested | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| New manzamine alkaloids from an Indo-Pacific sponge. Pharmacokinetics, oral availability, and the significant activity of several manzamines against HIV-I, AIDS opportunistic infections, and inflammatory diseases. |
| AID646700 | Antiviral activity against Hepatitis C virus infected in human HuH7 cells assessed as decrease in viral RNA level after 96 hrs by RT-PCR | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and antiviral activity of 2'-deoxy-2'-fluoro-2'-C-methyl-7-deazapurine nucleosides, their phosphoramidate prodrugs and 5'-triphosphates. |
| AID1172370 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID154792 | Antiviral activity against subtype isolate O strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID290121 | Antiviral activity against HSV2 in CCL81 cells | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiviral activity of C-fluoro-branched cyclopropyl nucleosides. |
| AID1754644 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID104415 | Concentration of the drug resulting in 50% reduction of the viral cytopathic effect against HIV-1 replication in MT-2 cells. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID1407646 | Antiviral activity against Human immunodeficiency virus 1 NL4-3 infected in human CEM-GFP cells after 7 days by p24 ELISA | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
| AID548813 | Antiviral activity against HIV1 isolate 060 harboring reverse transcriptase M41L/D67N/K70R/L210W/T215Y/K219E mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID574198 | Cytotoxicity against human skeletal muscle Myotube assessed as change in POLG mitochondrial RNA level on day 5 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID1377173 | Antiviral activity against HIV1 isolate 89.6 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID571595 | Cmax in HIV-1 infected patient at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1446820 | Antiviral activity against HIV1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID1546660 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells to | | | |
| AID42622 | Compound was tested for Anti-HIV activity by plaque reduction assay with wild type HIV-1LAI virus in HT4-6C human CD4+ lymphocytes | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Synthesis and in vitro activity of long-chain 5'-O-[(alkoxycarbonyl)phosphinyl]-3'-azido-3'-deoxythymidines against wild-type and AZT- and foscarnet-resistant strains of HIV-1. |
| AID42620 | Compound was tested for Anti-HIV activity by plaque reduction assay with A018-post virus in HT4-6C human CD4+ lymphocytes | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Synthesis and in vitro activity of long-chain 5'-O-[(alkoxycarbonyl)phosphinyl]-3'-azido-3'-deoxythymidines against wild-type and AZT- and foscarnet-resistant strains of HIV-1. |
| AID83222 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID246192 | Effective concentration to inhibit HIV-1 activity in human peripheral blood mononuclear cells | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Synthesis, antiviral activity, and mechanism of drug resistance of D- and L-2',3'-didehydro-2',3'-dideoxy-2'-fluorocarbocyclic nucleosides. |
| AID548812 | Antiviral activity against HIV1 isolate 058 harboring reverse transcriptase M41L/D67N/K70R/L210W/T215F/K219Q mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID218531 | Compound was evaluated for its toxicity by Calorimetric assay in vero cells | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID235795 | Selectivity index was measured as the ratio of CC50(HIV-1) to that of EC50(HIV-1) | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
| Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication. |
| AID341997 | Antimicrobial activity against Streptococcus sp. 07706-1 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID153147 | Concentration required to kill 100% of unactivated PBMCs | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID406050 | Oral bioavailability in rhesus monkey at 60 mg/kg | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Pharmacokinetics of the anti-human immunodeficiency virus agent 1-(beta-D-dioxolane)thymine in rhesus monkeys. |
| AID572985 | Cytotoxicity against human HeLa P4/R5 cells after 2 to 4 hrs by MTT assay | 2009 | Antimicrobial 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. |
| AID583436 | Cytotoxicity against human HepG2 cells assessed as reduction in viable cells at 50 uM after 15 days by trypan blue dye exclusion assay relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID85885 | Antiviral activity against Herpes simplex virus type-1 | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID45041 | Cytotoxic concentration required to reduce viability of uninfected cells in CEM-SS cell line | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| S-acyl-2-thioethyl phosphoramidate diester derivatives as mononucleotide prodrugs. |
| AID373382 | Stability in human CEM cells assessed as total intracellular radioactive phosphorylated metabolite remaining at 2 uM incubated for 24 hrs measured after 24 hrs of compound removal assessed per 10'6 cells relative to 0 hrs after compound removal | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID152616 | In vitro anti-HIV activity was determined in peripheral blood mononuclear cells. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine. |
| AID675188 | Antiviral activity against HIV-1 subtype 3B infected in CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID1483272 | Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID376300 | Cytotoxicity against human C8166 cells by MTT method | 2006 | Journal of natural products, Apr, Volume: 69, Issue:4
| Nortriterpenoids from Schisandra lancifolia. |
| AID71777 | Concentration that reduces Friend murine leukemia virus titer by 50% | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Unsaturated and carbocyclic nucleoside analogues: synthesis, antitumor, and antiviral activity. |
| AID583456 | Cytotoxicity against human HepG2 cells assessed as inhibition of mitochondrial respiratory chain complex I activity at 50 uM after 15 days relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID573977 | Antiretroviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID1174084 | Antiviral activity against Hepatitis B virus | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs. |
| AID142331 | Thymidine Influx Inhibition constant for the compound in fresh Murine Erythrocytes | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID405341 | Toxicity against human H9c2 cells assessed as elevation of lactate levels at 10 uM after 6 days by NAD+ reduction assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID698306 | Antiviral activity against HIV1 containing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID104760 | Dose required to reduce the viability of mock-infected cells by 50% | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID685332 | Antiviral activity against HIV-2 ROD infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
| AID85887 | Antiviral activity against HSV-1 (herpes simplex virus); Not determined | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
| Nucleosides and nucleotides. 183. Synthesis of 4'alpha-branched thymidines as a new type of antiviral agent. |
| AID548816 | Antiviral activity against HIV1 isolate 066 harboring reverse transcriptase 184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1757985 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID155102 | Effective concentration required to inhibit 50% of HIV-1 in peripheral blood mononuclear cells (PBMC) | 1997 | Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21
| Probing the mechanism of action and decomposition of amino acid phosphomonoester amidates of antiviral nucleoside prodrugs. |
| AID87665 | Compound was tested for antiviral activity against HSV-2 | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Synthesis and biological evaluation of novel D-2'-azido-2',3'-dideoxyarabinofuranosyl-4'-thiopyrimidines and purines. |
| AID155289 | Compound was evaluated for inhibition of p24 production in HIV infected peripheral blood mononuclear cells | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
| 5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series. |
| AID15240 | Percentage of total protein recovered in P2 subregion in mouse brain that contains myelin fragments, synaptosomes (pinched-nerve endings), and mitochondria after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID423783 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID548305 | Antiviral activity against HIV1 subtype B isolate Ba-L infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID556525 | Antiviral activity against Human immunodeficiency virus 1 clone 38086 harboring K49R, V60I, I135V, Q145M, Q174H, G196E, Q207E, R211K, V245K mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
| AID666973 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
| AID104235 | Therapeutic index is the ratio between IC50/EC50 of HIV-I A17 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID516491 | Cytotoxicity against human MT2 cells by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist. |
| AID557273 | Antiviral activity against HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID548809 | Antiviral activity against HIV1 isolate 215 harboring reverse transcriptase D67N/K70E mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID81946 | In vitro toxicity to C8166 (human CD4) cells. | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
| 6-Aminoquinolones as new potential anti-HIV agents. |
| AID1060630 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID1357804 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID482690 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as time-of-addition prolongation at 0.5 ug/ml after 31 hrs post infection by ELISA | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
| "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
| AID1193054 | Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability after 5 days by Cell Titer 96 Aqueous One Solution cell proliferation assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Molecular docking and antiviral activity of N-substituted benzyl/phenyl-2-(3,4-dimethyl-5,5-dioxidopyrazolo[4,3-c][1,2]benzothiazin-2(4H)-yl)acetamides. |
| AID423279 | Antiviral activity against wild type HIV2 CDC310319 infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro. |
| AID1888705 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID373569 | Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.02 uM after 24 hrs by luciferase assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID104298 | The compound was tested for effective concentration required to protect MT-4 cells against the cytopathicity of HIV-2(ROD) | 2002 | Bioorganic & medicinal chemistry letters, Mar-11, Volume: 12, Issue:5
| New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation. |
| AID332929 | Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay | 1994 | Journal of natural products, Jan, Volume: 57, Issue:1
| Anti-AIDS agents, 10. Acacetin-7-O-beta-D-galactopyranoside, an anti-HIV principle from Chrysanthemum morifolium and a structure-activity correlation with some related flavonoids. |
| AID26769 | Partition coefficient (logP) | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5
| Potential anti-AIDS drugs. Lipophilic, adenosine deaminase-activated prodrugs. |
| AID82923 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 22 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID346970 | Antiviral activity against HIV 3B in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Studies on anti-HIV quinolones: new insights on the C-6 position. |
| AID1504694 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID363850 | Cytotoxicity against human Caco-2 cells after 72 hrs | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
| Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities. |
| AID105753 | Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 125 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID154774 | Antiviral activity against WEJO virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID246047 | Effective concentration against HIV-I RTMDR1 in MT-4 cells | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Anti-AIDS agents. 60. Substituted 3'R,4'R-di-O-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) analogues as potent anti-HIV agents. |
| AID576148 | Antiviral activity against simian immunodeficiency virus 69R infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID152630 | The compound was tested for antiviral activity against AZT resistant strain 10 HIV in PBM cells. | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID330485 | Antiviral activity against HIV1 3B infected in MT4 cells by MTT | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID563940 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S/T165A mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID46940 | Therapeutic index is the ratio between IC50/EC50 of HIV-I RFII strain in CEM cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID693595 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 A17 harbouring RT K103N/Y181C mutant infected in human C8166 cells | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors. |
| AID157568 | Antiviral activity against human immunodeficiency virus type-1 (HIV-1) in PBM cells | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID7783 | Unbound fraction (plasma) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID47625 | The 90% inhibitory concentration expresses cellular toxicity measured against normal human granulocyte-monocyte cells | 1989 | Journal 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. |
| AID214060 | Effective concentration required for antiviral activity against Macrophage cell line of U937 cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID283694 | Selectivity index, ratio of CC50 for C8166 cells to IC50 for HIV1 infected C8166 cells | 2007 | Journal of natural products, Apr, Volume: 70, Issue:4
| Bioactive lignans from Peperomia heyneana. |
| AID1446818 | Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID282742 | Cytotoxicity against C8166 cells by MTT assay | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
| AID342004 | Antibacterial activity against deoxyribonucleotide kinase-deficient Escherichia coli KY895 expressing Staphylococcus aureus recombinant thymidine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID576146 | Antiviral activity against Human immunodeficiency virus 2 CDC 310342 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID472673 | Therapeutic index, ratio of CC50 for human CEM cells expressing GFP to IC50 for Human immunodeficiency virus 1 NL4.3 | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Synthesis and anti-HIV activity of alkylated quinoline 2,4-diols. |
| AID523484 | Antiviral activity against HIV1 with RT connection domain L100I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID1141959 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1356067 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by cytoTox-Glo reagent based assay | 2018 | Journal of natural products, 07-27, Volume: 81, Issue:7
| Kleinhospitine E and Cycloartane Triterpenoids from Kleinhovia hospita. |
| AID571621 | Drug level in HIV-1 infected patient urine at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1543134 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV NL4-3 infected in human MT4 cells | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6
| Potent Anti-HIV Ingenane Diterpenoids from Euphorbia ebracteolata. |
| AID576389 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 6.25 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID676996 | Cytotoxicity against human HeLa cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
| Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID83250 | Effective concentration required for antiviral activity against HIV strain MS (HIV-2) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID1754645 | Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID1815382 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID232315 | EC50 of HIV-2 in CEM/TK versus EC50 of HIV-2 in CEM/0 | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID548556 | Antiviral activity against HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID734116 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathicity treated post-viral infection measured after 5 days by Cell-Titer Glo assay | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| 9-[2-(R)-(Phosphonomethoxy)propyl]-2,6-diaminopurine (R)-PMPDAP and its prodrugs: optimized preparation, including identification of by-products formed, and antiviral evaluation in vitro. |
| AID398467 | Inhibition of HIV2 reverse transcriptase p66/p51 | 1995 | Journal of natural products, Jul, Volume: 58, Issue:7
| Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase. |
| AID103003 | Effective concentration required for antiviral activity against M cell line of macrophage cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID1200845 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
| AID1197833 | Resistance index, ratio of EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant to EC50 for wild type HIV1 3B | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
| AID154796 | Antiviral activity against TEKI virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID1572521 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | | | |
| AID104757 | Compound dose required to reduce the viability of mock-infected cells by 50% | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. |
| AID1545930 | Antiproliferative activity against human KB cells by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | 1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships. |
| AID573987 | Antiviral activity against Protease inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID154805 | Antiviral activity against subtype isolate G strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID83232 | Compounds were evaluated for anti-RT activity by MTT dose and %protection was reported at 7 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID481807 | Ratio of Vmax to Km for human TK1 relative to ATP | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID644283 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
| Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins. |
| AID665832 | Antiviral activity against HIV infected in human TZM-bl cells at 10 uM after 48 hrs by luciferase-based reporter gene assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Design, synthesis and antiviral activity of novel quinazolinones. |
| AID707985 | Cytotoxicity against human C8166 cells after 3 days by MTT assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of inhibitors to block interactions of HIV-1 integrase with human LEDGF/p75 via structure-based virtual screening and bioassays. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID83056 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1357783 | Antiviral activity against wild-type HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID549089 | Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID279933 | Decrease in fatty acid synthase activity in lean Wistar rat inguinal adipose tissue assessed at 70 mg/kg/day by DNA quantification assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID576157 | Cytotoxicity against human H9 cells by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID45989 | Cytotoxic concentration which is required to reduce human CEM cell viability by 50%. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID1483275 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID267855 | Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
| AID586325 | Cytotoxicity against human MOLT3 cells after 24 hrs by MTS assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
| AID676999 | Antiviral activity against HIV1 NL43 infected din human MT4 cells pre-incubated in presence of compound for 48 hrs followed by TZM cells infection with compound treated virus supernatant by X-gal staining based microscopy | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
| Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID1815377 | Anti-HIV activity against HIV-1 IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID1460942 | Antiviral activity against HIV-1 NL4-3 harboring reverse transcriptase E138A mutant infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID82925 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 22 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID125177 | In vitro inhibitory activity against Moloney murine leukemia virus (M-MULV) replication, a mammalian T-lymphotropic retrovirus | 1987 | Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
| Synthesis and antiviral activity of various 3'-azido, 3'-amino, 2',3'-unsaturated, and 2',3'-dideoxy analogues of pyrimidine deoxyribonucleosides against retroviruses. |
| AID1191403 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID357962 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 of HIV1 3B | 2001 | Journal of natural products, Oct, Volume: 64, Issue:10
| Anti-AIDS agents. 48.(1) Anti-HIV activity of moronic acid derivatives and the new melliferone-related triterpenoid isolated from Brazilian propolis. |
| AID439728 | Antiviral activity against HIV2 KR X3 infected in human TZM-b1 cells assessed as reduction in luciferase activity after 2 days by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. |
| AID45012 | Concentration that reduced by 50% the HIV induced CPE (cytopathic effect) on day 22. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID42398 | Inhibition of p24 antigen formation in infected C8166-cells | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. |
| AID83213 | Compounds were evaluated for anti-RT activity by MTT dose and % cell / viability was reported at 13 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID287874 | Selectivity index, Ratio of CC50 for human Caco-2 cells to IC50 for rotavirus RF infected human Caco2 cells after viral attachment | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9
| An efficient synthesis of 3-fluoro-5-thio-xylofuranosyl nucleosides of thymine, uracil, and 5-fluorouracil as potential antitumor or/and antiviral agents. |
| AID780328 | Cytotoxicity against human PBMC | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
| Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors. |
| AID105582 | Inhibitory activity against HIV-1 replication in MT-4 cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. |
| AID1352321 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103 N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID644281 | Antiviral activity against R5 tropic HIV1 JR-CSF in PM1/CCR5 cells assessed as protection from virus-induced cytopathogenicity measuring capsid p24 level after 5 days by ELISA | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
| Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins. |
| AID574197 | Cytotoxicity against human skeletal muscle Myoblast assessed as change in Tfam mitochondrial RNA level on day 5 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID232754 | Selectivity index is the ratio of IC50 value to that of EC50 value | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine. |
| AID460292 | Antiviral activity against HIV1 NL4-3 infected in GFP expressing human CEM cells assessed as inhibition of viral p24 antigen production at non-toxic concentration after 7 days postinfection by ELISA | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols. |
| AID47462 | In vitro antiviral test was performed on HIV(LAV strain) infected CEM cells | 1989 | Journal 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. |
| AID423278 | Antiviral activity against recombinant HIV2 ROD carrying HIV2 UC2 reverse transcriptase infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro. |
| AID584803 | Inhibition of citrate synthase in human subcutaneous preadipocytes at 6 uM after 30 to 60 days by photometric analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1316341 | Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID89135 | Anti-HIV-1 activity against syncytial plaque formation at a conc. of 0.0003 uM | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID1357800 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID104594 | Tested for cytotoxic concentration in MT-4 cell culture | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID341995 | Antimicrobial activity against Escherichia coli ATCC 25922 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID576145 | Antiviral activity against Human immunodeficiency virus 2 CDC 310319 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID15241 | Percentage of total protein recovered in P3 subregion in mouse brain that contains microsomal fraction after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID1377174 | Antiviral activity against NRTI-resistant HIV1 isolate 1617-1 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID369080 | Cytotoxicity against human CEM cells after 3 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID16366 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into cerebellum | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID210869 | Inhibitory activity against thymidine kinase (TK) from L1210 cells | 1983 | Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
| Synthesis and biological activity of various 3'-azido and 3'-amino analogues of 5-substituted pyrimidine deoxyribonucleosides. |
| AID542934 | Antiproliferative activity against mouse 3T3-F442A cells assessed as [3H]thymidine incorporation at 1 uM | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1884225 | Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID666972 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
| AID519967 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells by phenosense assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID104596 | The concentration required to cause a 50% inhibition of cell proliferation was determined in MT-4 cell culture. | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Carbocyclic dinucleoside polyphosphonates: interaction with HIV reverse transcriptase and antiviral activity. |
| AID542938 | Antiproliferative activity against mouse 3T3-F442A cells assessed as [3H]thymidine incorporation at 0.1 uM | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID334753 | Antiviral activity against Feline leukemia virus infected in cat CRFK cells assessed as inhibition of viral replication after 7 days by ELISA | 1992 | Journal of natural products, Apr, Volume: 55, Issue:4
| Fistularin 3 and 11-ketofistularin 3. Feline leukemia virus active bromotyrosine metabolites from the marine sponge Aplysina archeri. |
| AID1053514 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID153135 | Concentration required to kill 50% of activated PBMCs | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID405344 | Toxicity against human H9c2 cells assessed as increase in mitochondrial superoxide production at 50 uM by flow cytometry | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID46198 | Inhibitory effect against HIV-2 replication in CEM /TK-(thymidine kinase deficient) cells. | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
| Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase. |
| AID1203615 | Antioxidant activity assessed as thiol peroxidase-like activity assessed as concentration required to oxidize 50% of benzenethiol during reduction of hydrogen peroxide measured for 180 secs by UV spectroscopic analysis | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID106965 | Concentration required to achieve 50% protection of MT-4 cells against cytopathic effect of HIV-1 | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
| A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID47450 | compound tested for inhibitory activity by plaque reduction assay against HIV-1 in CEM cells | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Synthesis and antiviral activity of novel acyclic nucleosides: discovery of a cyclopropyl nucleoside with potent inhibitory activity against herpesviruses. |
| AID154800 | Antiviral activity against subtype isolate B strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID563936 | Antiviral activity against wild-type HIV1 pNL4-3 infected in TZM-bl cells by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID1636357 | Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID104416 | Concentration of the drug resulting in 50% growth inhibition of normal, uninfected cells against HIV-1 replication in MT-2 cells. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID1884222 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID548539 | Antiviral activity against HIV1 group O isolate BCF03 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID607810 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for wild type HIV1 IIIB infected in C8166 cells | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID591001 | Antiviral activity against HIV1 Env-pseudovirus infected in human Jurkat E6-1 cells after 2 days by luciferase assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
| Asymmetric total synthesis of (+)- and (-)-clusianone and (+)- and (-)-clusianone methyl enol ether via ACC alkylation and evaluation of their anti-HIV activity. |
| AID163316 | Concentration of compound required to inhibit 50% of host cell replication of Rauscher-Murine leukemia virus | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia |
| AID1888695 | Antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID1267617 | Inhibition of NCp7 of HIV1 3B persistently infected in HUT78 cells assessed as accumulation of unprocessed Gag polyprotein after 43 hrs by Western blot analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID680202 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.05 uM, AZT: 1000 uM) in OAT4-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID1223466 | Drug metabolism in non-diabetic human liver microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID157416 | In vitro Cytotoxic concentration which destroyed HIV-1 LAV infected peripheral blood lymphocytes (PBL) completely | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID342010 | Inhibition of Staphylococcus aureus CCM 885 recombinant thymidine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID86697 | The compound was tested in vitro for anticancer activity against HepG2 cells; Not determined | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID154780 | Antiviral activity against subtype isolate B strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID341187 | Drug level in human CD4+CEM cells assessed as increase in 3'-azido-2',3'-dideoxythymidine triphosphate level at 0.1 uM after 6 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID1221982 | Fraction absorbed in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID493724 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis of highly functionalized 2,4-diaminoquinazolines as anticancer and anti-HIV agents. |
| AID665271 | Antiviral activity against HIV1 3B harboring wild type RT infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID735333 | Cytotoxicity against human 1A2 cells assessed as inhibition of metabolic activity by XTT assay | 2013 | Journal of natural products, Apr-26, Volume: 76, Issue:4
| Cytotoxic, antitopoisomerase IIα, and anti-HIV-1 activities of triterpenoids isolated from leaves and twigs of Gardenia carinata. |
| AID757626 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1157593 | Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID21236 | Partition coefficient for 1-octanol/water was evaluated | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID569565 | Cytotoxicity against human C1866 cells | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
| Compounds from Kadsura angustifolia with anti-HIV activity. |
| AID154960 | Antiviral activity against HIV I strain (LAV) in human peripheral blood mononuclear (PBM) cells; Range is 0.002 - 0.009 | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
| Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells. |
| AID1561717 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenesulfonamide assessed as protection ag | | | |
| AID576382 | Antiviral activity against Human immunodeficiency virus 1 3B infected in AA5 cells infected with 0.78 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID624606 | Specific activity of expressed human recombinant UGT1A1 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID747602 | Antiviral activity against Hepatitis C virus infected in human HuH7 cells | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors. |
| AID83428 | Effective concentration required for antiviral activity against HIV strain WOME (syncytia inducing) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID576203 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 3.13 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID232738 | Selectivity index expressed as ratio of IC50 (CEM-C113) to EC50 from RT assay | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
| Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs. |
| AID557277 | Ratio of EC50 for HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID592681 | Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
| QSAR-based permeability model for drug-like compounds. |
| AID235503 | Selectivity index calculated as the ratio between CC50 and EC50 | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. |
| AID83223 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID19628 | Partition coefficient (logP) | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID46395 | Inhibition of human immunodeficiency virus-1 (HIV-1) induced cytopathicity in CEM cells | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20
| Acyclic nucleotide analogs derived from 8-azapurines: synthesis and antiviral activity. |
| AID354616 | Therapeutic index, ratio of IC50 for mock-infected human H9 cells to EC50 for HIV1 3B | 1996 | Journal of natural products, Nov, Volume: 59, Issue:11
| Two new lignans, interiotherins A and B, as anti-HIV principles from Kadsura interior. |
| AID235684 | Selectivity Index measured as the ratio of EC50(CEM-SS) to that of CC50(CEM-SS). | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID257169 | Antiviral activity against HIV1 Y188L mutant strain infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
| AID1077217 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-2 ROD infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID1565095 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID1161592 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral entry compound treated at 200 uM at 6 hrs post infection measured 3 to 4 days post infection by time-of-addition assay | 2014 | Journal of medicinal chemistry, Sep-11, Volume: 57, Issue:17
| Conjugation of a nonspecific antiviral sapogenin with a specific HIV fusion inhibitor: a promising strategy for discovering new antiviral therapeutics. |
| AID83080 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 7 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID423782 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID587744 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID104940 | The cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% on HIV-1 virus LAV-2ROD strain | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1156487 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
| AID1457057 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID232050 | Selectivity index expressed as the ratio of CC50/ EC50 | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
| 2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. |
| AID576378 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 50 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID586313 | Antiviral activity against Human T-cell leukemia/lymphoma virus type 1 infected in human PBMC assessed as inhibition of tax/rex gene expression at 0.27 ug/ml after 3 weeks post infection by quantitative real time RT-PCR | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
| AID287871 | Antiviral activity against rotavirus RF in human Caco-2 cells after neutralization of virus in solution pre-incubated with compound for 12 hrs before infection | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9
| An efficient synthesis of 3-fluoro-5-thio-xylofuranosyl nucleosides of thymine, uracil, and 5-fluorouracil as potential antitumor or/and antiviral agents. |
| AID1055509 | Cytotoxicity against human CEM cells | 2013 | European journal of medicinal chemistry, , Volume: 70 | Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides. |
| AID575959 | Antiviral activity against Human immunodeficiency virus 1 subtype E CMU02 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID548568 | Selectivity ratio of EC50 for HIV1 52534-2 harboring reverse transcriptase 41L//74V/210W/215Y/184V/69SSS mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID45038 | Antiviral activity in CEM-SS cell line infected with HIV-1 and cytotoxic concentration required to reduce the viability of uninfected cells by 50% | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID104597 | Tested for anti-HIV -1 Activity in MT-4 cell culture | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID525114 | Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID515879 | Antimalarial activity against Plasmodium falciparum 3D7 at 100 uM by SYBR green assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
| Potential application of thymidylate kinase in nucleoside analogue activation in Plasmodium falciparum. |
| AID619513 | Antiviral activity against HIV1 infected in human CEM-T4 cells assessed as reduction in viral protein p24 production preincubated for 24 hrs measured after 8 days by MTT assay | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
| Aryl H-phosphonates 17: (N-aryl)phosphoramidates of pyrimidine nucleoside analogues and their synthesis, selected properties, and anti-HIV activity. |
| AID373354 | Drug metabolism in human CEM cells assessed as radioactive 2', 3'-didehydro-3'-deoxy-4'-ethynylthymidine monophosphate accumulation at 2 uM after 12 hrs assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID523480 | Antiviral activity against HIV1 with RT connection domain G190S/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID282743 | Inhibition of HIV1-3B replication in C8166 cells | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
| AID46382 | Antiviral activity against site directed resistant isolate HIV-1 Y181C in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID152661 | Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain HTLV IIIB wild type. | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
| Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. |
| AID1352316 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID1504700 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID1391087 | Antiviral activity against HIV1 harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID46589 | Inhibitory concentration against HIV-1 infected CEM cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID539770 | Antiviral activity against Human immunodeficiency virus 1 infected in human CEM-SS cells assessed as virus induced cytopathic effects | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
| 1-Benzyl derivatives of 5-(arylamino)uracils as anti-HIV-1 and anti-EBV agents. |
| AID45033 | Tested for cytotoxic concentration in CEM-SS cell culture | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID341369 | Antiviral activity against HIV1 NL4-3 replication in human MT4 cells at 0.01 uM pretreated 48 hrs before infection assessed as protection at 1 uM by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID619636 | Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID611661 | Cytotoxicity against human C8166 cells by MTT colorimetric assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID42385 | Pprotection of C8166 cells against the cytopathic effect of HIV isolate RF | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
| 1-(3-cyano-2,3-dideoxy-beta-D-erythro-pentofuranosyl)thymine (cyanothymidine): synthesis and antiviral evaluation against human immunodeficiency virus. |
| AID104943 | 50% inhibition of MT-4 cell proliferation. | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| Uncharged AZT and D4T derivatives of phosphonoformic and phosphonoacetic acids as anti-HIV pronucleosides. |
| AID142323 | Reduced GM-CSF dependent colony formation in murine bone marrow progenitor cells at 5uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID548586 | Antiviral activity against HIV1 isolate 166 harboring reverse transcriptase L74V mutant gene obtained as site-directed mutant of NL4-3 by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID604026 | Unbound CSF to plasma concentration ratio in human | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID666132 | Antiviral activity against HIV1 infected in CEM cells after 72 hrs by GFP reporter gene assay | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
| Truncated phosphonated C-1'-branched N,O-nucleosides: a new class of antiviral agents. |
| AID106976 | Effective concentration achieving 50% protection of MT-4 cells against the cytopathic effect of HIV-1 | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
| 5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity. |
| AID664469 | Antiviral activity against wild type HIV1 clade B 94US3393IN clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infecti | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID154797 | Antiviral activity against WEJO virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID289145 | Antiviral activity against HIV1 with reverse transcriptase K65R mutation assessed as reduction of potency relative to wild type | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs. |
| AID1761018 | Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID106901 | Effective concentration required for antiviral activity against HIV strain IIIB in MT-2 cells by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID106594 | Concentration required to cause 50% death of uninfected MT-4 cells (expressed in AZT equivalent) | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities. |
| AID197924 | Concentration required to inhibit HIV reverse transcriptase | 1992 | Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
| 3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine. |
| AID1377176 | Antiviral activity against HIV1 isolate LAV infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6
| Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
| AID1157594 | Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID548584 | Antiviral activity against HIV1 isolate 160 harboring reverse transcriptase S68G/V75(I/T)/F77L/Y115F/F116Y /Q151M mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID153102 | Cytotoxic concentration against PBMC cells | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi |
| AID106037 | Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
| Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin- 2(1H)-one (TIBO) derivatives. |
| AID154811 | Anti-HIV activity against human peripheral blood mononuclear (PBM) cell lines infected with M184V Pitt (FTC resistant isolate) | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents. |
| AID1068980 | Antiviral activity against HIV-1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents. |
| AID1720640 | Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT to EC50 for inhibition of reverse transcriptase/nucleocapsid protein 7 in wild type HIV1 3B infected in | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID104785 | Cytotoxic concentration based on the reduction of viability of mock-infected cells | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID604021 | Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID1743622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID1289705 | Inhibition of human TERT-regulated Wnt/beta-catenin signalling in human MGC803 cells assessed as decrease in cyclin D1 protein expression at 3 mmol/L after 48 hrs by Western blotting method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID519884 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID572973 | Ratio of IC50 for HIV1 harboring reverse transcriptase M41L/L210W/T215Y mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID78752 | Cytotoxic concentration against HIV-1 infected H9 cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID105125 | Compound was evaluated for its inhibitory effect on the replication of HIV-1(IIIB) in MT-4 cells | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Synthesis and biological evaluation of thymine nucleosides fused with 3',4'-tetrahydrofuran ring. |
| AID82933 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 7 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID222677 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 24 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID23366 | Hydrolysis half life in phosphate buffer at the specified pH; Not available | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID1720086 | Cytotoxicity against Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry, 06-01, Volume: 28, Issue:11
| Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment. |
| AID341368 | Antiviral activity against HIV1 NL4-3 replication in human MT4 cells at 0.01 uM pretreated 24 hrs before infection assessed as protection at 1 uM by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID584611 | Toxicity in human subcutaneous preadipocytes assessed as decrease of insulin-sensitizing adipokine expression at 6 uM after 30 days by RT-PCR analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1203623 | Cytotoxicity against human 5637 cells assessed as growth inhibition after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID1720639 | Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID269764 | Antiviral activity against HIV1 NL4-3 | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
| Azadideoxyadenosine: synthesis, enzymology, and anti-HIV activity. |
| AID1157581 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID235794 | Selectivity index was determined in CEM-SS cells | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | | | |
| AID1228736 | Antiviral activity against HIV2-ROD infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5
| Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID1884228 | Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID104311 | Effective dose required for 50% inhibition of HIV-1 antigen production in MT-4 cultures | 1998 | Journal of medicinal chemistry, Jan-15, Volume: 41, Issue:2
| Synthesis and anti-HIV-1 activity of novel 2,3-dihydro-7H-thiazolo[3,2-a]pyrimidin-7-ones. |
| AID22007 | Solubility was determined with phosphate buffer (0.10M, 5 mL). | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| Design, synthesis, and structure-activity relationship of novel dinucleotide analogs as agents against herpes and human immunodeficiency viruses. |
| AID45373 | Antiviral activity in CEM-SS cell line infected with HIV-1 and Concentration required to inhibit the replication of HIV-1 by 50% was determined | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID231665 | CC50/EC50 ratio expressed as selectivity index(SI) | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Specific anti-HIV-1 "acyclonucleosides" which cannot be phosphorylated: synthesis of some deoxy analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID271058 | Antiviral activity against HIV1 NL4-3 replication in human MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID157569 | Antiviral activity against human peripheral blood mononuclear cells, infected with HIV-1(strain LAV) | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID1193106 | Cytotoxicity against cat CRFK cells assessed as cell viability at 10 uM after 24 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Novel fused tetrathiocines as antivirals that target the nucleocapsid zinc finger containing protein of the feline immunodeficiency virus (FIV) as a model of HIV infection. |
| AID1300995 | Antiviral activity against HIV1 3B infected in human MT4 cells at 50 to 100 times antiviral EC50 added 1 to 25 hrs post infection assessed as time required for loss of inhibition of viral replication measured at 30 hrs post infection by p24 ELISA method | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | | | |
| AID1457760 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 6 days by XTT tetrazolium dye-based assay | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs. |
| AID133198 | Quantity of anylate in P1 subregion in mouse brain that contains nuclei and cell debris, after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID152657 | Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17 variant. | 1999 | Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
| Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. |
| AID217742 | In vitro cytotoxicity in vero cells. | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
| Enantiomeric synthesis of D- and L-cyclopentenyl nucleosides and their antiviral activity against HIV and West Nile virus. |
| AID1700257 | Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability incubated for 48 hrs by CellTiter 96 aqueous nonradioactive cell proliferation assay | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24
| Bivalent HIV-1 fusion inhibitors based on peptidomimetics. |
| AID222399 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 8 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID548559 | Antiviral activity against HIV1 7303-3 harboring reverse transcriptase 41L/44D/67N/69D/118I/210W/215Y mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID558367 | Drug level in HIV-infected pregnant woman maternal blood plasma at 300 mg, po BID by LC/MS/MS analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID154934 | Effective concentration against HIV-1 strain LAV in human peripheral blood mononuclear (PBM) cells. | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| L-beta-(2S,4S)- and L-alpha-(2S,4R)-dioxolanyl nucleosides as potential anti-HIV agents: asymmetric synthesis and structure-activity relationships. |
| AID45534 | Concentration required to achieve 50% protection of CEM-SS cells against the cytopathic effect of HIV-1. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
| Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils. |
| AID1060626 | Fold resistance, ratio of EC50 for HIV1 RES056 expressing K103N/Y181C mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID300151 | Selectivity index, ratio of CC50 for rhesus monkey MA104 cells to IC50 for Rotavirus RF | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID83227 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1292010 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID519961 | Selectivity ratio of EC50 for 0.02 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.02 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1457758 | Antiviral activity against tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells assessed as inhibition of viral replication inhibition of virus-induced cytopathic effect after 6 days by XTT d | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs. |
| AID210897 | In Vitro inhibition of Thymidine Monophosphatase Kinase of Mycobacterium tuberculosis (TMPKm) | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
| 3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase. |
| AID83231 | Compounds were evaluated for anti-RT activity by MTT dose and %protection was reported at 13 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1304399 | Inhibition of HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rC)/oligo(dG) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID757623 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID548808 | Antiviral activity against HIV1 isolate 212 harboring reverse transcriptase L210W/T215Y mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID573988 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID736856 | Cytotoxicity against human C8166 cells by MTT assay | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Dibenzocyclooctadiene lignans and norlignans from fruits of Schisandra wilsoniana. |
| AID1757994 | Cytotoxicity against human CEM-TK(-) cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID104790 | Cytotoxic concentration which is required to reduce human MT-4 cell viability by 50%. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID105344 | Protection of MT-4 cells against the cytopathic effect of HIV-1 (4 days) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiviral activity of 8-aza analogs of chiral [2-(phosphonomethoxy) propyl]guanines. |
| AID104799 | Cytotoxicity against MT-4 cells | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Synthesis and biological evaluation of thymine nucleosides fused with 3',4'-tetrahydrofuran ring. |
| AID235480 | Selectivity index is the ratio of CC50 to EC50 | 1990 | Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
| 5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity. |
| AID574194 | Cytotoxicity against human skeletal muscle Myoblast assessed as change in POLG mitochondrial RNA level on day 2 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID154769 | Concentration required to inhibit replication of HIV-1 HTLV-IIIB strain in PBL (peripheral blood lymphocytes) cells | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1304405 | Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human MT4 cells to EC50 for antiviral activity against HIV-1 3B | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID1156488 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for wild type HIV1 3B | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
| AID548580 | Antiviral activity against HIV1 isolate 070 harboring reverse transcriptase 65R/S68G mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID573986 | Antiviral activity against non nucleoside reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID210901 | In Vitro inhibition of Thymidine Monophosphatase Kinase (TMPKh); not determined | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
| 3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase. |
| AID1157583 | Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID520605 | Cytotoxicity against human WI38 cells by neutral red assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Anti-BK virus activity of nucleoside analogs. |
| AID330489 | Antiviral activity against HIV1 RES056 infected in MT4 cells by MTT | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID426889 | Inhibition of HIV1 viral replication infected in human PBMC cells assessed as viral p24Ag concentration after 7 days postinfection by ELISA | 2009 | Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
| Synthesis, antiviral activity and molecular modeling of oxoquinoline derivatives. |
| AID210290 | In vitro antiviral activity against T-cells | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID248294 | Inhibitory concentration was determined against PHA stimulated human peripheral blood mononuclear cells | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Synthesis, antiviral activity, and mechanism of drug resistance of D- and L-2',3'-didehydro-2',3'-dideoxy-2'-fluorocarbocyclic nucleosides. |
| AID1652588 | Cytotoxicity in human CEM/0 cells assessed as reduction in cell viability incubated for 4 to 5 days | | | |
| AID198594 | In vitro inhibition of HIV-1 reverse transcriptase at 100 uM; NA = not applicable | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi |
| AID573981 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for Human immunodeficiency virus 2 EHO | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID326391 | Selectivity index, ratio of CC50 for C8166 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
| 1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro. |
| AID417243 | AUC in HIV-infected human assessed as zidovudine monophosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID487830 | Cytotoxicity against human MT2 cells after 6 days by XTT assay | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Anti-AIDS agents 82: synthesis of seco-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents. |
| AID379884 | Cytotoxicity against human H9 cells after 4 days | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12
| Rubrisandrins A and B, lignans and related anti-HIV compounds from Schisandra rubriflora. |
| AID1687682 | Antiviral activity against HIV-1 Y181C mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID1743638 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID676995 | Selectivity index, ratio of CC50 for human HeLa cells to IC50 for Plasmodium falciparum 3D7 ring stage cells | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
| Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID235440 | Selective index as the ratio of CC50 to that of IC50 value against Jurkat cells. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID1705191 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID665274 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1456310 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
| Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
| AID1199054 | Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID197946 | In vitro inhibitory activity against human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. |
| AID82109 | Evaluated for the antiretroviral activity against Human immunodeficiency virus type 1 | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
| Acyclic purine phosphonate analogues as antiviral agents. Synthesis and structure-activity relationships. |
| AID1504699 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID664470 | Antiviral activity against wild type HIV1 clade C 98USMSC5016 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround infect | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID1710777 | Cytotoxicity against human HeLa cells assessed as changes in cell morphology incubated for 3 to 6 days by light microscopic analysis | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID86854 | The EC50 value was measured on hepatitis B virus | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
| Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2', 3'-unsaturated L-nucleosides. |
| AID572775 | Antiviral activity against HIV1 harboring reverse transcriptase L74V mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1055510 | Antiviral activity against HIV2 ROD infected in human CEM cells assessed as virus-induced giant cell formation after 4 days by microscopic analysis | 2013 | European journal of medicinal chemistry, , Volume: 70 | Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides. |
| AID569222 | Antiviral activity against HIV1 NL4.3 infected in human CEM-GFP T cells assessed as inhibition of p24 antigen production after 7 days by ELISA | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
| Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5. |
| AID45025 | Effective concentration required to achieve 50% inhibition of HIV-1 181C (nevirapine-resistant HIV-1) multiplication in CEM-SS cells. | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID235811 | Selectivity by CC50 of CEM cells/EC50 of CEM cells against HIV-1 | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID707988 | Antiviral activity against HIV-1 3B infected in C8166 cells assessed as virus-induced cytopathic effect measuring scintia formation after 3 days by microscopy | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of inhibitors to block interactions of HIV-1 integrase with human LEDGF/p75 via structure-based virtual screening and bioassays. |
| AID548826 | Antiviral activity against HIV1 isolate 174 harboring reverse transcriptase M184V mutant gene obtained as site-directed mutant of NL4-3 by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID235799 | Selectivity index which is the ratio between CC50 and EC50 | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Decomposition pathways and in vitro HIV inhibitory effects of isoddA pronucleotides: toward a rational approach for intracellular delivery of nucleoside 5'-monophosphates. |
| AID1631596 | Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 10 uM measured after 4 days by p24 ELISA | 2016 | Bioorganic & medicinal chemistry, 09-01, Volume: 24, Issue:17
| Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA. |
| AID363846 | Antiviral activity against rotavirus RF in human Caco-2 cells assessed as neutralization of virus before its attachment after 72 hrs | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
| Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities. |
| AID1220800 | Drug metabolism in bile duct-cannulated monkey assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
| Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
| AID587737 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as time required to cause 50% loss in compound potency at 10 t | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID1610042 | Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID235878 | Ratio of EC50/CC50 | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
| Structure-activity relationships of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine analogues: effect of substitutions at the C-6 phenyl ring and at the C-5 position on anti-HIV-1 activity. |
| AID358594 | Antiviral activity against Human immunodeficiency virus | 2001 | Journal of natural products, Nov, Volume: 64, Issue:11
| Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp. |
| AID104243 | Anti-HIV activity based on reduction of the viability of mock-infected MT-2 cells. | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
| AID46838 | Effective concentration required to inhibit the replication of HIV-1 by 50% in CEM/TK cells | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID1238318 | Cytotoxicity against human PM1 cells expressing CCR5 by MTT assay in presence of 5 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID569161 | Antiviral activity against HIV1 NL4.3 infected in human CEM-GFP T cells assessed as inhibition of p24 antigen production at highest non cytotoxic concentration after 7 days by ELISA | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
| Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5. |
| AID780329 | Cytotoxicity against human CEM cells | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
| Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors. |
| AID106776 | Compound was evaluated for antiviral activity against MT-4 cells. Cell culture inhibitor concentration (CIC95) is defined as those which inhibited by >95% the spread of HIV-1 IIIb infection in susceptible cell culture; value ranges from 0.012-0.025 uM | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one. |
| AID45843 | Compound was evaluated for cytotoxicity against thymidine kinase deficient CEM cell line infected with HIV-1 | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9
| Anti-HIV pronucleotides: decomposition pathways and correlation with biological activities. |
| AID519868 | Antiviral activity against HIV1 subtype B-92US076 infected in 1 hr-pretreated PBMC cells assessed as inhibition of p24 antigen production measured on day 5 postinfection by ELISA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1636356 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID648424 | Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1221970 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID341191 | Metabolic stability of the compound in human CD4+ CEM cells assessed as 3'-azido-2',3'-dideoxythymidine monophosphate intracellular levels at 200 nM after 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID89170 | Concentration required to inhibit HIV-1 replication in acutely infected H9 lymphocytes by 50% | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Anti-AIDS agents. 52. Synthesis and anti-HIV activity of hydroxymethyl (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone derivatives. |
| AID47289 | Compound was evaluated for its cytotoxicity against CEM cells. | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine. |
| AID542933 | Induction of preadipocyte differentiation in mouse 3T3-F442A cells assessed as adiponectin mRNA expression on day 9 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID222499 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 24 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID584082 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase L100I, K103Q, H221H/Y mutant infected in human SupT1 cells derived from 11 viral passages with efavirenz assessed as inhibition of viral replication after 21 days relative to drug sensi | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID105400 | AntiHIV-1 activity measured in MT-4 cells at 5 to 6 different concentrations, using the reverse transcriptase (RT) assay | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC). |
| AID1632130 | Selectivity index, ratio of IC50 for HDF to IC50 for human MCF7 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID417051 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine diphosphate level at 600 mg administered in two courses, first BID for 7 to 14 days followed by QD for 7 days and second course the subjects were switched to the other regimen measured per | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID47140 | Effective concentration required to inhibit HIV-1 induced cytopathicity by 50% in CEM cells | 2001 | Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
| Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase. |
| AID378287 | Cytotoxicity against mock-infected human H9 cells | 2000 | Journal of natural products, Dec, Volume: 63, Issue:12
| Anti-AIDS agents 38. Anti-HIV activity of 3-O-acyl ursolic acid derivatives. |
| AID766741 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Synthesis and evaluation of novel 3-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents. |
| AID548831 | Antiviral activity against HIV1 isolate 194 harboring reverse transcriptase M41L/T215Y/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID89134 | Concentration of compound required to 50% growth inhibition of HIV-1 in CEM-SS cells | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID279923 | Effect on LDL cholesterol level in cafteria-fed Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1460941 | Antiviral activity against HIV-1 NL4-3 harboring reverse transcriptase K103N mutant infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID7699 | Compound was tested in vitro for inhibition of cytopathogenicity of LAV(IIIB) in CD4+ T-cells (A3.01) | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID105554 | Effective concentration required to protect MT-4 cells against cytopathogenicity of HIV-1 LAI | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude. |
| AID1754638 | Cytotoxicity against mock-infected human MT4 cells incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID304872 | Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells after 5 days by MTT method relative to wild type NL4-3 | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants. |
| AID1193051 | Antiviral activity against HIV1 LAV-1 infected in human PBMC cells after 6 days by RT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Molecular docking and antiviral activity of N-substituted benzyl/phenyl-2-(3,4-dimethyl-5,5-dioxidopyrazolo[4,3-c][1,2]benzothiazin-2(4H)-yl)acetamides. |
| AID81252 | Effective concentration required to inhibit HIV-1 replication in CEM/TK cell line | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| S-acyl-2-thioethyl phosphoramidate diester derivatives as mononucleotide prodrugs. |
| AID104420 | Conc. required to cause 50% death of uninfected MT-4 cells | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID1275545 | Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID456310 | Cytotoxicity against human PBMC by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands. |
| AID346971 | Antiviral activity against HIV ROD in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Studies on anti-HIV quinolones: new insights on the C-6 position. |
| AID247943 | Inhibitory concentration against uninfected Vero cells | 2005 | Journal of medicinal chemistry, Jun-02, Volume: 48, Issue:11
| Synthesis, antiviral activity, and mechanism of drug resistance of D- and L-2',3'-didehydro-2',3'-dideoxy-2'-fluorocarbocyclic nucleosides. |
| AID38035 | Effective concentration required for antiviral activity against B(EBV+) cell line of AA5 cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID635347 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
| AID83284 | Effective concentration required for antiviral activity against HIV strain G9106 (AZT-resistant strain) by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID46059 | Inhibition of wild type HIV-1-IIIB strain replication in CEM-SS cells | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors. |
| AID553576 | Antiviral activity against HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID125353 | Compound was evaluated for anti-HIV activity against HIV-1Lal inoculated with Molt-4 cells | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
| 'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker. |
| AID373573 | Binding affinity to TK1 in human H9 cells assessed as conversion of [3H]azidothymidine to [3H]azidothymidine monophosphate by scintillation counting | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID542937 | Antiproliferative activity against mouse 3T3-F442A cells assessed as [3H]thymidine incorporation at 180 uM | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID152656 | Inhibition of cell growth against HIV-1 infected PBM (Human peripheral blood mononuclear) cells | 1993 | Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
| Structure-activity relationships of beta-D-(2S,5R)- and alpha-D-(2S,5S)-1,3-oxathiolanyl nucleosides as potential anti-HIV agents. |
| AID576388 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 12.5 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID232354 | Ratio of CC50 in CEM-CL13 cells to EC50 in HIV-1 LA1 infected CEM-CL13 cells. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs. |
| AID211649 | Compounds were evaluated for their potential toxic effect on uninfected PHA-stimulated human T-lymphoblastoid cell line (CEM) | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID279935 | Increase in AMPK phosphorylation level in rat inguinal adipose cells at 70 mg/kg/day | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1483279 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID222389 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 2 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID548549 | Antiviral activity against HIV1 subtype B isolate 92TH014 infected in human MDM after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID47455 | Antiviral test was performed against HIV (LAV strain) on CEM cells using 50 tissue culture infectious units. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID584614 | Toxicity in human subcutaneous preadipocytes assessed as decrease of cell viability measured every 5 days at 6 uM after 30 days using oil red O fluorescence staining by conventional fluorescence microscopy | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1457054 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID81086 | Anti HIV-1 activity against the virus NL4-3 using fusion assay | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
| Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid. |
| AID355254 | Cytotoxicity against uninfected PHA-stimulated human PBMC assessed as thymidine incorporation after 24 hrs by trypan blue exclusion method | 1997 | Journal of natural products, Sep, Volume: 60, Issue:9
| In vitro anti-HIV activity of biflavonoids isolated from Rhus succedanea and Garcinia multiflora. |
| AID1729160 | Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID1636440 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
| AID1884486 | Antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID1298245 | Cytotoxicity against human MT4 cells after 5 days MTT assay | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
| AID619629 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID647165 | Antiviral activity against HIV1 3B infected human TZM-bl cells assessed as inhibition of viral replication by luciferase reporter assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Synthesis and antiviral activities of novel gossypol derivatives. |
| AID45009 | Concentration required to reduce the viability of uninfected cells (CEM-CL13) by 50% on day 7. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID341179 | Antiviral activity against R5-HIV1Ba-L assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID1235866 | Cytotoxicity against human C8166 cells by MTT assay | 2015 | Journal of natural products, Aug-28, Volume: 78, Issue:8
| Kadcoccinic Acids A-J, Triterpene Acids from Kadsura coccinea. |
| AID520604 | Antimicrobial activity against BK polyomavirus ATCC VR837 infected in human WI38 cells assessed as reduction in viral titer after 7 days by PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Anti-BK virus activity of nucleoside analogs. |
| AID105131 | Activity against HIV-1 in MT-4 cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID611608 | Antiviral activity against wild-type HIV1 3B infected in human C8166 cells assessed as protection against virus-induced cytopathogenicity after 3 days by measuring syncytia under inverted microscope | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1543133 | Cytotoxicity against human MT4 cells measured after 3 days by CytoTox-Glo assay | 2019 | Journal of natural products, 06-28, Volume: 82, Issue:6
| Potent Anti-HIV Ingenane Diterpenoids from Euphorbia ebracteolata. |
| AID1068979 | Antiviral activity against HIV-2 ROD infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents. |
| AID548558 | Antiviral activity against HIV1 4755-5 harboring reverse transcriptase 41L/44D/67N/69D/118I/210W/215Y/184V mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID664472 | Antiviral activity against multidrug-resistant HIV1 clade B 4775-5 clinical isolate infected in PHA-P-stimulated human PBMC assessed as reverse transcriptase activity incubated for 6 hrs followed by incubated in drug-free medium for 6 days by multiround i | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID417247 | Tmax in HIV-infected human assessed as zidovudine triphosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID757622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID104763 | Cytotoxic concentration against MT-4 cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID1520507 | Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity. |
| AID287873 | Antiviral activity against rotavirus RF infected human Caco-2 cells following viral attachment after 72 hrs | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9
| An efficient synthesis of 3-fluoro-5-thio-xylofuranosyl nucleosides of thymine, uracil, and 5-fluorouracil as potential antitumor or/and antiviral agents. |
| AID82920 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 15 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID235704 | Selectivity index of CD50 to ED50 of MT-4 cells | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides. |
| AID572983 | Cytotoxicity against african green monkey Vero cells after 2 to 4 days by MTT assay | 2009 | Antimicrobial 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. |
| AID45996 | Cytotoxic activity against CEM cell lines. | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Synthesis, in vitro anti-breast cancer activity, and intracellular decomposition of amino acid methyl ester and alkyl amide phosphoramidate monoesters of 3'-azido-3'-deoxythymidine (AZT). |
| AID397591 | Therapeutic index, ratio of cytotoxicity against human H9 cells to EC50 for HIV1 3B | 2001 | Journal of natural products, Feb, Volume: 64, Issue:2
| Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program. |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4
| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID626424 | Antiviral activity against Human immunodeficiency virus 1 assessed as inhibition of viral replication by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| Synthesis and anti-HIV-1 activity of 4-substituted-7-(2'-deoxy-2'-fluoro-4'-azido-β-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidine analogues. |
| AID282749 | Cytotoxicity against macrophages | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
| AID83221 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1754647 | Antiviral activity against HIV1 harboring RT RES056 mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID523347 | Antiviral activity against HIV1 with RT connection domain N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID83075 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 21 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID519890 | Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID105766 | Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 5 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID81069 | Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells. | 1988 | Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
| Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides. |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1594064 | Cytotoxicity against cat CRFK cells measured after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Synthesis and comparison of substituted 1,2,3-dithiazole and 1,2,3-thiaselenazole as inhibitors of the feline immunodeficiency virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID559936 | Antiviral activity against HIV1 X4 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID197808 | In vitro inhibition of HIV-1 reverse transcriptase; NA = not applicable | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi |
| AID291763 | Therapeutic index, Ratio of CC50 for human C8166 cells to EC50 for HIV1 | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro. |
| AID15237 | Percentage of radioactivity in P3 subregion in mouse brain that contains microsomal fraction after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID1589122 | Cytotoxicity in human NHDF cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1815381 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID82563 | Cellular toxicity was measured in CEM cells after 8 days by using a [3H]- thymidine uptake assay | 1989 | Journal 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. |
| AID572981 | Cytotoxicity against human PBMC after 2 to 4 days by MTT assay | 2009 | Antimicrobial 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. |
| AID209368 | Cytotoxic concentration to inhibit HIV replication in TK CEM-SS cell line | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
| Rational design of a new series of pronucleotide. |
| AID604024 | Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID675187 | Antiviral activity against HIV-1 subtype B US/92/727 infected in PBMC assessed as inhibition of viral replication after 7 days by XTT assay | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID548807 | Antiviral activity against HIV1 isolate 211 harboring reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1213031 | Drug metabolism assessed as UGT2B7 activity in human liver microsome assessed as of O-glucuronidation at 25 to 200 uM incubated for 60 mins by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
| Human UDP-glucuronosyltransferase isoforms involved in haloperidol glucuronidation and quantitative estimation of their contribution. |
| AID154958 | Anti-viral activity against HIV-1 in human PBM cells | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
| Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID106910 | Effective antiviral dose required to block the spread of HIV-1 IIIb infection in MT-2 cells by monitoring the formation of syncytia | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID523355 | Antiviral activity against HIV1 with RT connection domain Y181C/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID1610044 | Therapeutic index, ratio of CC50 for human PBMC cells to IC50 for antiviral activity against HIV1 VB51 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID1720644 | Cytotoxicity in human TZM assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID45026 | Effective concentration required to achieve 50% inhibition of HIV-1 LAI replication in human T4 lymphoblastoid CEM-SS cells. | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID1504704 | Antiviral activity against HIV1 3B harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID1884489 | Antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID543110 | Antiproliferative activity against mouse 3T3-F442A cells assessed as mtDNA depletion | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1757993 | Antiviral activity against HIV-1 infected in human CEM-TK(-) cells assessed as reduction in viral multiplication by measuring decrease in reverse transcriptase activity incubated for 6 days | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID423784 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID106771 | Cytotoxic dose to reduce the viability of MT-4 cells by 50 % was determined | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Synthesis, antiretrovirus effects, and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine. |
| AID1757976 | Cytotoxicity against human CEM-SS cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs. |
| AID47141 | Effective concentration required to inhibit HIV-2 induced cytopathicity by 50% in CEM cells | 2001 | Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
| Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase. |
| AID287284 | Cytotoxicity against human PBMC after 6 days | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors. |
| AID581050 | Increase in mitochondrial DNA level in differentiated mouse 3T3-F442A cells at 10 uM by real-time PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Effects of zidovudine and stavudine on mitochondrial DNA of differentiating 3T3-F442a cells are not associated with imbalanced deoxynucleotide pools. |
| AID104968 | 50% effective concentration of compound which is required to protect human MT-4 cells against cytopathogenicity of HIV-2. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID79128 | Evaluated for the anti-HIV activity against HIV-1 replication in mock-infected H9 cells | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents. |
| AID83060 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID398469 | Inhibition of RNA polymerase | 1995 | Journal of natural products, Jul, Volume: 58, Issue:7
| Mechanistic evaluation of new plant-derived compounds that inhibit HIV-1 reverse transcriptase. |
| AID548306 | Antiviral activity against HIV1 subtype B isolate ADA infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID284451 | Cytotoxicity against Vero cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Enantioselective synthesis and antiviral activity of purine and pyrimidine cyclopentenyl C-nucleosides. |
| AID1687683 | Antiviral activity against HIV-1 E138K mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID222689 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 2 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID574199 | Cytotoxicity against human skeletal muscle Myotube assessed as change in Tfam mitochondrial RNA level on day 5 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID248082 | Concentration required to produce 50% toxicity against mock-infected H9 cells | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents. |
| AID1292007 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as cell viability after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID342553 | Cytotoxicity against human thymidine kinase-deficient CEM cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID235700 | Selectivity index is the ratio of CC50 and EC50 in MT-4 cells | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID1460943 | Antiviral activity against HIV-1 NL4-3 harboring reverse transcriptase Y181C mutant infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID1303216 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and anti-HIV activity of novel quinoxaline derivatives. |
| AID361402 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2002 | Journal of natural products, Nov, Volume: 65, Issue:11
| New saponins from the starfish Certonardoa semiregularis. |
| AID557278 | Ratio of EC50 for HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1379961 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
| AID682145 | TP_TRANSPORTER: inhibition of E1S uptake (E1S: 40 uM, AZT: 1000 uM) in Xenopus laevis oocytes | 1999 | The Journal of biological chemistry, May-07, Volume: 274, Issue:19
| Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. |
| AID1391081 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID493820 | Cytotoxicity against human CEM cells expressing green fluorescent protein by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus. |
| AID1311576 | Cytotoxicity against human HepG2 cells assessed as growth inhibition measured after 3 days by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| Synthesis and cytotoxic evaluation of novel indenoisoquinoline-substituted triazole hybrids. |
| AID82981 | Cytotoxicity was tested in HL60 cells by the trypan blue exclusion assay. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC). |
| AID104258 | In vitro Cytotoxic concentration which reduced G 691-2(post-AZT) infected MT-2 cells by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID1604016 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review. |
| AID369078 | Antiviral activity against HIV1 LAI infected in CEM cells | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID548823 | Antiviral activity against HIV1 isolate 160 harboring reverse transcriptase S68G/V75(I/T)/F77L/Y115F/F116Y /Q151M mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID106893 | Anti-HIV activity against HIV-I IIIB strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID235683 | Selectivity Index measured as the ratio of EC50 to that of CC50 values. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| A new class of HIV-1-specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). |
| AID1197832 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
| AID78760 | Anti-HIV activity was measured in H9-cells by MAGI assay | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID290120 | Antiviral activity against HSV1 in CCL81 cells | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiviral activity of C-fluoro-branched cyclopropyl nucleosides. |
| AID1631598 | Antiviral activity against HIV-1 NL4-3 infected in human U87 cells expressing CD4.CXCR4 assessed as inhibition of p24 production at 100 uM measured after 4 days by p24 ELISA | 2016 | Bioorganic & medicinal chemistry, 09-01, Volume: 24, Issue:17
| Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA. |
| AID157555 | Anti-HIV activity in Human peripheral blood mononuclear (PBM) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID542924 | Antiproliferative activity against mouse 3T3-F442A cells assessed as [3H]thymidine incorporation | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1710802 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 3 to 6 days by MTS assay | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID1316342 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID106749 | Cytotoxicity based on the reduction of the viability of mock-infected MT-4 cells using the MTT method | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety. |
| AID576191 | Antiviral activity against Human immunodeficiency virus 1 3B expressing nef protein infecting in CEM-SS cells assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1077218 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID696752 | Antiviral activity against HIV1 infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect | 2012 | Journal of natural products, Nov-26, Volume: 75, Issue:11
| Antiviral chromones from the stem of Cassia siamea. |
| AID106080 | Inhibitory concentration against HIV-1 infected MT-4 cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID284449 | Cytotoxicity against PBM cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Enantioselective synthesis and antiviral activity of purine and pyrimidine cyclopentenyl C-nucleosides. |
| AID548576 | Antiviral activity against HIV1 isolate 063 harboring reverse transcriptase M41L/D67N/K70R/M184V/L210W/T215Y/K219E mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID539774 | Selectivity index, ratio of CC50 for human CEM-SS cells to EC50 for Human immunodeficiency virus 1 infected in human CEM-SS cells | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
| 1-Benzyl derivatives of 5-(arylamino)uracils as anti-HIV-1 and anti-EBV agents. |
| AID548317 | Antiviral activity against HIV1 subtype E isolate 93TH073 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID89026 | Antiviral activity against drug-resistant HIV-1 virus (M184v) in Human peripheral blood mononuclear (PBM) cells | 2004 | Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
| Synthesis, structure-activity relationships, and mechanism of drug resistance of D- and L-beta-3'-fluoro-2',3'-unsaturated-4'-thionucleosides as anti-HIV agents. |
| AID376302 | Selectivity index, CC50 for human C8166 cells to EC50 for HIV1 3B | 2006 | Journal of natural products, Apr, Volume: 69, Issue:4
| Nortriterpenoids from Schisandra lancifolia. |
| AID576391 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 12.5 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID751133 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV-1 3B | 2013 | Journal of natural products, Jun-28, Volume: 76, Issue:6
| Bioactive dibenzocyclooctadiene lignans from the stems of Schisandra neglecta. |
| AID1443666 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID80886 | Effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-1 (HTLV-IIIB). | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| A new class of HIV-1-specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). |
| AID46644 | Concentration required to reduce CEM/0 cell viability by 50% | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID46608 | In vitro inhibition of CEM-SS cell growth by 50 % | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| In vitro evaluation of phosphocholine and quaternary ammonium containing lipids as novel anti-HIV agents. |
| AID693591 | Antiviral activity against wild type HIV1 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect after 3 days by syncytium reduction assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors. |
| AID1285841 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as cytopathic effect by counting the number of syncytia by microscopy | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
| Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors. |
| AID104421 | Cytotoxic conc. which reduces the cell viability of HIV-1 IIIB infected T4 lymphoblastoid MT-4 cells by 50% | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID25912 | Half-life for the compound after intravenous administration into BALB/c Mice in plasma samples. | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID1589117 | Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1504701 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID232355 | Ratio of CC50 value that of EC50 value(HIV-1) | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs. |
| AID83234 | Compounds were evaluated for anti-RT activity by MTT dose and %protection was reported at 9 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID519887 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID79304 | Inhibitory concentration required to inhibit HIV replication in H9 lymphocytes growth by 50% | 1999 | Bioorganic & medicinal chemistry letters, Jan-18, Volume: 9, Issue:2
| Substituted 7H-pyrido[4,3-c]carbazoles with potent anti-HIV activity. |
| AID45011 | Concentration that reduced by 50% the HIV induced CPE (cytopathic effect) on day 19. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1203618 | Toxicity in rat liver assessed as change in AST release relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID1352314 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID376815 | Cytotoxicity against human H9 cells | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Bioactive kaurane diterpenoids from Annona glabra. |
| AID47641 | Concentration of the drug resulting in 50% growth inhibition of normal, uninfected cells against HIV-1 replication in CEM cells. | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID587742 | Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID402092 | Cytotoxicity against mock-infected human H9 cells after 4 days | 1998 | Journal of natural products, Sep, Volume: 61, Issue:9
| Anti-AIDS agents. 30. Anti-HIV activity of oleanolic acid, pomolic acid, and structurally related triterpenoids. |
| AID235474 | Selectivity index is the ratio between CD50 and ED50 | 1996 | Journal of medicinal chemistry, Jun-07, Volume: 39, Issue:12
| Synthesis and potent anti-HIV-1 activity of novel 6-benzyluracil analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID718521 | Antiviral activity against HIV-1 3B infected in MT4 cells assessed as protection against virus-induced cytopathicity relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| POMA analyses as new efficient bioinformatics' platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues. |
| AID46383 | Antiviral activity against site directed resistant isolate HIV-1 Y188C in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID157574 | Compound was evaluated for its anti-HIV activity in vitro in peripheral blood mononuclear (PBM) cells | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine. |
| AID1223472 | Uncompetitive substrate inhibition of UGT2B7 in non-diabetic human kidney microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID81443 | Inhibition of HIV-1 IIIB replication in MT2 (human lymphocyte) cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi |
| AID1126506 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
| Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1652585 | Antiviral activity against HIV1 3B infected in human CEM/0 cells assessed as inhibition of viral-induced giant cell formation incubated for 4 to 5 days by microscopy | | | |
| AID542939 | Cytotoxicity against mouse 3T3-F442A cells at 1 uM after 24 hrs by trypan blue staining | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID45192 | Compound was evaluated for the effect of Order of Addition on Cytoprotection against HIV-1RF at dilution 100, Pretreat with 100 uM | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID519862 | Antiviral activity against HIV1 subtype B-LAI infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1304404 | Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human CEM-SS cells to EC50 for antiviral activity against HIV-1 RF | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID82922 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 22 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID83059 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID232747 | Selectivity index is calculated by dividing the TC25(MT2) by ID50(MT2) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID152820 | Anti-HIV activity against multidrug resistant HIV MM strain by inhibition of HIV p24 antigen expression in peripheral blood mononuclear cells(PBMC) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
| AID571604 | Half life in HIV-1 infected patient at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1220794 | Plasma clearance in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1674928 | Antiproliferative activity against human MDA-MB-231 cells at 6.25 to 100 uM incubated for 24 to 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
| Evaluation of the effect of synthetic compounds derived from azidothymidine on MDA-MB-231 type breast cancer cells. |
| AID106964 | Concentration of compound required to achieve 50% protection of MT-4 cells against HIV-1 virus induced cytopathic effect | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Specific anti-HIV-1 "acyclonucleosides" which cannot be phosphorylated: synthesis of some deoxy analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID200175 | Compound was evaluated for enzymatic inhibitory activity against recombinant HIV reverse transcriptase | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
| 5-Alkyl-2-[(methylthiomethyl)thio]-6-(benzyl)-pyrimidin-4-(1H)-ones as potent non-nucleoside reverse transcriptase inhibitors of S-DABO series. |
| AID83067 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID89136 | Anti-HIV-1 activity against syncytial plaque formation at a conc. of 0.0007 uM | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID1729159 | Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID334755 | Cytotoxicity against cat CRFK cells assessed as reduction in cell viability after 5 days by MTT assay | 1992 | Journal of natural products, Apr, Volume: 55, Issue:4
| Fistularin 3 and 11-ketofistularin 3. Feline leukemia virus active bromotyrosine metabolites from the marine sponge Aplysina archeri. |
| AID1357786 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | | | |
| AID45008 | Concentration required to reduce the viability of uninfected cells (CEM-CL13) by 50% on day 22. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID460293 | Antiviral activity against HIV1 NL4-3 infected in GFP expressing human CEM cells assessed as inhibition of viral infection measured after 9 days postinfection by microfluorometry | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols. |
| AID1815385 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID681387 | TP_TRANSPORTER: uptake in Xenopus laevis oocytes | 2000 | The Journal of pharmacology and experimental therapeutics, Sep, Volume: 294, Issue:3
| Rat multispecific organic anion transporter 1 (rOAT1) transports zidovudine, acyclovir, and other antiviral nucleoside analogs. |
| AID1200847 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
| AID1729150 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID1172374 | Cytotoxicity against human 143B cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID416385 | Antiviral activity against HIV1 BH10 in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS method | 2009 | Bioorganic & medicinal chemistry, Mar-15, Volume: 17, Issue:6
| Synthesis and antiviral evaluation of thieno[3,4-d]pyrimidine C-nucleoside analogues of 2',3'-dideoxy- and 2',3'-dideoxy-2',3'-didehydro-adenosine and -inosine. |
| AID104791 | Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50%. | 1991 | Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
| Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin- 2(1H)-one (TIBO) derivatives. |
| AID1687686 | Cytotoxicity against human MT4 cells assessed as inhibition of cell viability by measuring reduction in absorbance at OD540 by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID394136 | Inhibition of polymerase activity of HIV1 recombinant reverse transcriptase expressed in Escherichia coli at 50 uM | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
| Synthesis, HIV-RT inhibitory activity and SAR of 1-benzyl-1H-1,2,3-triazole derivatives of carbohydrates. |
| AID576199 | Cytotoxicity against human AA5 cells by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1720642 | Fold resistance, ratio of EC50 for inhibition of reverse transcriptase K103N/Y181C double mutant/nucleocapsid protein 7 in HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT a | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID600423 | Selectivity index, ratio of CC50 for human C8166-CCR5 cells to EC50 for HIV1 NL4-3 | 2009 | Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14
| Novel 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2)-curcumin, kojic acid, quercetin, and baicalein conjugates as HIV agents. |
| AID83062 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID142321 | Reduced GM-CSF dependent colony formation in murine bone marrow progenitor cells at 50 uM | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID47139 | Effective concentration of required to inhibit the replication of HIV-1 BY 50% in CEM cells | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID369079 | Cytotoxicity against human PBM cells after 3 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID157412 | Inhibitory activity against the HIV-1-induced cytopathic effect in fresh human peripheral blood lymphocytes | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID1888704 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID1589120 | Cytotoxicity in human U87 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | | | |
| AID1077220 | Cytotoxicity against human MT4 cells assessed as growth inhibition after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID548313 | Antiviral activity against HIV1 subtype C isolate 93MW959 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID360655 | Antiviral activity against HIV1 MN infected in human C8166 cells assessed as reduction in antigen gp120 production by ELISA | 2001 | Journal of natural products, May, Volume: 64, Issue:5
| Naphthopyranone glycosides from Paepalanthus microphyllus. |
| AID104613 | Antigen p24 content in culture fluid at 10e-5 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID218240 | Cytotoxicity against Vero cells | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
| Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID378288 | Therapeutic index, IC50 for human T-lymphoid H9 cells to EC50 for HIV1 3B isolate | 2000 | Journal of natural products, Dec, Volume: 63, Issue:12
| Anti-AIDS agents 38. Anti-HIV activity of 3-O-acyl ursolic acid derivatives. |
| AID1743636 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID154765 | In vitro antiviral activity against PBL cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID1726077 | Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. |
| AID47454 | Antiviral test was performed against HIV (LAV strain) on CEM cells using 30 tissue culture infectious units. T | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID587743 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID89167 | Inhibitory activity against HIV-1 (HTLV-IIIB strain) replication in MT-4 cells | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). |
| AID83219 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID106596 | Cytotoxicity against MT-4 (human leukemia) cells. | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID157393 | Cytotoxic concentration based on the reduction of viability of mock-infected peripheral blood lymphocytes (PBL) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID1754646 | Antiviral activity against HIV1 harboring RT F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID1443663 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | | | |
| AID378286 | Antiviral activity against HIV1 3B isolate replication in human H9 cells assessed as decrease in viral p24 level after 4 days | 2000 | Journal of natural products, Dec, Volume: 63, Issue:12
| Anti-AIDS agents 38. Anti-HIV activity of 3-O-acyl ursolic acid derivatives. |
| AID47303 | Cytotoxicity against CEM cells | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
| Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID619638 | Antiviral activity against HIV-1 3B harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID481804 | Ratio of Vmax to Km for Ureaplasma parvum thymidine kinase | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID310350 | Cytotoxicity against MT2 cells by XTT assay | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Anti-AIDS agents 73: structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. |
| AID320328 | Antiviral activity against HIV with reverse transcriptase K65R mutation assessed as fold resistance relative to wild type | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor. |
| AID1357792 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID267854 | Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
| AID1743626 | Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID46082 | Compound was tested for cytotoxicity against HIV-1 in CEM-SS cells | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Rational design of a new series of mixed anti-HIV pronucleotides. |
| AID698304 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID511695 | Cytotoxicity against human CEM-SS cells infected with HIV1 3B after 6 days by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Identification of novel human immunodeficiency virus type 1-inhibitory peptides based on the antimicrobial peptide database. |
| AID1483277 | Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID587747 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID279928 | Increase in cellularity in cafteria-fed Wistar rat inguinal tissue assessed as DNA content at 70 mg/kg/day | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID665272 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C RT mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID89003 | Anti-HIV-1 activity against syncytial plaque formation | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID1267625 | Antiviral activity against NRTI/NNRTI-resistant HIV1 L6 harboring reverse transcriptase V75I/F77L/K103N/F116Y/Q151M/M184V mutant infected in human MT4 cells | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID45006 | Concentration required to reduce the viability of uninfected cells (CEM-CL13) by 50% on day 11. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID104782 | Cytotoxic concentration against HIV-1 infected MT-4 cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID584617 | Toxicity in human subcutaneous preadipocytes assessed as acquisition of adipocyte shape at 6 uM after 30 days using oil red O fluorescence staining by conventional fluorescence microscopy | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1379959 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
| AID217728 | Cytotoxicity against Vero cells was determined. | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents. |
| AID235314 | Selective index is the ratio between IC50 and EC50 | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity. |
| AID525106 | Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID576152 | Cytotoxicity against human CEM-SS cells by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID373365 | Drug metabolism in human CEM cells assessed as radioactive 2', 3'-didehydro-3'-deoxy-4'-ethynylthymidine triphosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID46637 | Inhibition of HIV-1 LA1 cytopathic effects on CEM-CL13 cells in vitro. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs. |
| AID548827 | Antiviral activity against HIV1 isolate 180 harboring reverse transcriptase K65R mutant gene obtained as site-directed mutant of NL4-3 by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID590345 | Antiviral activity against 0.05 MOI Human immunodeficiency virus 1 NL4.3 infected in human CEM cells expressing green fluorescent protein assessed as p24 antigen production at 5 uM measured 7 days post infection by ELISA | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
| Synthesis of 9-substituted derivatives of berberine as anti-HIV agents. |
| AID28922 | In vitro Apparent partition coefficients of mixed aryl phosphodiester was determined | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID523477 | Antiviral activity against HIV1 with RT connection domain G190A/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID698302 | Antiviral activity against HIV1 containing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID380077 | Cytotoxicity against human C8166 cells by MTT assay | 2006 | Journal of natural products, Feb, Volume: 69, Issue:2
| Triterpenoids from Schisandra lancifolia with anti-HIV-1 activity. |
| AID217732 | Cytotoxicity was determined in Vero cells, relative to RVT | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
| 2('),3(')-didehydro-2('),3(')-dideoxynucleosides are degraded to furfuryl alcohol under acidic conditions. |
| AID89147 | Anti-HIV-1 activity against syncytial plaque formation at a conc. of 0.006 uM | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID1275547 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID106917 | Anti-HIV activity against HIV-I G910-6 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID295755 | Cytotoxicity against human HeLa cells at 125 uM after 48 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 17, Issue:11
| Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates. |
| AID557283 | Ratio of EC50 for HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1226479 | Cytotoxicity against BHK cells infected with West Nile virus replicon assessed as cell viability at 10 uM after 3 days by CellTiter 96 aqueous one solution cell proliferation assay relative to control | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| 5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus. |
| AID665551 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID1610043 | Antiviral activity against HIV1 VB51 infected in human PBMC cells incubated for 5 days by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID604022 | Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID779528 | Antiviral activity against HIV-1 RESO56 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
| AID22170 | Therapeutic index calculated from IC50 and EC50 values of the compound | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
| Nucleoside conjugates. 15. Synthesis and biological activity of anti-HIV nucleoside conjugates of ether and thioether phospholipids. |
| AID511694 | Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of viral replication after 6 days by XTT assay | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Identification of novel human immunodeficiency virus type 1-inhibitory peptides based on the antimicrobial peptide database. |
| AID95292 | Inhibitory concentration against HIV-1 infected Jurkat cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID578850 | Cytotoxicity against human CEM cells after 5 days by trypan blue assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors. |
| AID1223469 | Drug metabolism in non-diabetic human kidney microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID81965 | Protection of MT-4 lymphocytes by the compound against HIV-1 infectivity in vitro at a concentration of 0.016 ug/mL (0.00006 uM/mL) | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| HIV-1 neutralization and tumor cell proliferation inhibition in vitro by simplified analogues of pyrido[4,3,2-mn]thiazolo[5,4-b]acridine marine alkaloids. |
| AID330487 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID23323 | Relative brain exposure of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine. |
| AID542931 | Induction of preadipocyte differentiation in mouse 3T3L1 cells assessed as C/EBPalpha mRNA expression on day 6 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID665552 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID619635 | Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1710794 | Antiviral activity against Human immunodeficiency virus 2 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 3 to 6 days by light microscopic analysis | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID20871 | Partition coefficient (P) in 1-octanol and 0.1 M Na3PO4 at pH 7 | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and in vitro evaluation of some modified 4-thiopyrimidine nucleosides for prevention or reversal of AIDS-associated neurological disorders. |
| AID717254 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID214213 | inhibition of HIV-1 induced RT production in U1 cells | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID287286 | Cytotoxicity against Vero cells after 3 days | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors. |
| AID232746 | Selectivity index is calculated by dividing the TC25(CEM) by ID50(CEM) | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5
| Chemical genetics reveals a complex functional ground state of neural stem cells. |
| AID155276 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain A17 variant (Y181C,K103N) in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
| N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. |
| AID283693 | Cytotoxicity against C8166 cells by MTT method | 2007 | Journal of natural products, Apr, Volume: 70, Issue:4
| Bioactive lignans from Peperomia heyneana. |
| AID417241 | AUC in HIV-infected human assessed as zidovudine triphosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1705189 | Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID1589121 | Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1220798 | Half life in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1242368 | Inhibition of CXCR4 in human Jurkat cells assessed as reduction in HIV-Nef-M1-induced mitochondrial membrane depolarization at 0.01 to 100 uM by JC1 dye based fluorescence depolarization assay | 2015 | ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
| Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase. |
| AID426888 | Inhibition of HIV1 viral replication infected in human PBMC cells assessed as viral p24Ag concentration after 7 days postinfection by ELISA relative to untreated control | 2009 | Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
| Synthesis, antiviral activity and molecular modeling of oxoquinoline derivatives. |
| AID341352 | Metabolic stability of the compound in human CEM cells assessed as 3'-azido-2',3'-dideoxythymidine monophosphate intracellular levels at 200 nM after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID698298 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID24685 | Concentration in plasma after intravenous administration of (5S,6S-IMAZT) | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID1457061 | Ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID152622 | In vitro antiviral activity against HIV-1 in human PBM cells. | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
| Enantiomeric synthesis of D- and L-cyclopentenyl nucleosides and their antiviral activity against HIV and West Nile virus. |
| AID706457 | Therapeutic index, ratio of CC50 for human MT4 cells to IC50 for HIV-1 NL4-3 | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18
| Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors. |
| AID82284 | Tested in vitro against HIV-1 LAI from MT-4 cells using MTT assay | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity. |
| AID222396 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 2 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1228734 | Cytotoxicity against human MT4 cells assessed as inhibition of cell metabolism after 72 hrs by MTS assay | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5
| Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID401232 | Antiviral activity against HSV1 | 2004 | Journal of natural products, Apr, Volume: 67, Issue:4
| Isolation of salicin derivatives from Homalium cochinchinensis and their antiviral activities. |
| AID47307 | Cytotoxicity against uninfected PHA-stimulated CEM cells was determined. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| 1,3-dioxolanylpurine nucleosides (2R,4R) and (2R,4S) with selective anti-HIV-1 activity in human lymphocytes. |
| AID1687681 | Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID235698 | Selectivity index is defined as CC25(MT2 cells) / CC50(MT2 cells) | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID342552 | Antiviral activity against HIV1 infected human thymidine kinase-deficient CEM cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID780330 | Antiviral activity against Human immunodeficiency virus 1 infected in human PBMC assessed as inhibition of viral replication after 5 days by RT-PCR method | 2013 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
| Synthesis, docking, and biological studies of phenanthrene β-diketo acids as novel HIV-1 integrase inhibitors. |
| AID200005 | Inhibition of reverse transcriptase of HIV-1 (strain RF)-infected MT-4 cells in RPMI 1640 growth medium in MTM assay | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
| Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. |
| AID1316805 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
| AID78738 | Concentration required to inhibit uninfected H9 cell growth by 50% | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Anti-AIDS agents. 52. Synthesis and anti-HIV activity of hydroxymethyl (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone derivatives. |
| AID417053 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine monophosphate level at 600 mg administered in two courses, first QD for 7 days followed by BID for 7 to 14 days and second course the subjects were switched to the other regimen measured pe | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1446816 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID283692 | Antiviral activity against on HIV1 3b infected C8166 cells assessed as syncytial cell formation after 3 days | 2007 | Journal of natural products, Apr, Volume: 70, Issue:4
| Bioactive lignans from Peperomia heyneana. |
| AID46970 | Concentration required to reduce the viability of mock-infected CEM cells by 50% | 2001 | Bioorganic & medicinal chemistry letters, Dec-03, Volume: 11, Issue:23
| Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase. |
| AID42400 | Selectivity index in HIV-1 infected C8166 (human CD4) cells. | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
| 6-Aminoquinolones as new potential anti-HIV agents. |
| AID1572518 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID46599 | Tested for in vitro drug concentration which results in 50% survival of uninfected untreated control CEM cells | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine. |
| AID1316333 | Cytotoxicity against human mock-infected MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID1322999 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
| AID279936 | Effect on AMPK phosphorylation level in rat epididymal adipose cell at 70 mg/kg/day | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID46839 | Antiviral activity in CEM/TK cell line infected with HIV-1 and cytotoxic concentration required to reduce the viability of uninfected cells by 50% | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID81235 | Compound was evaluated for the antiviral activity against compound resistant virus isolate 4 x AZT with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID341183 | Antiviral activity against R5-HIV1MDR/G assessed as inhibition of p24 Gag protein production in human PHA-PBMC by ELISA | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID1221975 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1191400 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID78959 | Compound was tested for the cytotoxicity in H-9 cells infected with HIV-IIIB over 9 days | 1996 | Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
| Synthesis and HIV inhibition activity of 2',3'-dideoxy-3'-C-hydroxymethyl nucleosides. |
| AID515991 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
| Anti-AIDS agents 84. Synthesis and anti-human immunodeficiency virus (HIV) activity of 2'-monomethyl-4-methyl- and 1'-thia-4-methyl-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) analogs. |
| AID405334 | Toxicity in human HepG2/C3A cells assessed as induction of cell death at 50 uM after 10 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID154806 | Antiviral activity against subtype isolate O strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID141779 | Inhibitory activity on moloney murine leukemia retrovirus. | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
| Anti-HIV-I activity of linked lexitropsins. |
| AID1289706 | Inhibition of human TERT-regulated Wnt/beta-catenin signalling in human MGC803 cells assessed as decrease in c-myc protein expression at 3 mmol/L after 48 hrs by Western blotting method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID300147 | Selectivity index, ratio of CC50 for human Caco-2 cells to IC50 for Rotavirus RF | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID106755 | Cytotoxicity indicative of 50% survival concentration in virus-uninfected MT-4 cells. | 2002 | Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
| Synthesis and biological evaluation of novel D-2'-azido-2',3'-dideoxyarabinofuranosyl-4'-thiopyrimidines and purines. |
| AID257168 | Antiviral activity against HIV1 K103N mutant strain infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
| AID320329 | Antiviral activity against HIV with reverse transcriptase 6TAMs mutation assessed as fold resistance relative to wild type | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor. |
| AID208557 | In vitro inhibitory activity against uninfected T4 cells | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
| Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents. |
| AID559938 | Antiviral activity against HIV1 R5X4 infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID1635807 | Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 4736-2 expressing integrase N155H mutant to EC50 for HIV1 expressing wild-type integrase | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H. |
| AID664468 | Cytotoxicity against human HeLa P4/R5 cells after 48 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID1508589 | Inhibition of HIV-induced cytopathogenicity in MT-4 cell (ZIDOVUDINE control) | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
| Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes. |
| AID373355 | Drug metabolism in human CEM cells assessed as radioactive 2', 3'-didehydro-3'-deoxy-4'-ethynylthymidine diphosphate accumulation at 2 uM after 12 hrs assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID105158 | Effective concentration required to achieve 50% protection of MT-4 cells against cytopathic effect of HIV-1 (4 days) | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs. |
| AID231792 | Ratio of cytotoxic concentration (CC50) in test-II to that of EC50 of compound | 2000 | Bioorganic & medicinal chemistry letters, Dec-04, Volume: 10, Issue:23
| Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes. |
| AID105759 | Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.00032 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID46995 | Compound was tested for cytotoxicity against HIV-1 in CEM/TK- cells | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Rational design of a new series of mixed anti-HIV pronucleotides. |
| AID206710 | Inhibitory concentration against methicillin-resistant Staphylococcus aureus; Not tested | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| New manzamine alkaloids from an Indo-Pacific sponge. Pharmacokinetics, oral availability, and the significant activity of several manzamines against HIV-I, AIDS opportunistic infections, and inflammatory diseases. |
| AID1761011 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID155823 | Concentration required to kill 50% of PBMCs | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID133200 | Quantity of anylate in P3 subregion in mouse brain that contains microsomal fraction after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID576379 | Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID83538 | Tested for the determination of percentage toxicity at 20 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID574190 | Cytotoxicity against human skeletal muscle Myoblast assessed as change in MTCO3 mitochondrial RNA level on day 2 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID341359 | Drug uptake in human CD4+CEM cells assessed as 3'-azido-2',3'-dideoxythymidine diphosphate half life at 200 nM | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID548801 | Antiviral activity against HIV1 isolate 194 harboring reverse transcriptase M41L/T215Y/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1204144 | Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| PMA-SiO2 catalyzed synthesis of indolo[2,3-c]quinolines as potent anti cancer agents. |
| AID501754 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 4 days by p24 antigen based ELISA assay | 2010 | Bioorganic & medicinal chemistry, Sep-01, Volume: 18, Issue:17
| Conjugates of betulin derivatives with AZT as potent anti-HIV agents. |
| AID456303 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands. |
| AID1316337 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID290119 | Antiviral activity against HIV1 in MT4 cells | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiviral activity of C-fluoro-branched cyclopropyl nucleosides. |
| AID587748 | Ratio of EC50 for single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to virus immed | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID83566 | Tested for the determination of percentage protection at 5 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID1407647 | Therapeutic index, ratio of CC50 for human CEM-GFP cells to IC50 for HIV-1 NL4-3 infected in human CEM-GFP cells | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Design, synthesis, docking studies and biological screening of 2-thiazolyl substituted -2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazines as potent HIV-1 reverse transcriptase inhibitors. |
| AID1705193 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID104458 | Inhibitory concentration determined on an HIV infection model mediated by CXCR4; Not tested | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. |
| AID576142 | Antiviral activity against Human immunodeficiency virus 1 subtype O BCF01 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1504696 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID376816 | Antiviral activity against HIV infected in human H9 cells assessed as viral replication | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Bioactive kaurane diterpenoids from Annona glabra. |
| AID1292008 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV2 ROD infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID1888698 | Antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID282751 | Selectivity index, ratio of CC50 for monocyte-macrophages to EC50 for HIV1-3 Ba-L infected macrophages | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
| AID46372 | Antiproliferative activity was determined against human T-lymphocyte cells-CEM | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
| Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription. |
| AID1285843 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as reduction in p24 antigen level incubated for 2 hrs followed by cell plating for 72 hrs by ELISA method | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
| Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors. |
| AID1520505 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells by luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity. |
| AID1152371 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1223449 | Drug metabolism in diabetic human kidney microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID693587 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
| AID279921 | Effect on HDL cholesterol level in cafteria-fed Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1743619 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID279932 | Decrease in cytochrome c oxidase activity in cafteria-fed Wistar rat inguinal adipose tissue at 70 mg/kg/day by DNA quantification assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID350158 | Therapeutic index, ratio of CC50 for human MT2 cells to EC50 for HIV1 3B | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents. |
| AID548800 | Antiviral activity against HIV1 isolate 192 harboring reverse transcriptase M41L/T215Y mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID284319 | Inhibition of bovine rotavirus RF infectivity following virus attachment to MA 104 cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-2-keto-beta-D-glucopyranosyl derivatives of N4-benzoyl cytosine. |
| AID1575286 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by measuring number of syncytia after 3 days by inverted microscopic method | 2019 | Journal of natural products, 01-25, Volume: 82, Issue:1
| 3,4- seco-Norclerodane Diterpenoids from the Roots of Polyalthia laui. |
| AID1884490 | Antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID611912 | Antiviral activity against Human immunodeficiency virus 1 assessed as inhibition of virus-induced cytopathic effects by cell based assay | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus. |
| AID79114 | Concentration required to inhibit HIV-1 replication in H9 lymphocyte cells | 2000 | Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
| Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues. |
| AID1815393 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID548799 | Antiviral activity against HIV1 isolate 188 harboring reverse transcriptase T215Y/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1565092 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | | | |
| AID548546 | Antiviral activity against HIV1 subtype B isolate Ba-L infected in human MDM after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID685330 | Antiviral activity against HIV-1 RES056 harboring RT K103N/Y181C mutant gene infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
| AID572984 | Cytotoxicity against human CEM cells after 2 to 4 days by MTT assay | 2009 | Antimicrobial 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. |
| AID538999 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by FACS analysis in presence of 10 % human serum | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
| Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds. |
| AID1226481 | Cytotoxicity against BHK cells infected with Dengue virus replicon assessed as cell viability at 10 uM after 3 days by CellTiter 96 aqueous one solution cell proliferation assay relative to control | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| 5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus. |
| AID21032 | Partition coefficient which is the ratio of its concentration in octanol to concentration in water | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and antiviral (HIV-1, HBV) activities of 5-halo-6-methoxy(or azido)-5,6-dihydro-3'-fluoro-3'-deoxythymidine diastereomers. Potential prodrugs to 3'-fluoro-3'-deoxythymidine. |
| AID291851 | Antiviral activity against HTLV1 in human PBMC at 25 uM | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID581051 | Increase in mitochondrial DNA level in differentiated mouse 3T3-F442A cells at 1 uM by real-time PCR | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Effects of zidovudine and stavudine on mitochondrial DNA of differentiating 3T3-F442a cells are not associated with imbalanced deoxynucleotide pools. |
| AID525111 | Antiviral activity against HIV 1 NL4.3 assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID354614 | Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of p24 antigen production after 4 days by ELISA | 1996 | Journal of natural products, Nov, Volume: 59, Issue:11
| Two new lignans, interiotherins A and B, as anti-HIV principles from Kadsura interior. |
| AID284318 | Antiviral activity against bovine rotavirus RF in MA 104 cells assessed as neutralization of virus in solution before cell attachment | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-2-keto-beta-D-glucopyranosyl derivatives of N4-benzoyl cytosine. |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1884229 | Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID409956 | Inhibition of mouse brain MAOB | 2008 | Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
| Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. |
| AID1238315 | Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay in presence of 5 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID470647 | Antiviral activity against HIV1 infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect | 2009 | Journal of natural products, Sep, Volume: 72, Issue:9
| Bioactive Nortriterpenoids from Schisandra grandiflora. |
| AID548536 | Antiviral activity against HIV1 subtype G isolate G3 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1141969 | Ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1763903 | Antiviral activity against HIV-1 IIIB harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID235006 | Compound was tested for anti HIV activity by measuring therapeutic index in H9 lymphocytes; IC50/EC50 | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| Anti-AIDS agents. 33. Synthesis and anti-HIV activity of mono-methyl substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogues. |
| AID718368 | Cytotoxicity against HIV2 ROD infected in human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
| AID267859 | Cytotoxicity against MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
| AID1368353 | Antiviral activity against HIV-1 3B infected in human TZM-bl cells at 10 uM treated simultaneously with viral infection for 2 hrs followed by compound washout measured after 2 days by luciferase reporter assay | 2018 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 28, Issue:1
| Synthesis and biological evaluation of water-soluble derivatives of chiral gossypol as HIV fusion inhibitors targeting gp41. |
| AID1687684 | Antiviral activity against HIV-1 RES056 mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
| AID222395 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 24 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID405582 | Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates. |
| AID681578 | TP_TRANSPORTER: uptake in OAT-K1-expressing MDCK cells | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
| Multispecific substrate recognition of kidney-specific organic anion transporters OAT-K1 and OAT-K2. |
| AID46046 | Inhibitory activity against the cytopathic effect of HIV-2 A17 (pyridinone-res) strain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID217743 | The compound was tested for toxicity in Vero cells | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID46375 | Antiviral activity against site directed 4X AZT resistant isolate HIV-1 in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID154939 | Toxicity against human peripheral blood mononuclear (PBM) cells | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents. |
| AID82064 | Visual cytotoxicity scored on HFF cells at time of HCMV plaque enumeration | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiproliferative and antiviral activity of 2'-deoxy-2'-fluoroarabinofuranosyl analogs of the nucleoside antibiotics toyocamycin and sangivamycin. |
| AID1141960 | Antiviral activity against HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1710786 | Cytotoxicity against African green monkey Vero cells assessed as changes in cell morphology incubated for 3 to 6 days by light microscopy | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID326389 | Antiviral activity against HIV1 3B in C8166 cells by syncytium reduction assay | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
| 1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro. |
| AID779526 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
| AID1204143 | Cytotoxicity against human HeLa cells after 48 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| PMA-SiO2 catalyzed synthesis of indolo[2,3-c]quinolines as potent anti cancer agents. |
| AID333025 | Inhibition of PKC epsilon | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2
| Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. |
| AID515990 | Cytotoxicity against human H9 cells after 6 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
| Anti-AIDS agents 84. Synthesis and anti-human immunodeficiency virus (HIV) activity of 2'-monomethyl-4-methyl- and 1'-thia-4-methyl-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) analogs. |
| AID1754639 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Antiviral activity against HIV-1 IIIB infected in human MT4 cells | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID617754 | Antiviral activity against HIV | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Synthesis and biological evaluation of 2',4'- and 3',4'-bridged nucleoside analogues. |
| AID1289720 | Inhibition of human TERT mRNA expression in human MGC803 cells at 3 mmol/L after 48 hrs by RT-PCR method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID1565091 | Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID1221966 | Ratio of plasma AUC in po dosed mdr1 knock out mouse to plasma AUC in po dosed wild type mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID47449 | Tested in vitro for anticancer activity against CEM cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID553577 | Antiviral activity against HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID271054 | Cytotoxicity against human MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID199660 | Inhibition of HIV-1 reverse transcriptase from peripheral blood mononuclear cells | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID45541 | Effective concentration against 50% survival of HIV -1 infected cells relative to uninfected untreated control (in vitro anti HIV-1 activity) | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity. |
| AID766740 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Synthesis and evaluation of novel 3-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents. |
| AID1199051 | Cytotoxicity against human MT4 cells assessed as inhibition of overall cell metabolism after 5 days by MTT assay | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID284150 | Inhibition of SIV-induced cytopathogenicity in CEM174 cells | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
| The design, synthesis, and biological evaluation of novel substituted purines as HIV-1 Tat-TAR inhibitors. |
| AID1231485 | Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
| AID575950 | Antiviral activity against Human immunodeficiency virus 1 ROJO infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1761016 | Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID155273 | Ability to inhibit the replication of RT-MDR (V106A) strain of HIV-1 p24 antigen production in PBMC | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
| N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. |
| AID279929 | Decrease in inguinal adipocyte size in cafteria-fed Wistar rat at 70 mg/kg/day | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID32066 | Required dose to reduce viability of normal uninfected ATH8 cells. | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID405342 | Toxicity against human H9c2 cells assessed as elevation of lactate levels at 50 uM after 6 days by NAD+ reduction assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID1457052 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID549088 | Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1632124 | Cytotoxicity against human MCF7 cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID645268 | Antiviral activity against HIV1 harboring VSV glycoprotein-G co-transfected with luciferase gene infected in human TZM-bl cells assessed as inhibition of viral replication after 48 hrs by microplate luminometer based luciferase assay | 2012 | European journal of medicinal chemistry, Apr, Volume: 50 | Hydroxyl may not be indispensable for raltegravir: Design, synthesis and SAR Studies of raltegravir derivatives as HIV-1 inhibitors. |
| AID83079 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 7 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1714435 | Selectivity index, ratio of CC50 for human PBMC to EC50 for inhibition of of HIV1 92US727 replication in PHA-P-stimulated human PBMCs | 2016 | Journal of medicinal chemistry, 12-08, Volume: 59, Issue:23
| Synthesis and Antiviral Evaluation of Octadecyloxyethyl Benzyl 9-[(2-Phosphonomethoxy)ethyl]guanine (ODE-Bn-PMEG), a Potent Inhibitor of Transient HPV DNA Amplification. |
| AID1053509 | Antiviral activity against AZT-resistant Human immunodeficiency virus 1 expressing D67N/K70R/T215F/K219Q reverse transcriptase mutation | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID523485 | Antiviral activity against HIV1 with RT connection domain L100I/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID103518 | Tested for intracellular levels of AZT phosphate against MCF-7 cell lines. | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
| Synthesis, in vitro anti-breast cancer activity, and intracellular decomposition of amino acid methyl ester and alkyl amide phosphoramidate monoesters of 3'-azido-3'-deoxythymidine (AZT). |
| AID89150 | Anti-HIV-1 activity against syncytial plaque formation at a conc. of 0.012 uM | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID16516 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into hippocampus | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID105522 | Concentration which reduced the cytopathic effect of HIV-1 in MT-4 infected cells | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
| Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs. |
| AID519962 | Selectivity ratio of EC50 for 0.05 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.05 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID630371 | Cytotoxicity against human KB cells assessed as cell survival after 72 hrs by sulforhodamine B colorimetric assay | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Synthesis and anticancer activity of 5'-chloromethylphosphonates of 3'-azido-3'-deoxythymidine (AZT). |
| AID681577 | TP_TRANSPORTER: uptake in OAT-K2-expressing MDCK cells | 2001 | The Journal of pharmacology and experimental therapeutics, Oct, Volume: 299, Issue:1
| Multispecific substrate recognition of kidney-specific organic anion transporters OAT-K1 and OAT-K2. |
| AID154933 | Effective conc. required to achieve 50% inhibition of HIV-2 D194 multiplication in PBM (peripheral blood mononuclear) cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID15236 | Percentage of radioactivity in P2 subregion in mouse brain that contains myelin fragments, synaptosomes (pinched-nerve endings), and mitochondria after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID19636 | Partition coefficient (logP) (1-pentanol) | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| Design, synthesis, and structure-activity relationship of novel dinucleotide analogs as agents against herpes and human immunodeficiency viruses. |
| AID1053512 | Therapeutic index, ratio of CC50 for human CEM-SS cells to EC50 for Human immunodeficiency virus 1 3B | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID152628 | Antiviral activity against HIV-1xxBRU mutant strain in human PBM cells | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
| Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID1763899 | Antiviral activity against HIV-1 IIIB harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID548563 | Antiviral activity against HIV1 8415-2 harboring reverse transcriptase 65R/184V mutant gene infected in human PBMC by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID78761 | Anti-HIV activity was measured in H9-cells. | 1998 | Journal of medicinal chemistry, Nov-05, Volume: 41, Issue:23
| Anti-AIDS agents. 34. Synthesis and structure-activity relationships of betulin derivatives as anti-HIV agents. |
| AID202327 | Tested in vitro for anticancer activity against SK-MES-1 cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID548574 | Antiviral activity against HIV1 isolate 060 harboring reverse transcriptase M41L/D67N/K70R/L210W/T215Y/K219E mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID548837 | Antiviral activity against HIV1 isolate 211 harboring reverse transcriptase D67N/K70R/T215F/K219E/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID224947 | Compound was tested for anti-HIV activity in normal peripheral blood mononuclear cells infected with HIV-2 virus by inhibition of reverse transcriptase activity | 1998 | Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
| Enhancing effects of a mono-bromo substitution at the para position of the phenyl moiety on the metabolism and anti-HIV activity of d4T-phenyl methoxyalaninyl phosphate derivatives. |
| AID1285845 | Antiviral activity against HIV1 74V infected in human C8166 cells assessed as reduction in p24 antigen level incubated for 4 hrs followed by cell plating for 72 hrs by ELISA method | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
| Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors. |
| AID1316803 | Antiviral activity against HIV-1 3B infected in human MT-4 cells assessed as protection against virus induced cytopathic effect after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
| AID79123 | Concentration which was toxic to 50% of the mock-infected H9 lymphocyte. | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24
| Synthesis and anti-HIV activity of oleanolic acid derivatives. |
| AID43940 | Compound was tested for inhibitory activity against erythroid (BFU-E) progenitor cells | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID519893 | Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID607808 | Antiviral activity against Human immunodeficiency virus 2 ROD infected in C8166 cells assessed as reduction in virus-induced cytopathic effect after 3 days by syncytium reduction assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1200843 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
| AID52553 | Inhibitory activity based on the inhibition of [Ca2+] mobilization induced by human SDF-1alpha stimulation through CXCR4; N.T. means not tested | 2002 | Bioorganic & medicinal chemistry letters, Mar-25, Volume: 12, Issue:6
| Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety. |
| AID417052 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine monophosphate level at 600 mg administered in two courses, first BID for 7 to 14 days followed by QD for 7 days and second course the subjects were switched to the other regimen measured pe | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID662535 | Cytotoxicity against human MT4 cells assessed as reduction of cell viability | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| Pharmacophore-based small molecule CXCR4 ligands. |
| AID576384 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 0.78 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1565100 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID235027 | Therapeutic index (IC50/EC50) of compound was determined in acutely infected H9 cell | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Anti-AIDS agents. Part 47: Synthesis and anti-HIV activity of 3-substituted 3',4'-Di-O-(S)-camphanoyl-(3'R,4'R)-(+)-cis-khellactone derivatives. |
| AID665550 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12
| Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
| AID89030 | Effective antiviral dose required to block the spread of HIV-1D34 infection in human peripheral blood mononuclear cells | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID99154 | Inhibitory effect of compound on the proliferation of murine leukemia cells L1210/0. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID222686 | In Vivo detection of total AZT in Mice plasma after oral administration of 20 mg/kg after 0.5 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1597909 | Antiviral activity against FIV infected in cat FL-4 cells assessed as reduction in viral RNA level measured after 7 days by qRT-PCR analysis | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID1191399 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
| Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID1157582 | Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID481801 | Activity of human TK1 relative to ATP | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID81266 | Effective concentration against HIV-1 | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| New manzamine alkaloids from an Indo-Pacific sponge. Pharmacokinetics, oral availability, and the significant activity of several manzamines against HIV-I, AIDS opportunistic infections, and inflammatory diseases. |
| AID1197829 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
| AID1221976 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID685333 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
| AID214083 | Antiviral activity was determined in chronically infected U1 cell line with HIV-1 | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID449492 | Selective index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
| Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID104577 | Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50% | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| A new class of HIV-1-specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). |
| AID104240 | In vitro Cytotoxic concentration which destroyed HIV-1 LAV infected MT-2 cells completely | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID231375 | Ratio of CD50/ED50 | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5
| Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides. |
| AID287285 | Cytotoxicity against human CEM cells after 6 days | 2007 | Bioorganic & medicinal chemistry, Feb-01, Volume: 15, Issue:3
| Synthesis and biological evaluation of novel 5(H)-phenanthridin-6-ones, 5(H)-phenanthridin-6-one diketo acid, and polycyclic aromatic diketo acid analogs as new HIV-1 integrase inhibitors. |
| AID569223 | Cytotoxicity against human CEM-GFP cells after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
| Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5. |
| AID46002 | 50% effective concentration of compound which is required to protect human CEM cells against HIV-2 induced giant cell formation. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID1888701 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID8449 | Tested in vitro for anticancer activity against 9L cells; Not determined | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID279930 | Decrease in epididymal adipocyte size in cafteria-fed Wistar rat at 70 mg/kg/day | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID284151 | Cytotoxicity against CEM174 cells | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
| The design, synthesis, and biological evaluation of novel substituted purines as HIV-1 Tat-TAR inhibitors. |
| AID717257 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID573997 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for MK-0518-resistant Human immunodeficiency virus harboring G140S and Q148H mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID1060629 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs. |
| AID572778 | Ratio of IC50 for HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID79440 | Tested for in vitro therapeutic index as the ratio of IC50 to EC50 in acutely infected H9 Lymphocytes | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
| Anti-AIDS agents. 15. Synthesis and anti-HIV activity of dihydroseselins and related analogs. |
| AID217733 | Evaluated in vitro for their potential toxic effects against Vero cells | 2003 | Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
| Synthesis, anti-HIV activity, and molecular mechanism of drug resistance of L-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID1743621 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID79299 | Concentration required to inhibit HIV-1 replication by 50% in acutely infected H9 lymphocytes | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| Anti-AIDS agents. Part 58: synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues. |
| AID100404 | The compound was tested in vitro for anticancer activity against LNCaP cells; Not determined | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID1483271 | Inhibition of HIV1 3B reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID222490 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 0.5 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID584615 | Toxicity in human subcutaneous preadipocytes assessed as decrease of cell cultures at 6 uM after 30 days using oil red O fluorescence staining by conventional fluorescence microscopy | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID83230 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID152615 | In vitro anti-HIV activity was determined in PBM cells infected with HIV-1 | 2003 | Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
| Synthesis, anti-HIV activity, and molecular mechanism of drug resistance of L-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID279926 | Increase in plasma insulin level in lean Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID357034 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7
| Anti-AIDS agents. 46. Anti-HIV activity of harman, an anti-HIV principle from Symplocos setchuensis, and its derivatives. |
| AID78942 | Inhibitory activity against HIV-1 replication in mock infected H9 cells | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents. |
| AID84778 | Antiviral activity against Herpes simplex virus type-2 | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID519965 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT infected in human MT2 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1220789 | Ratio of drug level in blood to plasma in mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID79112 | Antiviral activity against HIV-1(IIIB) infected H9 cell lines. | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24
| Synthesis and anti-HIV activity of oleanolic acid derivatives. |
| AID1635806 | Fold resistance, ratio of EC50 for raltegravir-resistant HIV1 1556-1 expressing integrase Y143C mutant to EC50 for HIV1 expressing wild-type integrase | 2016 | Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
| 3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H. |
| AID1460937 | Antiviral activity against wild type HIV-1 NL4-3 infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID1884492 | Antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID584634 | Toxicity in human subcutaneous preadipocytes assessed as decrease of C/EBPalpha expression at 6 uM after 18 days by RT-PCR analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID548543 | Cytotoxicity against human PBMC up to 1000 nM by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID32219 | Minimum inhibitory concentration of the compound, achieving a complete protection of ATH8 cells against the cytopathic effect of HTLV-III / LAV reverse transcriptase | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
| Chemotherapeutic approaches to the treatment of the acquired immune deficiency syndrome (AIDS). |
| AID575952 | Antiviral activity against Human immunodeficiency virus 1 TEKI infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1316339 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID83214 | Compounds were evaluated for anti-RT activity by MTT dose and % cell / viability was reported at 7 days of culture | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID287872 | Selectivity index, Ratio of CC50 for human Caco-2 cells to IC50 for rotavirus RF in human Caco2 cells after neutralization of virus in solution before infection | 2007 | Bioorganic & medicinal chemistry, May-01, Volume: 15, Issue:9
| An efficient synthesis of 3-fluoro-5-thio-xylofuranosyl nucleosides of thymine, uracil, and 5-fluorouracil as potential antitumor or/and antiviral agents. |
| AID1357789 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID1729156 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID235904 | Selectivity index expressed as ratio of IC50 (CEM-C113) to EC50 from MTT assay | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
| Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs. |
| AID1457059 | Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID42621 | Compound was tested for Anti-HIV activity by plaque reduction assay with E89K virus in HT4-6C human CD4+ lymphocytes | 1997 | Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
| Synthesis and in vitro activity of long-chain 5'-O-[(alkoxycarbonyl)phosphinyl]-3'-azido-3'-deoxythymidines against wild-type and AZT- and foscarnet-resistant strains of HIV-1. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1594066 | Inhibition of nucleocapsin protein in FIV infected in cat FL-4 cells assessed as reduction in viral RNA replication measured after 7 days by qRT-PCR analysis | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Synthesis and comparison of substituted 1,2,3-dithiazole and 1,2,3-thiaselenazole as inhibitors of the feline immunodeficiency virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID1761014 | Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID79110 | Compound was evaluated for antiviral activity against H9 cells. Cell culture inhibitor concentration (CIC95) is defined as those which inhibited by >95% the spread of HIV-1 IIIb infection in susceptible cell culture | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
| Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one. |
| AID581776 | Antiviral activity against HIV-1 3B infected in human PBMC assessed as inhibition of viral replication by ELISA | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent. |
| AID46197 | Inhibitory effect against HIV-1 replication in CEM cells. | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
| Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase. |
| AID1304538 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in viral replication measured on day 3 post infection by luciferase reporter gene assay | 2016 | Journal of natural products, Mar-25, Volume: 79, Issue:3
| Carolignans from the Aerial Parts of Euphorbia sikkimensis and Their Anti-HIV Activity. |
| AID1597907 | Acute cytotoxicity against cat CRFK cells assessed as decrease in cell viability at 10 uM measured after 24 hrs by MTT assay relative to control | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID330488 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID571599 | Ratio of AUC (0 to 12 hrs) in HIV-1 infected patient at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir to AUC (0 to 12 hrs) in HIV-1 infected patient at 200 mg, po bid on day 1 coadministered with 500 mg, po bid amdoxovir | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1220787 | Fraction unbound in dog plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID493819 | Therapeutic index, ratio of CC50 for human CEM cells expressing green fluorescent protein to IC50 for HIV1 NL4.3 | 2010 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
| Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus. |
| AID1152372 | Antiviral activity against HIV1 RES056 harboring RT K103N,Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID21905 | Concentration in mouse blood 20 min post injection at a dose 240 mocromol/kg | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID470648 | Cytotoxicity against human C8166 cells by MTT assay | 2009 | Journal of natural products, Sep, Volume: 72, Issue:9
| Bioactive Nortriterpenoids from Schisandra grandiflora. |
| AID46001 | 50% effective concentration of compound which is required to protect human CEM cells against HIV-1 induced giant cell formation. | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID1356066 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay | 2018 | Journal of natural products, 07-27, Volume: 81, Issue:7
| Kleinhospitine E and Cycloartane Triterpenoids from Kleinhovia hospita. |
| AID1888692 | Selectivity index, ratio of CC50 for toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induc | | | |
| AID1391086 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID46007 | Anti-HIV activity against HIV-I RFII strain in CEM cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID3044 | Compound was evaluated for the inhibition of cell replication human peripheral blood lymphocytes (PBL's). | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Novel acyclonucleotides: synthesis and antiviral activity of alkenylphosphonic acid derivatives of purines and a pyrimidine. |
| AID732657 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV-1 3B infected in human C8166 cells | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Antiviral phenolic compounds from Arundina gramnifolia. |
| AID548810 | Antiviral activity against HIV1 isolate 217 harboring reverse transcriptase D67N/K70E/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID431619 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID1483269 | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID1483283 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y188L mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID1761019 | Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID152780 | Inhibitory activity was evaluated in human peripheral blood mononuclear (PBM) cells infected with Human immunodeficiency virus-1 | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
| Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2', 3'-unsaturated L-nucleosides. |
| AID289143 | Cytotoxicity against MT2 cells | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs. |
| AID279925 | Effect on ratio of total cholesterol to HDL cholesterol in cafteria-fed Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID226288 | ratio of Ki (Ki TMPKh / KiTMPKmt); not determined | 2003 | Journal of medicinal chemistry, Aug-28, Volume: 46, Issue:18
| 3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase. |
| AID1174086 | Cytotoxicity against human CEM cell | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs. |
| AID1443664 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID154799 | Antiviral activity against subtype isolate A strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Hologram QSAR model for the prediction of human oral bioavailability. |
| AID401233 | Antiviral activity against HSV2 | 2004 | Journal of natural products, Apr, Volume: 67, Issue:4
| Isolation of salicin derivatives from Homalium cochinchinensis and their antiviral activities. |
| AID106916 | Anti-HIV activity against HIV-I A17 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID548567 | Selectivity ratio of EC50 for HIV1 1617-1 harboring reverse transcriptase 69K/70G/75I/77L/116Y/151M/184V mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID619640 | Antiviral activity against HIV-1 3B harboring RT K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID619639 | Antiviral activity against HIV-1 3B harboring RT F227L and V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID583445 | Cytotoxicity against human HepG2 cells assessed as increase in extracellular lactate secretion at 50 uM after 15 days relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID46017 | Compound was evaluated for anti-HIV activity against thymidine kinase deficient CEM cell line infected with HIV-1 | 1998 | Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9
| Anti-HIV pronucleotides: decomposition pathways and correlation with biological activities. |
| AID235634 | Selectivity index is the ratio of CC50/EC50 | 1989 | Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
| A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID44791 | Effective dose to achieve 50% protection of C8166 cells acutely infected with HIV-2 strain IIIB | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Decomposition pathways and in vitro HIV inhibitory effects of isoddA pronucleotides: toward a rational approach for intracellular delivery of nucleoside 5'-monophosphates. |
| AID676992 | Antiplasmodial activity against Plasmodium falciparum 3D7 ring stage cells assessed as reduction parasitemia by Malstat assay | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
| Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID269763 | Antiviral activity against HIV1 TEKI | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
| Azadideoxyadenosine: synthesis, enzymology, and anti-HIV activity. |
| AID235562 | Selectivity Index measured as ratio of CC50 to that of EC50 in PBMCs | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
| Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils. |
| AID46442 | Compound was tested for inhibitory activity against HIV-1 replication in CEM-SS cells | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Rational design of a new series of mixed anti-HIV pronucleotides. |
| AID1406278 | Cytotoxicity against human MT4 cells after 3 days by CytoTox-Glo assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Identification, structural modification, and dichotomous effects on human immunodeficiency virus type 1 (HIV-1) replication of ingenane esters from Euphorbia kansui. |
| AID698300 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID330490 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES053 | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
| Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID732659 | Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of syncytia formation after 3 days | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Antiviral phenolic compounds from Arundina gramnifolia. |
| AID584612 | Toxicity in fully differentiated human subcutaneous preadipocytes assessed as cell death at 6 uM after 30 days using oil red O fluorescence staining by conventional fluorescence microscopy | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID105349 | Tested for the inhibitory activity of HIV-2 infected MT-4 cells | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| 1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity. |
| AID46767 | In vitro antiviral activity against CEM cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID1199052 | Antiviral activity against Human immunodeficiency virus 1 3b infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay | 2014 | Journal of natural products, Jun-27, Volume: 77, Issue:6
| Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead. |
| AID572975 | Ratio of IC50 for HIV1 harboring reverse transcriptase D67N/K70R/T215F/K219Q mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID693583 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
| AID525107 | Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID257166 | Antiviral activity against wild type HIV1 NL4-3 infected MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
| AID1447284 | Cytotoxicity against human P4R5 MAGI cells after 2 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
| Synthesis and anti-HIV activities of unsymmetrical long chain dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID519873 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID377705 | Antibacterial activity against Mycobacterium intracellular by alamar blue assay | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7
| Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID16520 | Distribution of analyte (pmol/mg) in mouse brain regions after Jugular Vein Injection into striatum | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID47111 | In vitro inhibition of HIV-1 replication in human T-lymphocytic cells (CEM). | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID81240 | Compound was evaluated for the antiviral activity against compound resistant virus isolate M184I with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID1228737 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1-3B | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5
| Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID1186008 | Antiviral activity against HIV1 infected in 293T cells assessed as time of 50% failure | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
| AID405343 | Toxicity against human HepG2/C3A cells assessed as increase in mitochondrial superoxide production at 50 uM by flow cytometry | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID32831 | Inhibitory activity against HIV in Alex cells | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and antiviral activity of some acyclic and C-acyclic pyrrolo[2,3-d]pyrimidine nucleoside analogues. |
| AID576141 | Antiviral activity against Human immunodeficiency virus 1 subtype G JV 1083 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID525102 | Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID417236 | Half life in HIV-infected human assessed as zidovudine triphosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1275544 | Antiviral activity against HIV1 3B expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
| AID635345 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
| AID83265 | Effective concentration required for antiviral activity against HIV strain 205 by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID235793 | Selectivity index was determined in C8166 cells | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
| AID332930 | Cytotoxicity against human H9 cells after 3 days | 1994 | Journal of natural products, Jan, Volume: 57, Issue:1
| Anti-AIDS agents, 10. Acacetin-7-O-beta-D-galactopyranoside, an anti-HIV principle from Chrysanthemum morifolium and a structure-activity correlation with some related flavonoids. |
| AID377972 | Cytotoxicity against human H9 cells | 1999 | Journal of natural products, Jan, Volume: 62, Issue:1
| Novel anti-HIV lancilactone C and related triterpenes from Kadsura lancilimba. |
| AID47336 | Compound was tested for inhibitory activity against human myeloid cells (CFU-GM) | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID542936 | Antiproliferative activity against mouse 3T3-F442A cells assessed as [3H]thymidine incorporation at 6 uM | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1316807 | Selectivity index, ratio of CC50 for human MT-4 cells to IC50 for HIV-2 ROD infected in human MT-4 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
| AID291850 | Antiviral activity against HTLV1 in human PBMC at 100 uM | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID574200 | Cytotoxicity against human skeletal muscle Myoblast at 100 uL on day 5 by WST-1 assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID576144 | Antiviral activity against Human immunodeficiency virus 1 subtype O BCF03 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID47474 | Percent reduction in p24 gag expression in CEM cells | 1990 | Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
| Synthesis and anti-HIV activity of carbocyclic 2',3'-didehydro-2',3'-dideoxy 2,6-disubstituted purine nucleosides. |
| AID1888694 | Antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID234033 | Therapeutic Index (IC50/EC50) of the compound | 2001 | Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
| 3,28-Di-O-(dimethylsuccinyl)-betulin isomers as anti-HIV agents. |
| AID1289718 | Inhibition of human TERT-regulated Wnt/beta-catenin signalling in human MGC803 cells assessed as decrease in cyclin-D1 mRNA expression at 3 mmol/L after 48 hrs by RT-PCR method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID232768 | Selectivity index of IC50 and CD50 of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1). |
| AID512144 | Therapeutic index, ratio of IC50 for human CEM cells to EC50 for HIV1 | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
| Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents. |
| AID417259 | Cmax in HIV-infected human assessed as zidovudine triphosphate level in PBMC at 600 mg QD for 7 days measured per 10'6 cells in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1352312 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID83070 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 10 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1483286 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID81089 | Anti-HIV activity was determined | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Structure-activity relationships of 2'-fluoro-2',3'-unsaturated D-nucleosides as anti-HIV-1 agents. |
| AID45853 | Cytotoxic concentration against HIV-1 infected CEM cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID1275543 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID377706 | Antiviral activity against HIV1 3B assessed as reverse transcriptase activity by enzyme immunoassay | 2006 | Journal of natural products, Jul, Volume: 69, Issue:7
| Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases. |
| AID300148 | Antiviral activity against Rotavirus RF in human Caco-2 cells assessed as inhibition of infectivity following virus attachment after 72 hrs | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID83063 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1165074 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
| AID153144 | Effective concentration required to inhibit the replication of HIV-1 with no pretreatment of activated PBMCs | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID376817 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Bioactive kaurane diterpenoids from Annona glabra. |
| AID1406279 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 NL4-3 infected in human MT4 cells | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Identification, structural modification, and dichotomous effects on human immunodeficiency virus type 1 (HIV-1) replication of ingenane esters from Euphorbia kansui. |
| AID1410484 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B reverse transcriptase infected in human MT4 cells | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
| AID548303 | Antiviral activity against HIV1 subtype A isolate 92UG029 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID584817 | Toxicity in human subcutaneous preadipocytes assessed as effect on mitochondrial mass at 6 uM after 30 days using JC-1 red/green fluorescence dye by flow cytometry analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID89000 | In vitro inhibition of HIV-1 plaque formation | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| In vitro evaluation of phosphocholine and quaternary ammonium containing lipids as novel anti-HIV agents. |
| AID104938 | Cytotoxic concentration required to reduce the viability of mock-infected MT-4 cells by 50% | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID431621 | Cytotoxicity against human MT4 cells by MTT assay | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID675191 | Cytotoxicity against human PBMC | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID452271 | Cytotoxicity against human CEM cells after 5 days | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus. |
| AID104935 | In vitro antiviral activity against (monocyte macrophages) cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID1209583 | Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
| AID199981 | Inhibition of HIV-1 reverse transcriptase; + = active | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID1572520 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | | | |
| AID216188 | Tested in vitro for cytotoxicity against Vero cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID1304409 | Antiviral activity against HIV-1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID1517758 | Therapeutic index, ratio of CC50 for human CEM-GFP cells to IC50 for antiviral activity against HIV-1 NL4-3 infected in human CEM-GFP cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-isoxazol-3-yl-acetamide analogues as heat shock protein 90 (HSP90) inhibitors with significant anti-HIV activity. |
| AID269765 | Cytotoxicity against human PBMC | 2006 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 16, Issue:15
| Azadideoxyadenosine: synthesis, enzymology, and anti-HIV activity. |
| AID201966 | The compound was tested in vitro for anticancer activity against SK-MEL-28 cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID578847 | Antiviral activity against Human immunodeficiency virus 1 LAI infected in human PBMC assessed as inhibition of viral replication after 5 days by reverse transcriptase assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors. |
| AID235201 | Therapeutic index expressed as IC50/EC50 | 2004 | Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
| Anti-AIDS agents. Part 58: synthesis and anti-HIV activity of 1-thia-di-O-(-)-camphanoyl-(+)-cis-khellactone (1-thia-DCK) analogues. |
| AID389378 | Antiviral activity against HIV1 3B in human MT4 cells assessed as protection of cell against virus-induced cytopathogenicity | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID373361 | Drug metabolism in human CEM cells assessed as radioactive zidovudine diphosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID341350 | Metabolic stability of the compound in human CD4+ CEM cells assessed as 3'-azido-2',3'-dideoxythymidine diphosphate intracellular levels at 200 nM after 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID106971 | Concentration required to inhibit the cytopathicity of HIV-1 strain BRU by 50% in MT-4 cells (expressed in AZT equivalent) | 2002 | Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
| Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities. |
| AID1443669 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID46371 | Anti-HIV activity against HIV-I RFII strain in CEM cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID216020 | Cytotoxic concentration against Vero cells was determined on day 3 | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID1068978 | Cytotoxicity against human MT4 cells | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents. |
| AID361400 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2002 | Journal of natural products, Nov, Volume: 65, Issue:11
| New saponins from the starfish Certonardoa semiregularis. |
| AID1884541 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID104980 | Dose required to achieve 50% protection of MT-4 cells from HIV-1 induced cytopathogenicity | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. |
| AID693585 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
| AID228281 | Compound was evaluated for the cytotoxic activity by using Microculture Tetrazolium assay (MTA) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
| N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. |
| AID154794 | Antiviral activity against ROJO virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID83078 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 21 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID678994 | TP_TRANSPORTER: uptake in Xenopus laevis oocytes | 2000 | Biochemical pharmacology, Jul-15, Volume: 60, Issue:2
| Role of organic cation transporters in the renal secretion of nucleosides. |
| AID279924 | Effect on ratio of total cholesterol to HDL cholesterol in lean Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID83394 | Antiviral activity against Human immunodeficiency virus type-1 | 1999 | Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
| Nucleosides and nucleotides. 185. Synthesis and biological activities of 4'alpha-C-branched-chain sugar pyrimidine nucleosides. |
| AID1589124 | Selectivity index, ratio of IC50 for cytotoxicity in human NHDF cells to IC50 for cytotoxicity in human KB cells | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1457060 | Ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID1298246 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
| AID155270 | Ability to inhibit the replication of A17 variant (Y181C,K103N) strain of HIV-1 p24 antigen production in PBMC | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
| N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. |
| AID152625 | Tested in vitro for anti HIV-1 activity against PBM cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID373572 | Binding affinity to TK1 in human H9 cells assessed as conversion of [14C]thyminide to [14C]thymidine monophosphate by scintillation counting | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID572783 | Antiviral activity against HIV1 harboring reverse transcriptase M41L/D67N/K70R/T215F/K219Q mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID217719 | Compound was evaluated for its cytotoxicity against vero cells. | 1998 | Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
| Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine. |
| AID155467 | The compound was tested for toxicity in peripheral blood mononuclear cells | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID572972 | Antiviral activity against HIV1 harboring reverse transcriptase diserine insert between residues 69 and 70 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID619634 | Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID548824 | Antiviral activity against HIV1 isolate 162 harboring reverse transcriptase A62V/V75I/F77L/Y115F/F116Y/Q151M/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID320325 | Antiviral activity against wild type HIV1 3B in MT2 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor. |
| AID519856 | Antiviral activity against pseudotype HIV1 NL-RLuc infected in human MT2 cells measured on day 5 postinfection by luciferase reporter gene assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1289704 | Inhibition of human TERT-regulated Wnt/beta-catenin signalling in human MGC803 cells assessed as decrease in beta-catenin protein expression at 3 mmol/L after 48 hrs by Western blotting method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID235682 | Selectivity Index measured as the ratio of CC50 to that of EC50(HIV-2) values. | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiviral activity of 8-aza analogs of chiral [2-(phosphonomethoxy) propyl]guanines. |
| AID456304 | Cytotoxicity against human MT4 cells by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands. |
| AID1172371 | Cytotoxicity against human H460 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID736855 | Antiviral activity against HIV1 assessed as reduction in virus-induced cytopathogenicity | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Dibenzocyclooctadiene lignans and norlignans from fruits of Schisandra wilsoniana. |
| AID417049 | Drug metabolism in HIV-infected human PBMC assessed as zidovudine diphosphate level at 600 mg administered in two courses, first QD for 7 days followed by BID for 7 to 14 days and second course the subjects were switched to the other regimen measured per | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1320863 | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
| AID1165075 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
| AID1457759 | Selectivity ratio of EC50 for tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells to EC50 for CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
| Expanding the Antiviral Spectrum of 3-Fluoro-2-(phosphonomethoxy)propyl Acyclic Nucleoside Phosphonates: Diamyl Aspartate Amidate Prodrugs. |
| AID46975 | In vitro cytotoxic concentration in CEM cells. | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2',3'-dideoxyadenosine and 2', 3'-dideoxy-2',3'-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system. |
| AID583437 | Cytotoxicity against human HepG2 cells assessed as reduction in viable cells at 50 uM after 6 days by trypan blue dye exclusion assay relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID618860 | Cytotoxicity against african green monkey Vero cells after 3 days by hemocytometry | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides. |
| AID558388 | Ratio of drug level in HIV-infected pregnant woman cord blood plasma to maternal blood plasma at 300 mg, po BID by LC/MS/MS analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID310349 | Antiviral activity against HIV1 | 2007 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 17, Issue:23
| Anti-AIDS agents 73: structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. |
| AID308282 | Cytotoxicity against H9 cells assessed as growth inhibition | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Anti-AIDS agents 72. Bioisosteres (7-carbon-DCKs) of the potent anti-HIV lead DCK. |
| AID499276 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
| Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
| AID235697 | Selectivity index is defined as CC25(H9 cells) / CC50(H9 cells) | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID45990 | Cytotoxic concentration required to inhibit 50% of HIV-1 in CEM cells | 1997 | Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21
| Probing the mechanism of action and decomposition of amino acid phosphomonoester amidates of antiviral nucleoside prodrugs. |
| AID548829 | Antiviral activity against HIV1 isolate 188 harboring reverse transcriptase T215Y/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID717256 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs. |
| AID548817 | Antiviral activity against HIV1 isolate 067 harboring reverse transcriptase A62V/D67G/T69SVG/V75I/T215I mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1316340 | Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID481800 | Activity of Ureaplasma parvum thymidine kinase relative to dThd | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID718523 | Antiviral activity against HIV-2 ROD infected in MT4 cells assessed as inhibition of virus-induced cytopathicity | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| POMA analyses as new efficient bioinformatics' platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues. |
| AID46823 | Antiviral activity was measured on HIV-2 in wild-type CEM/O cells | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| cycloSal-2',3'-dideoxy-2',3'-didehydrothymidine monophosphate (cycloSal-d4TMP): synthesis and antiviral evaluation of a new d4TMP delivery system. |
| AID472248 | Antiviral activity against HIV1 NL4-3 co-transfected with VSV glycoprotein plasmid in human 293T cells after 48 hrs by luciferase reporter gene assay | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6
| Chemical constituents of Heteroplexis micocephala. |
| AID1203626 | Induction of apoptosis in human 5637 cells assessed as DNA fragmentation at 50 to 100 uM after 48 hrs by TUNEL assay relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID155460 | Inhibitory effect on p24 production in HIV-infected peripheral blood mononuclear cells. | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| Structure-based design of N-[2-(1-piperidinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID284321 | Cytotoxicity against human Caco-2 cells after 72 hrs | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-2-keto-beta-D-glucopyranosyl derivatives of N4-benzoyl cytosine. |
| AID199849 | Antiviral activity against Human Immunodeficiency Virus by Reverse transcriptase assay in CEM-SS cells | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole. |
| AID624612 | Specific activity of expressed human recombinant UGT1A9 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
| AID492209 | Antiviral activity against HIV1 BAL by p24 assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Discovery of orally available spirodiketopiperazine-based CCR5 antagonists. |
| AID106024 | Compound was evaluated for the inhibition of cell replication of human fibroblast (MRC-5) cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Novel acyclonucleotides: synthesis and antiviral activity of alkenylphosphonic acid derivatives of purines and a pyrimidine. |
| AID1157587 | Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID429826 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6
| Lignans with anti-HIV activity from Schisandra propinqua var. sinensis. |
| AID481803 | Activity of human TK1 by Michaelis-Menten plot | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID1261365 | Antiviral activity against HIV1 infected in human peripheral blood mononuclear cells assessed as inhibition of reverse transcriptase activity incubated for 6 days | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of dihydropyrimidine α,γ-diketobutanoic acid derivatives targeting HIV integrase. |
| AID104970 | Antiviral activity in MT-4 cell line infected with HIV-1 and Concentration required to inhibit the replication of HIV-1 by 50% was determined | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID152652 | Evaluated in vitro for their potential toxic effects on uninfected PHA-stimulated human PBM cells | 2003 | Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
| Synthesis, anti-HIV activity, and molecular mechanism of drug resistance of L-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID373362 | Drug metabolism in human CEM cells assessed as radioactive zidovudine triphosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID1348220 | Antiviral activity against HIV1 pNL4-3 infected in HEK293 cells assessed as reduction in viral transcription by measuring decrease in luciferase activity at 1 uM after 20 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
| AID1077223 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID125500 | Inhibitory effect of compound on the proliferation of human T-lymphocyte cells Molt4/C8 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID405340 | Toxicity against human HepG2/C3A cells assessed as elevation of lactate levels at 50 uM after 6 days by NAD+ reduction assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID1443660 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID291762 | Antiviral activity against HIV1 assessed as syncytium reduction | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro. |
| AID581055 | Cytotoxicity against differentiated mouse 3T3-F442A cells assessed as increase in TTP content after 10 days | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Effects of zidovudine and stavudine on mitochondrial DNA of differentiating 3T3-F442a cells are not associated with imbalanced deoxynucleotide pools. |
| AID83071 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 14 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1815388 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID736854 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Dibenzocyclooctadiene lignans and norlignans from fruits of Schisandra wilsoniana. |
| AID542932 | Induction of preadipocyte differentiation in mouse 3T3L1 cells assessed as C/EBPalpha mRNA expression on day 4 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID42393 | Concentration which results in 50% survival of uninfected untreated control C8166 cells (cytotoxicity of the compound) | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
| AID614142 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
| AID81239 | Compound was evaluated for the antiviral activity against compound resistant virus isolate L100I with amino acid changes in the HIV-1 reverse transcriptase (RT) | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI. |
| AID489453 | Cytotoxicity against human MT2 cells by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14
| Synthesis and anti-HIV activity of 2'-deoxy-2'-fluoro-4'-C-ethynyl nucleoside analogs. |
| AID279937 | Decrease in fatty acid synthase activity in lean Wistar rat epididymal adipose tissue assessed at 70 mg/kg/day by DNA quantification assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID47445 | In vitro cytotoxicity in CEM cells. | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
| Enantiomeric synthesis of D- and L-cyclopentenyl nucleosides and their antiviral activity against HIV and West Nile virus. |
| AID232053 | Selectivity index is the ratio of CC50 to EC50 | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID1203625 | Induction of apoptosis in human 5637 cells at 50 uM after 48 hrs by annexin V-PE/7-AAD staining-based flow cytometric analysis (Rvb = 7.36%) | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID487828 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of viral p24 antigen production after 6 days by ELISA | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Anti-AIDS agents 82: synthesis of seco-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents. |
| AID1238310 | Cytotoxicity against human MT4 cells by MTT assay in presence of 2.5 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID548304 | Antiviral activity against HIV1 subtype A isolate 92UG037 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID572782 | Antiviral activity against HIV1 harboring reverse transcriptase M41L/L210W/T215Y mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1197830 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
| AID257173 | Cytotoxicity against MT4 cells by MTT method | 2005 | Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
| Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity. |
| AID83398 | Evaluated in vitro for the concentration required to produce 50% inhibition of replication of HIV-1 | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Synthesis and biological evaluation of prodrugs of zidovudine. |
| AID333020 | Therapeutic index, IC50 for human H9 cells to EC50 for HIV1 3B | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2
| Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. |
| AID335637 | Antiviral activity against HIV1 3B replication in human C8166 cells at 100 uM after 5 to 7 days by MTT-formazan method | 1992 | Journal of natural products, Aug, Volume: 55, Issue:8
| Constituents of Eriobotrya japonica. A study of their antiviral properties. |
| AID456309 | Antiviral activity against HIV1 BaL infected in human PBMC assessed as inhibition of viral replication by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands. |
| AID422691 | Ratio of IC50 for HIV1 with reverse transcriptase K70E/M184V mutation to IC50 for wild type HIV1 | 2007 | Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
| Novel drug resistance pattern associated with the mutations K70G and M184V in human immunodeficiency virus type 1 reverse transcriptase. |
| AID439738 | Inhibition of Influenza A virus (A/Bar-headed Goose/Qinghai/59/05(H5N1)) hemagglutininin-mediated viral entry into human A549 cells assessed as luciferase activity after 48 hrs postinfection by luminometry | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of the first series of small molecule H5N1 entry inhibitors. |
| AID1220799 | Drug metabolism in gallbladder-cannulated mouse assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID662534 | Antiviral activity against X4-tropic HIV1 NL4.3 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| Pharmacophore-based small molecule CXCR4 ligands. |
| AID571612 | Cmax in HIV-1 infected patient on day 1 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID32218 | Protection of ATH8 cells against the cytopathic effect of HIV isolate HTLF IIIB | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
| 1-(3-cyano-2,3-dideoxy-beta-D-erythro-pentofuranosyl)thymine (cyanothymidine): synthesis and antiviral evaluation against human immunodeficiency virus. |
| AID519966 | Antiviral activity against 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells by phenosense assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID574187 | Cytotoxicity against human skeletal muscle Myoblast assessed as increase in mitochondrial DNA on day 5 by RT-PCR relative to untreated control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID282744 | Selectivity index, ratio of CC50 for C8166 cells to IC50 for HIV-3B infected C8166 cells | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
| AID1504703 | Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID557281 | Ratio of EC50 for HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID104946 | Cytotoxicity was determined as the dose required to reduce the viability of uninfected MT-4 cells by 50% | 1987 | Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
| Synthesis and anti-HIV activity of various 2'- and 3'-substituted 2',3'-dideoxyadenosines: a structure-activity analysis. |
| AID155287 | Compound was evaluated for cellular proliferation (on viability of peripheral blood mononuclear cells) using microculture tetrazolium assay (MTA). | 1998 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
| Structure-based design of N-[2-(1-piperidinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea and N-[2-(1-piperazinylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
| AID379885 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 3B | 2006 | Journal of natural products, Dec, Volume: 69, Issue:12
| Rubrisandrins A and B, lignans and related anti-HIV compounds from Schisandra rubriflora. |
| AID300149 | Selectivity index, ratio of CC50 for human Caco-2 cells to IC50 for Rotavirus RF after attachment to Caco2 cells | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID1141968 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID369081 | Cytotoxicity against african green monkey Vero cells after 3 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, Feb-01, Volume: 17, Issue:3
| 5'-O-Aliphatic and amino acid ester prodrugs of (-)-beta-D-(2R,4R)-dioxolane-thymine (DOT): synthesis, anti-HIV activity, cytotoxicity and stability studies. |
| AID516489 | Displacement of [125I]-SDF-1-alpha from CXCR4 expressed in CHO cells | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist. |
| AID82282 | Inhibitory activity against HIV-1 IIIB in CEM-SS infected cells (Experiment 1) | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6
| A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor. |
| AID46800 | Concentration required to reduce 50% of the number of CEM/O cells in the HIV-1 infected cell cultures. | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17
| Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3'-azido-3'-deoxythymidine. |
| AID482025 | Inhibition of human TK1 by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| 3'-(1,2,3-Triazol-1-yl)-3'-deoxythymidine analogs as substrates for human and Ureaplasma parvum thymidine kinase for structure-activity investigations. |
| AID1379963 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
| AID379613 | Antiviral activity against HIV1 in human H9 cells assessed as inhibition of viral replication | 2000 | Journal of natural products, Mar, Volume: 63, Issue:3
| Sesquiterpene alkaloids from Tripterygium hypoglaucum and Tripterygium wilfordii: a new class of potent anti-HIV agents. |
| AID1357793 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID431622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID26380 | Dissociation constant (pKa) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID1352322 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID1508590 | Effective concentration for 50% protection of HIV-induced cytopathogenicity in MT-4 cells on the MTT assay (ZIDOVUDINE control) | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. |
| AID1705192 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID377973 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 3B | 1999 | Journal of natural products, Jan, Volume: 62, Issue:1
| Novel anti-HIV lancilactone C and related triterpenes from Kadsura lancilimba. |
| AID279920 | Effect on HDL cholesterol level in lean Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1157580 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID1461694 | Inhibition of P-gp in human MCF7/DX1 cells assessed as increase in calcein-AM accumulation at 500 uM incubated for 10 mins by flow cytometry | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
| Dual inhibitors of the human blood-brain barrier drug efflux transporters P-glycoprotein and ABCG2 based on the antiviral azidothymidine. |
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID572779 | Ratio of IC50 for HIV1 harboring reverse transcriptase L74V mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID284317 | Antiviral activity against bovine rotavirus RF in MA104 cells | 2007 | Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
| Fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-2-keto-beta-D-glucopyranosyl derivatives of N4-benzoyl cytosine. |
| AID1348217 | Antiviral activity against wild-type VSV-G pseudotyped HIV1 infected in HEK293 cells assessed as time of 50% failure at 1 uM measured at 48 hrs post infection by luciferase reporter gene assay | 2017 | Journal of natural products, 12-22, Volume: 80, Issue:12
| Oxazole-Containing Diterpenoids from Cell Cultures of Salvia miltiorrhiza and Their Anti-HIV-1 Activities. |
| AID46255 | Inhibitory activity against HIV-1 IIIB in CEM-SS infected cells (Experiment 2) | 1999 | Bioorganic & medicinal chemistry letters, Mar-22, Volume: 9, Issue:6
| A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor. |
| AID291759 | Inhibition of HIV1 reverse transcriptase at 200 ug/mL | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro. |
| AID104403 | Minimum compound concentration that reduced cell viability by 25% for HIV replication in MT-2 cells. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID1761020 | Antiviral activity against HIV-1 harboring reverse transcriptase RES056 mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID1165078 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
| AID665273 | Antiviral activity against HIV2 ROD mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID679291 | TP_TRANSPORTER: uptake in Xenopus laevis oocytes | 2000 | Biochemical pharmacology, Jul-15, Volume: 60, Issue:2
| Role of organic cation transporters in the renal secretion of nucleosides. |
| AID458875 | Cytotoxicity against human CEM-SS cells by MTT assay | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| 5-Modified-2'-dU and 2'-dC as mutagenic anti HIV-1 proliferation agents: synthesis and activity. |
| AID83074 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in preinfected PBL (peripheral blood lymphocytes) at 14 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID548315 | Antiviral activity against HIV1 subtype D isolate 92UG024 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID44657 | Ability to reduce 50% viability of C8166 cells acutely infected with HIV-2 strain IIIB | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Decomposition pathways and in vitro HIV inhibitory effects of isoddA pronucleotides: toward a rational approach for intracellular delivery of nucleoside 5'-monophosphates. |
| AID616199 | Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus 1 NL4-3 infected in human MT2 cells assessed as inhibition of viral replication after 48 hrs by luciferase activity reporter gene assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis of new 2'-deoxy-2'-fluoro-4'-azido nucleoside analogues as potent anti-HIV agents. |
| AID106239 | Concentration required for 50% protection of MT-4 cells against the cytopathic effect of HIV-1 | 1995 | Journal of medicinal chemistry, Mar-03, Volume: 38, Issue:5
| Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo-[4,5,1-jk][1,4]benzodiazepin- 2(1H)-one (TlBO) derivatives. 4. |
| AID1604013 | Inhibition of HIV-1 reverse transcriptase after 1 hr by ELISA | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review. |
| AID519888 | Antiviral activity against 0.05 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID235702 | Selectivity index is the ratio of CC50 and EC50 in peripheral blood lymphocytes (PBL). | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID556526 | Antiviral activity against Human immunodeficiency virus 1 clone Q9016 harboring K122E, Q145M, I202V, F214L mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
| AID423281 | Selectivity ratio of EC50 for multinucleoside-resistant HIV1 NL4-3 harboring A62V, V75I, F77L, F116Y, Q151M mutation in viral reverse transcriptase to EC50 for wild type HIV1 NL4-3 | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro. |
| AID499275 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
| Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
| AID105138 | Concentration of compound required to protect 50% of MT-4 cells against retroviral cytopathic effects by HIV-2 (ROD) | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID417253 | Cmin in HIV-infected human assessed as zidovudine triphosphate level in PBMC at 600 mg QD for 7 days measured per 10'6 cells in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1152846 | Cytotoxicity against cat CRFK cells assessed as cell viability after 7 days by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Evaluation of the antiviral efficacy of bis[1,2]dithiolo[1,4]thiazines and bis[1,2]dithiolopyrrole derivatives against the nucelocapsid protein of the Feline Immunodeficiency Virus (FIV) as a model for HIV infection. |
| AID574201 | Cytotoxicity against human skeletal muscle Myotube at 100 uL on day 5 by WST-1 assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Impact of nucleoside reverse transcriptase inhibitors on mitochondrial DNA and RNA in human skeletal muscle cells. |
| AID717451 | Cytotoxicity against human PBMC | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Synthesis, evaluation of anti-HIV-1 and anti-HCV activity of novel 2',3'-dideoxy-2',2'-difluoro-4'-azanucleosides. |
| AID569230 | Cytotoxicity against human CEM-GFP cells assessed as highest non cytotoxic concentration after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3
| Design and synthesis of caffeoyl-anilides as portmanteau inhibitors of HIV-1 integrase and CCR5. |
| AID1220786 | Fraction unbound in monkey plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID664467 | Antiviral activity against HIV1 BaL infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID282750 | Reduction of HIV1-p24 antigen production in HIV1-3 Ba-L infected macrophages | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. |
| AID105872 | Concentration required to reduce the number of viable uninfected cells by 50% | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| Design, synthesis, and structure-activity relationship of novel dinucleotide analogs as agents against herpes and human immunodeficiency viruses. |
| AID334754 | Ratio of ID50 for cat CRFK cells to ED50 for Feline leukemia virus | 1992 | Journal of natural products, Apr, Volume: 55, Issue:4
| Fistularin 3 and 11-ketofistularin 3. Feline leukemia virus active bromotyrosine metabolites from the marine sponge Aplysina archeri. |
| AID574002 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for wild-type Human immunodeficiency virus 2 ROD | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID104283 | Inhibition of cytopathic effect of HIV-1 strain RF in MT-4 cell culture | 1993 | Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
| A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships. |
| AID154786 | Antiviral activity against subtype isolate E strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID322392 | Antiviral activity against HIV1 3B assessed as inhibition of virus-induced cytopathogenicity in MT4 cells after 4 days by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs). |
| AID456306 | Antiviral activity against HIV1 LAI infected in human CEM-SS cells assessed as inhibition of viral replication by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
| Synthesis and anti-HIV evaluation of water-soluble calixarene-based bithiazolyl podands. |
| AID1736354 | Antiviral activity against VSVG/wild-type HIV-1 infected in human HEK 293T cells assessed as time during which compound exhibits 50% virologic failure at 1 uM treated at post-viral infection and measured at 48 hrs post-infection by luciferase reporter gen | | | |
| AID232916 | Selective index is the ratio of cytotoxic concentration to effective concentration against MT-4 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID104792 | Cytotoxic concentration required to reduce viability of mock-infected MT-4 cells (4 days) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiviral activity of 8-aza analogs of chiral [2-(phosphonomethoxy) propyl]guanines. |
| AID1884223 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wildtype HIV-1 3B infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID543109 | Induction of adipocyte differentiation in mouse 3T3-F442A cells assessed as C/EBPalpha mRNA expression on day 6 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID571596 | AUC (0 to 12 hrs) in HIV-1 infected patient at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID576204 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 50 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1223451 | Uncompetitive substrate inhibition of UGT2B7 in diabetic human kidney microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID45016 | Concentration of compound required to inhibit 50% of viral replication of human immunodeficiency virus in CEM-F cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| Synthesis and antiviral activity of several 2,5'-anhydro analogues of 3'-azido-3'-deoxythymidine, 3'-azido-2',3'-dideoxyuridine, 3'-azido-2',3'-dideoxy-5-halouridines, and 3'-deoxythymidine against human immunodeficiency virus and Rauscher-murine leukemia |
| AID81417 | Evaluated for anti-HIV activity | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
| Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2', 3'-unsaturated L-nucleosides. |
| AID19629 | Partition coefficient (logP) | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2'-fluoro-ara- and 2'-fluoro-ribo-2',3'- dideoxyadenosine as a strategy to bypass a metabolic blockade. |
| AID548832 | Antiviral activity against HIV1 isolate 200 harboring reverse transcriptase M41L/L210W/T215Y mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1304539 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CytoTox-Glo assay | 2016 | Journal of natural products, Mar-25, Volume: 79, Issue:3
| Carolignans from the Aerial Parts of Euphorbia sikkimensis and Their Anti-HIV Activity. |
| AID1594067 | Therapeutic index, ratio of CC50 for cat FL-4 cells to EC50 for inhibition of nucleocapsin protein in FIV infected in cat FL-4 cells | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Synthesis and comparison of substituted 1,2,3-dithiazole and 1,2,3-thiaselenazole as inhibitors of the feline immunodeficiency virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID573990 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for non nucleoside Protease inhibitor-resistant Human immunodeficiency virus 1 | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID452272 | Cytotoxicity against african green monkey Vero cells after 5 days | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus. |
| AID1152370 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
| Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID557282 | Ratio of EC50 for HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1331269 | Cytotoxicity against human C8166 cells measured after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
| Design, synthesis and anti-HIV-1 RT evaluation of 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives. |
| AID289142 | Inhibition of HIV1 reverse transcriptase | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | | | |
| AID718371 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
| AID548820 | Antiviral activity against HIV1 isolate 071 harboring reverse transcriptase 65R/S68N/184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID235641 | Selectivity index in the HIV-1 infected cell cultures. | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17
| Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3'-azido-3'-deoxythymidine. |
| AID45007 | Concentration required to reduce the viability of uninfected cells (CEM-CL13) by 50% on day 19. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1610039 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 92/BR/018 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID83055 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID105127 | Compound was evaluated for the inhibition of HIV-1 induced CPE (HTLV-III B strain ) replication in MT-4 cells | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
| Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
| AID1483284 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID155293 | Compound was evaluated for its toxicity by Calorimetric assay in PBM | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID82926 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 26 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID520606 | Selectivity index, ratio of CC50 for human WI38 cells to EC50 for BK polyomavirus ATCC VR837 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Anti-BK virus activity of nucleoside analogs. |
| AID1322998 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
| AID261443 | Cytotoxicity against human PBMC | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
| Synthesis and anti-HIV activity of D- and L-thietanose nucleosides. |
| AID46376 | Antiviral activity against site directed resistant isolate HIV-1 K101E in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID104939 | The cytotoxic concentration of compound required to reduce the viability of mock-infected MT-4 cells by 50% on HIV-1 virus A012D strain | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | | | |
| AID152970 | Effective concentration of compound against HIV-1 89.6 strain in PBMC cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| New bicyclam-GalCer analogue conjugates: synthesis and in vitro anti-HIV activity. |
| AID373384 | Stability in human CEM cells assessed as intracellular radioactive triphosphate metabolite accumulation at 2 uM incubated for 24 hrs measured after 24 hrs of compound removal assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID548805 | Antiviral activity against HIV1 isolate 204 harboring reverse transcriptase M41L/L210W/T215Y/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID542930 | Induction of preadipocyte differentiation in mouse 3T3L1 cells assessed as PPARgamma mRNA expression on day 4 by RT-PCR analysis | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID290122 | Antiviral activity against HCMV AD169 | 2007 | European journal of medicinal chemistry, Apr, Volume: 42, Issue:4
| Synthesis and antiviral activity of C-fluoro-branched cyclopropyl nucleosides. |
| AID575953 | Antiviral activity against Human immunodeficiency virus 1 WEJO infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID279938 | Decrease in fatty acid synthase activity in Wistar cafteria-fed rat epididymal adipose tissue at 70 mg/kg/day by DNA quantification assay | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID542926 | Induction of preadipocyte differentiation in mouse 3T3-F442A cells assessed as triglyceride accumulation at 6 uM after 9 days by oil red O staining relative to control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID235681 | Selectivity Index measured as the ratio of CC50 to that of EC50(HIV-1) values. | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Synthesis and antiviral activity of 8-aza analogs of chiral [2-(phosphonomethoxy) propyl]guanines. |
| AID644280 | Antiviral activity against R5 tropic HIV1 NL(AD8) in PM1/CCR5 cells assessed as protection from virus-induced cytopathogenicity after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
| Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins. |
| AID516492 | Selectivity index, ratio of CC50 for human PM1 cells expressing CCR5 to IC50 for HIV1 MNA | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist. |
| AID85880 | Cytotoxicity against HSV-1 (herpes simplex virus); Not determined | 1999 | Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
| Nucleosides and nucleotides. 183. Synthesis of 4'alpha-branched thymidines as a new type of antiviral agent. |
| AID261445 | Cytotoxicity against Vero cells | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
| Synthesis and anti-HIV activity of D- and L-thietanose nucleosides. |
| AID25126 | Half life of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine. |
| AID523352 | Antiviral activity against HIV1 with RT connection domain K103N/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID309232 | Antiviral activity against HIV1 3B replication in H9 cells | 2007 | Bioorganic & medicinal chemistry, Nov-01, Volume: 15, Issue:21
| Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. |
| AID46985 | Tested for anti-HIV -1 Activity in CEM/TK- cell culture | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID105756 | Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 5 uM concentration. | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID1357802 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase E138K mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | | | |
| AID1610036 | Antiviral activity against HIV1 UG070 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID222492 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 24 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID511696 | Therapeutic index, ratio of TC50 for human CEM-SS cells infected with HIV1 3B to EC50 for HIV1 3B infected in human CEM-SS cells | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Identification of novel human immunodeficiency virus type 1-inhibitory peptides based on the antimicrobial peptide database. |
| AID548541 | Antiviral activity against HIV2 isolate CBL-20 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1632122 | Cytotoxicity against human HeLa cells assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID1331270 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells | 2017 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
| Design, synthesis and anti-HIV-1 RT evaluation of 2-(benzyl(4-chlorophenyl)amino)-1-(piperazin-1-yl)ethanone derivatives. |
| AID519860 | Antiviral activity against HIV1 subtype B-SF-2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID45010 | Concentration that reduced by 50% the HIV induced CPE (cytopathic effect) on day 11. | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID342007 | Antibacterial activity against deoxyribonucleotide kinase-deficient Escherichia coli KY895 expressing Staphylococcus aureus recombinant deoxyguanosine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID681294 | TP_TRANSPORTER: inhibition of Calcein efflux (Calcein: 0.05 micro;M, Zidovudine: 0.02 uM) in UMCC-1/VP cells | 2002 | AIDS (London, England), Sep-06, Volume: 16, Issue:13
| The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein 1 (MRP-1). |
| AID1446819 | Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID679629 | TP_TRANSPORTER: Anti-HIV-1 activity in MT-4 and MT-4/DOX500 | 2003 | Molecular pharmacology, Jan, Volume: 63, Issue:1
| Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. |
| AID1447283 | Inhibition of HIV1 BaL dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
| Synthesis and anti-HIV activities of unsymmetrical long chain dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID1561719 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against v | | | |
| AID558395 | Ratio of drug level in HIV-infected pregnant woman amniotic fluid to maternal blood plasma at 300 mg, po BID by LC/MS/MS analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID104287 | Inhibitory activity toward HIV replication in MT-4 cells | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Side-chain derivatives of biologically active nucleosides. 1. Side-chain analogs of 3'-azido-3'-deoxythymidine (AZT). |
| AID214413 | Cytotoxic concentration against HIV-1 infected U937 cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID571591 | Apparent oral clearance in HIV-1 infected patient on day 10 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1228735 | Antiviral activity against HIV1-3B infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5
| Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
| AID693584 | Antiviral activity against HIV1 RES056 harbouring RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
| AID282659 | Cytotoxicity against MT2 cells | 2004 | Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
| (Z)- and (E)-[2-Fluoro-2-(hydroxymethyl)cyclopropylidene]methylpurines and -pyrimidines, a new class of methylenecyclopropane analogues of nucleosides: synthesis and antiviral activity. |
| AID82930 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 7 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID584814 | Toxicity in human subcutaneous preadipocytes assessed as effect on mitochondrial membrane potential at 6 uM after 30 days using JC-1 red/green fluorescence dye by flow cytometry analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID235232 | Therapeutic index was determined | 2001 | Bioorganic & medicinal chemistry letters, Dec-17, Volume: 11, Issue:24
| Synthesis and anti-HIV activity of oleanolic acid derivatives. |
| AID466208 | Antiviral activity against HIV1-infected human C8166 cells | 2010 | Journal of natural products, Feb-26, Volume: 73, Issue:2
| Chemical constituents from the leaves and stems of Schisandra rubriflora. |
| AID1172376 | Ratio of IC50 for human thymidine kinase-deficient 143B cells to IC50 for human 143B cells | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID1888689 | Antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | | | |
| AID247978 | Inhibitory concentration against HIV IIIB replication in H9 lymphocytes | 2004 | Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
| Anti-AIDS agents. 60. Substituted 3'R,4'R-di-O-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP) analogues as potent anti-HIV agents. |
| AID429825 | Antiviral activity against HIV1 3B in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6
| Lignans with anti-HIV activity from Schisandra propinqua var. sinensis. |
| AID83425 | Effective concentration required for antiviral activity against HIV strain TP1 by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID152644 | Cytotoxicity against human peripheral blood mononuclear (PBM) cells infected with HIV-I | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
| Asymmetric synthesis and biological evaluation of beta-L-(2R,5S)- and alpha-L-(2R,5R)-1,3-oxathiolane-pyrimidine and -purine nucleosides as potential anti-HIV agents. |
| AID423789 | Antiviral activity against MDR1-resistant HIV1 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID619642 | Ratio of EC50 for HIV-1 3B harboring RT E138K mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID698299 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID1157586 | Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Synthesis of novel fluoro analogues of MKC442 as microbicides. |
| AID379614 | Therapeutic index, ratio of IC50 for human H9 cells to EC50 for HIV1 | 2000 | Journal of natural products, Mar, Volume: 63, Issue:3
| Sesquiterpene alkaloids from Tripterygium hypoglaucum and Tripterygium wilfordii: a new class of potent anti-HIV agents. |
| AID571588 | Tmax in HIV-1 infected patient on day 10 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID199075 | RT activity in culture fluid at 10e-4 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID571590 | AUC (0 to 12 hrs) in HIV-1 infected patient on day 10 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID289144 | Antiviral activity against HIV1 with reverse transcriptase 6TAM mutation assessed as reduction of potency relative to wild type | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs. |
| AID104310 | Effective dose achieving 50% protection of MT-4 cells against the cytopathic effect of HIV | 1990 | Journal of medicinal chemistry, Jun, Volume: 33, Issue:6
| Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides. |
| AID548840 | Antiviral activity against HIV1 isolate 217 harboring reverse transcriptase D67N/K70E/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID612670 | Cytotoxicity against human C8166 cells by MTT assay | 2011 | Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
| Synthesis and biological evaluation of (±)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID707986 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV-1 3B infected in C8166 cells | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Discovery of inhibitors to block interactions of HIV-1 integrase with human LEDGF/p75 via structure-based virtual screening and bioassays. |
| AID516490 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
| CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist. |
| AID83220 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID417255 | Cmin in HIV-infected human assessed as zidovudine monophosphate level in PBMC at 600 mg QD for 7 days measured per 10'6 cells in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1693430 | Antiviral activity against HIV-1 NL(AD8) in human PM1/CCR5 cells assessed as virus induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Potent leads based on CA-19L, an anti-HIV active HIV-1 capsid fragment. |
| AID1652586 | Antiviral activity against HIV2 ROD infected in human CEM/0 cells assessed as inhibition of viral-induced giant cell formation incubated for 4 to 5 days by microscopy | | | |
| AID1221958 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1320865 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
| AID607876 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type Human immunodeficieny virus 1 3B infected in human MT4 cells | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID104612 | Antigen p24 content in culture fluid at 10e-4 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID1570217 | Antiviral activity against HIV1 infected in human C8166 cells | 2019 | European journal of medicinal chemistry, 10-15, Volume: 180 | An insight into the medicinal perspective of synthetic analogs of indole: A review. |
| AID1884220 | Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID1152847 | Antiviral activity against Feline immunodeficiency virus infected in cat FL-4 cells assessed as viral RNA production by RT-qPCR | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Evaluation of the antiviral efficacy of bis[1,2]dithiolo[1,4]thiazines and bis[1,2]dithiolopyrrole derivatives against the nucelocapsid protein of the Feline Immunodeficiency Virus (FIV) as a model for HIV infection. |
| AID152624 | The compound was tested for antiviral activity against AZT sensitive strain 9F HIV in PBM cells. | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID46643 | Concentration required to reduce 50% of the number of CEM/O cells in the mock infected cell cultures. | 1996 | Journal of medicinal chemistry, Aug-16, Volume: 39, Issue:17
| Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3'-azido-3'-deoxythymidine. |
| AID105760 | Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.008 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID259182 | Antiviral activity against HIV2 ROD in CEM cells | 2006 | Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
| Synthesis and antiviral evaluation of cyclic and acyclic 2-methyl-3-hydroxy-4-pyridinone nucleoside derivatives. |
| AID423158 | Antiviral activity against wild type HIV2 ROD produced from full length pROD9 infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro. |
| AID1754642 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID104423 | Cytotoxic concentration required to reduce the viability of HIV-1 by 50% MT-4 cells | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID583449 | Cytotoxicity against human HepG2 cells assessed as reduction in mitochondrial DNA content at 50 uM after 15 days by RT-PCR method relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID79276 | Anti-HIV activity was evaluated as the concentration required to inhibit HIV-1 replication in H9 lymphocyte cells by 50% | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
| Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs. |
| AID45193 | Compound was evaluated for the effect of Order of Addition on Cytoprotection against HIV-1RF at dilution 1000, Add at infection | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID363847 | Antiviral activity against rotavirus RF in human Caco-2 cells assessed as inhibition of infectivity following virus attachment after 72 hrs | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
| Synthesis and molecular modelling of unsaturated exomethylene pyranonucleoside analogues with antitumor and antiviral activities. |
| AID584635 | Toxicity in human subcutaneous preadipocytes assessed as decrease of PPARgamma expression at 6 uM after 18 days by RT-PCR analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID1237702 | Cytotoxicity against human CEM/0 cells assessed as reduction in cell proliferation incubated for 4 to 5 days | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
| Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides. |
| AID342550 | Antiviral activity against HIV1 infected human MT4 cells | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
| Phenyl phosphotriester derivatives of AZT: variations upon the SATE moiety. |
| AID542942 | Induction of adipocyte differentiation in mouse 3T3-F442A cells assessed as triglyceride accumulation at 1 uM on day 9 by oil red O staining relative to control | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID1572519 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID548822 | Antiviral activity against HIV1 isolate 157 harboring reverse transcriptase L74V/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID157399 | The cytotoxic concentration of compound required to reduce the viability of mock-infected PBL cells by 50% on HIV-1 virus HTLV-IIIB strain | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1884226 | Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID43810 | Minimal inhibitory concentration was measured as compound concentration that causes a microscopically visible alteration of C3H cell morphology. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine. |
| AID45023 | Cytotoxic concentration required to reduce the viability of HIV-1 by 50% in CEM-SS cells | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID1304407 | Inhibition of HIV-1 BH10 recombinant reverse transcriptase K103N mutant expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID698305 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID83555 | Tested for the determination of percentage protection at 1 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID1220788 | Fraction unbound in human plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1191973 | Cytotoxicity against mock-infected human HeLa cells by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
| AID1743637 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID427971 | Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression at > 0.5 uM followed by drug wash out and viral infection measured after 48 hrs by MAGI assay | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2. |
| AID104308 | Cytopathogenicity against HIV-1 induced, replication in MT-4 cells was determined | 1990 | Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
| Synthesis, antiretrovirus effects, and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine. |
| AID1763904 | Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID79291 | Compound was evaluated for anti-HIV activity in H9 lymphocytes | 1998 | Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
| Anti-AIDS agents. 32. Synthesis and anti-HIV activity of betulin derivatives. |
| AID563944 | Antiviral activity against HIV1 pNL4-3 harboring chimeric pTKD infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID105322 | Effective dose to achieve 50% protection of MT-4 cells from acutely infected HIV-1 strain IIIB | 1996 | Journal of medicinal chemistry, May-10, Volume: 39, Issue:10
| Decomposition pathways and in vitro HIV inhibitory effects of isoddA pronucleotides: toward a rational approach for intracellular delivery of nucleoside 5'-monophosphates. |
| AID152932 | Anti-HIV activity against multidrug resistant HIV TM strain by inhibition of HIV p24 antigen expression in peripheral blood mononuclear cells(PBMC) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
| AID222393 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT after 0.5 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1197834 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
| AID46390 | Compound was evaluated for its toxicity by Calorimetric assay in CEM | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1152848 | Therapeutic index, ratio of CC50 for cat CRFK cells to EC50 for Feline immunodeficiency virus infected in cat FL-4 cells | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Evaluation of the antiviral efficacy of bis[1,2]dithiolo[1,4]thiazines and bis[1,2]dithiolopyrrole derivatives against the nucelocapsid protein of the Feline Immunodeficiency Virus (FIV) as a model for HIV infection. |
| AID105348 | Tested for the inhibitory activity of HIV-1 infected MT-4 cells | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| 1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity. |
| AID106598 | Cytotoxic concentration of compound required to reduce the viability of mock infected MT-4 cells on the MTT assay in test I | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. |
| AID1632128 | Selectivity index, ratio of IC50 for HDF to IC50 for human HeLa cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID15235 | Percentage of radioactivity in P1 subregion in mouse brain that contains nuclei and cell debris, after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID718815 | Antiviral activity against HIV1 3B infected in human C8166 cells assessed as inhibition of syncytia after 3 days | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Structural modifications of 5,6-dihydroxypyrimidines with anti-HIV activity. |
| AID153131 | Conc. required to cause 50% death of uninfected PBMCs | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID373353 | Drug metabolism in human CEM cells assessed as radioactive zidovudine triphosphate accumulation at 2 uM after 2 hrs assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID342008 | Antibacterial activity against deoxyribonucleotide kinase-deficient Escherichia coli KY895 expressing Streptococcus pyogenes recombinant deoxyadenosine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID557274 | Antiviral activity against HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID681676 | TP_TRANSPORTER: uptake in OAT4-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID341372 | Antiviral activity against R5-HIV1MDR/G assessed as inhibition of p24 Gag protein in human PHA-PBMC by ELISA relative to X4-HIV1NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID1875662 | Antiviral activity against HIV NL4-3 infected in MT-4 cells assessed as viral replication measured after 4 days by p24-ELISA | 2022 | Journal of natural products, 11-25, Volume: 85, Issue:11
| Tigliane-Type Diterpene Esters from the Fruits of |
| AID1446817 | Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID291852 | Antiviral activity against HTLV1 in human PBMC at 1 uM | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID83112 | Effective concentration against cytopathicity of HIV-2 strain (ROD) in CEM cell line | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
| Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription. |
| AID105762 | Toxicity was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.2 uM concentration | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID106588 | Concentration required to reduce the viability of mock-infected MT-4 cells by 50%. | 1992 | Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
| Structure-activity relationships of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine analogues: effect of substitutions at the C-6 phenyl ring and at the C-5 position on anti-HIV-1 activity. |
| AID1223446 | Ratio of Vmax to Km in diabetic human liver microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | | | |
| AID1705190 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID152627 | Antiviral activity against (HIV-1M184V) mutant strain in human PBM cells | 2002 | Journal of medicinal chemistry, Oct-24, Volume: 45, Issue:22
| Stereoselective synthesis and antiviral activity of D-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID542935 | Antiproliferative activity against mouse 3T3-F442A cells assessed as [3H]thymidine incorporation at 3 uM | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID222494 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 48 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID235628 | Selectivity index determined for CC50 (test I) to EC50 x 10e3 | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. |
| AID1743629 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID45022 | Cytotoxic conc. which reduces the cell viability of HIV-1 LAI infected T4 lymphoblastoid CEM-SS cells by 50% | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID14728 | Pharmacokinetic parameter AUC for the compound after intravenous administration into BALB/c Mice in plasma samples. | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID405335 | Toxicity in human HepG2/C3A cells assessed as induction of cell death at 50 uM after 14 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID45180 | Tested for cytotoxic concentration on HIV-I Lai wild type in CEM-SS cell line | 2000 | Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
| Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. |
| AID106586 | Concentration of compound required to reduce MT-4 cells viability by 50%. | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine. |
| AID261442 | Antiviral activity against HIV1 in human PBMC | 2006 | Journal of medicinal chemistry, Mar-09, Volume: 49, Issue:5
| Synthesis and anti-HIV activity of D- and L-thietanose nucleosides. |
| AID604025 | Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID46044 | Inhibitory activity against the cytopathic effect of HIV-1 LAV strain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID676994 | Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
| Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID125503 | Antiproliferative activity was determined against human T-lymphocyte cells -Molt4/C8 | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
| Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription. |
| AID106241 | 90% inhibition of HIV replication in MT-4 cells | 2004 | Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
| Uncharged AZT and D4T derivatives of phosphonoformic and phosphonoacetic acids as anti-HIV pronucleosides. |
| AID747600 | Antiviral activity against Human immunodeficiency virus 1 LAI infected in human PBMC | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors. |
| AID221610 | In Vitro detection by Gray and Whittaker method for % of internalization by comparing with external nucleoside of 2000 nM/g | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID370731 | Antiviral activity against HIV1 3B infected human C8166 cells assessed as inhibition of syncytia formation by p24 antigen based assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. |
| AID1483282 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y181C mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID46983 | Tested for cytotoxic concentration in CEM/TK- cell culture | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID484741 | Cytotoxicity against human C8166 cells after 3 days by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
| Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro. |
| AID1356068 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV1 NL4-3 infected in human MT4 cells | 2018 | Journal of natural products, 07-27, Volume: 81, Issue:7
| Kleinhospitine E and Cycloartane Triterpenoids from Kleinhovia hospita. |
| AID1884540 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID79303 | Inhibitory activity against HIV-1 replication in H9 lymphocytes | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| Anti-AIDS agents. 42. Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone analogues. |
| AID1884227 | Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID491831 | Cytotoxicity against human H9 cells after 6 days by XTT assay | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID46657 | Concentration required to protect CEM/0 cells against the cytopathicity of HIV-2 by 50%. | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11
| Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers. |
| AID1316332 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID1231850 | Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6
| Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID1875663 | Therapeutic index, ratio of cytotoxicity against human MT4 cells to antiviral activity against HIV NL4-3 | 2022 | Journal of natural products, 11-25, Volume: 85, Issue:11
| Tigliane-Type Diterpene Esters from the Fruits of |
| AID1203627 | Cytotoxicity against human 5637 cells assessed as dead cells at 100 uM after 48 hrs by calcein/ethidium bromide staining-based fluorescence microscopic analysis relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID1289717 | Inhibition of human TERT-regulated Wnt/beta-catenin signalling in human MGC803 cells assessed as decrease in c-myc mRNA expression at 3 mmol/L after 48 hrs by RT-PCR method | 2016 | European journal of medicinal chemistry, Mar-03, Volume: 110 | Novel dihydropyrazole-chromen: Design and modulates hTERT inhibition proliferation of MGC-803. |
| AID225321 | Concentration required to reduce viability of mock-infected MT-4 cells | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID548309 | Antiviral activity against HIV1 isolate JR-CSF infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1077219 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
| AID548821 | Antiviral activity against HIV1 isolate 153 harboring reverse transcriptase L74V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID105746 | Protection was determined by evaluation of cluster morphology and reclustering properties in mock infected MT-4 cells at 0.00032 uM concentration; Range is 10-40 | 1987 | Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
| 3'-substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents. |
| AID523478 | Antiviral activity against HIV1 with RT connection domain G190A/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID423157 | Antiviral activity against wild type HIV1 NL4-3 produced from full length pR9deltaApa infected in human MAGIC-5A cells assessed as inhibition of Lac+ foci expression after 40 hrs | 2008 | Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
| Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro. |
| AID571598 | Half life in HIV-1 infected patient at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1220801 | Drug metabolism in bile duct-cannulated dog assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID519872 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID104430 | Effective concentration required to inhibit the replication of HIV-1 by 50% in MT-4 cells | 2003 | Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
| S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study. |
| AID222497 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 0.5 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1323001 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
| AID548814 | Antiviral activity against HIV1 isolate 061 harboring reverse transcriptase M41L/D67N/K70R/M184V/L210W/T215Y/K219E mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1304401 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID417264 | Half life in HIV-infected human plasma at 1500 mg | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID104259 | In vitro Cytotoxic concentration which reduced G 762-3(pre-AZT) infected MT-2 cells by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID163320 | Evaluated for the antiretroviral activity against Rauscher murine leukemia virus (R-MuLV) | 1990 | Journal of medicinal chemistry, Apr, Volume: 33, Issue:4
| Acyclic purine phosphonate analogues as antiviral agents. Synthesis and structure-activity relationships. |
| AID104251 | Anti-HIV activity based on inhibition of HIV-1 induced cytopathogenicity in MT-2 cells. | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
| AID1443670 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID335638 | Antiviral activity against HIV1 3B replication in human C8166 cells at 0.016 ug/ml after 5 to 7 days by MTT-formazan method | 1992 | Journal of natural products, Aug, Volume: 55, Issue:8
| Constituents of Eriobotrya japonica. A study of their antiviral properties. |
| AID1884487 | Cytotoxicity against human MT4 cells assessed as cell growth inhibition incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID519874 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID619514 | Selectivity index, ratio of CC50 for human CEM-T4 cells to EC50 for HIV1 infected human CEM-T4 cells | 2011 | Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
| Aryl H-phosphonates 17: (N-aryl)phosphoramidates of pyrimidine nucleoside analogues and their synthesis, selected properties, and anti-HIV activity. |
| AID1442803 | Antiviral activity against HIV1 HXB2 pseudovirus infected in human TZM-bl cells assessed as inhibition of viral entry treated 4 hrs post infection measured after 48 hrs by luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Synthesis, Antiviral Potency, in Vitro ADMET, and X-ray Structure of Potent CD4 Mimics as Entry Inhibitors That Target the Phe43 Cavity of HIV-1 gp120. |
| AID611573 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for Human immunodeficiency virus 1 3B infected in human C8166 cells | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Sesquiterpene and norsesquiterpene derivatives from Sanicula lamelligera and their biological evaluation. |
| AID47062 | Inhibition of p24 expression was measured at 1 uM using vVK/CV-1 assay | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
| AID397590 | Antiviral activity against HIV1 RF in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique | 2001 | Journal of natural products, Feb, Volume: 64, Issue:2
| Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program. |
| AID342006 | Antibacterial activity against deoxyribonucleotide kinase-deficient Escherichia coli KY895 expressing Staphylococcus aureus recombinant deoxyadenosine kinase | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID47002 | Compound was tested for inhibitory activity against HIV-1 replication in CEM/TK- cells | 1998 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
| Rational design of a new series of mixed anti-HIV pronucleotides. |
| AID364088 | Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of p24 antigen production at 5 uM by ELISA | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Anti-HIV-1 activity of phloroglucinol derivative, 6,6'-bieckol, from Ecklonia cava. |
| AID618858 | Cytotoxicity against phytohemagglutininin-stimulated human PBMC after 6 days by trypan blue exclusion assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis, antiviral activity, cytotoxicity and cellular pharmacology of l-3'-azido-2',3'-dideoxypurine nucleosides. |
| AID1303215 | Cytotoxicity against human MT4 cells infected with HIV1 3B assessed as cell growth inhibition after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and anti-HIV activity of novel quinoxaline derivatives. |
| AID56385 | Selective index is the ratio of inhibitory concentrations of cellular DNA polymerase alpha to HIV-1 reverse transcriptase | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID23368 | Hydrolysis half life in phosphate buffer; Not available | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
| cycloSal-Pronucleotides of 2'-fluoro-ara- and 2'-fluoro-ribo-2',3'- dideoxyadenosine as a strategy to bypass a metabolic blockade. |
| AID1209582 | Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
| AID25129 | Half life of the compound | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Brain targeting of anti-HIV nucleosides: synthesis and in vitro and in vivo studies of dihydropyridine derivatives of 3'-azido-2',3'-dideoxyuridine and 3'-azido-3'-deoxythymidine. |
| AID587738 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID439736 | Inhibition of Influenza A virus (A/Viet Nam/1203/2004(H5N1)) hemagglutininin-mediated viral entry into human A549 cells assessed as luciferase activity after 48 hrs postinfection by luminometry | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Discovery of the first series of small molecule H5N1 entry inhibitors. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | | | |
| AID373356 | Drug metabolism in human CEM cells assessed as radioactive 2', 3'-didehydro-3'-deoxy-4'-ethynylthymidine triphosphate accumulation at 2 uM after 12 hrs assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID197658 | Concentration that reduces Rauscher murine leukemia virus titer by 50% | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
| Unsaturated and carbocyclic nucleoside analogues: synthesis, antitumor, and antiviral activity. |
| AID222391 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 4 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID423788 | Antiviral activity against azidothymidine-resistant HIV1 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID611571 | Cytotoxicity against human C8166 cells after 3 days by MTT assay | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Sesquiterpene and norsesquiterpene derivatives from Sanicula lamelligera and their biological evaluation. |
| AID1616189 | Antiviral activity against HIV-1 NL4-3 infected in human MT-4 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Design and synthesis of pentacyclic triterpene conjugates and their use in medicinal research. |
| AID104238 | Therapeutic index is the ratio between IC50/EC50 of HIV-I IIIB strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID152819 | Anti-HIV activity against multidrug resistant HIV JSL strain by inhibition of HIV p24 antigen expression in peripheral blood mononuclear cells(PBMC) | 2003 | Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
| Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. |
| AID1316336 | Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID153106 | Inhibition of HIV-1 (IIIB) cytopathicity in human peripheral blood mononuclear cells. | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID40035 | Antiviral activity against Ba-L monocyte tropic isolate strain in monocyte | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID1220785 | Fraction unbound in rat plasma by ultracentrifugation method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID79286 | Concentration that inhibits HIV-1 replication in cell growth in H9 lymphocytes | 2003 | Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
| Anti-HIV agents. Part 55: 3'R,4'R-Di-(O)-(-)-camphanoyl-2',2'-dimethyldihydropyrano[2,3-f]chromone (DCP), a novel anti-HIV agent. |
| AID685335 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B | 2012 | Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
| Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors. |
| AID104261 | In vitro Cytotoxic concentration which reduced H 112-2(pre-AZT) infected MT-2 cells by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID200173 | Compound is evaluated in vitro for the inhibition single mutant of HIV-1 RTS (Y181C) | 1993 | Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
| 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase. |
| AID199076 | RT activity in culture fluid at 10e-5 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID1261368 | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth incubated for 5 days by CellTiter 96 AQueous One Solution cell proliferation assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Synthesis of dihydropyrimidine α,γ-diketobutanoic acid derivatives targeting HIV integrase. |
| AID548804 | Antiviral activity against HIV1 isolate 203 harboring reverse transcriptase M41L/L210W/T215Y/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID152623 | The compound was tested for antiviral activity against AZT resistant strain 9F HIV in PBM cells. | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6
| Structure-based identification of OATP1B1/3 inhibitors. |
| AID82918 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 15 days at a concentration 0.2 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1204140 | Cytotoxicity against human DU145 cells after 48 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| PMA-SiO2 catalyzed synthesis of indolo[2,3-c]quinolines as potent anti cancer agents. |
| AID519971 | Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 harboring M184V mutant RT to EC50 for 0.005 MOI HIV1 NL4-3 harboring wild type RT infected in human MT2 cells | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID83058 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID154973 | Effective concentration against HIV-1 in peripheral blood mononuclear cells(PBM). | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID46204 | Tested for the inhibitory activity of virus induced giant cell formation in HIV-1 infected CEM cells | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| 1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity. |
| AID572767 | Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication | 2009 | Antimicrobial 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. |
| AID1391085 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
| The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
| AID548577 | Antiviral activity against HIV1 isolate 066 harboring reverse transcriptase 184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID82924 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 22 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID389380 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
| 1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID548545 | Antiviral activity against HIV1 subtype A isolate 92UG037 infected in human MDM after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID81442 | Inhibition of HIV-1 D34 replication in human peripheral blood mononuclear cells. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi |
| AID1589119 | Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID222675 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 0.5 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID1520506 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 3 days by CellTiter-Glo luminescent assay | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Discovery and synthesis of novel beesioside I derivatives with potent anti-HIV activity. |
| AID548841 | Antiviral activity against HIV1 isolate 220 harboring reverse transcriptase K70E/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID90922 | Bone marrow toxicity was measured against human colony forming units-granulocyte monocyte (CFU-GM), concentration is 10.0 uM | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID273055 | Cytotoxicity against MT2 cells | 2006 | Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
| 9-{[3-fluoro-2-(hydroxymethyl)cyclopropylidene]methyl}adenines and -guanines. Synthesis and antiviral activity of all stereoisomers1. |
| AID45185 | Cytotoxicity against wild type HIV-1-IIIB strain infected CEMSS cells. | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| A new series of pyridinone derivatives as potent non-nucleoside human immunodeficiency virus type 1 specific reverse transcriptase inhibitors. |
| AID1352320 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID235212 | Therapeutic index is the ratio of IC50 to EC50 in H9 lymphocytes | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| Anti-AIDS agents. 42. Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone analogues. |
| AID429824 | Cytotoxicity against human C8166 cells by MTT assay | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6
| Lignans with anti-HIV activity from Schisandra propinqua var. sinensis. |
| AID1156484 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
| AID44815 | Concentration of compound that inhibits incorporation of radiolabeled amino acids by 50 % | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1). |
| AID104936 | In vitro antiviral activity against (monocyte macrophages) cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID1152845 | Cytotoxicity against cat CRFK cells assessed as cell viability at 10 uM after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12
| Evaluation of the antiviral efficacy of bis[1,2]dithiolo[1,4]thiazines and bis[1,2]dithiolopyrrole derivatives against the nucelocapsid protein of the Feline Immunodeficiency Virus (FIV) as a model for HIV infection. |
| AID105373 | Concentration required to reduce the number of viable cells in the untreated MT-4 cell culture | 1992 | Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
| 3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine. |
| AID341360 | Drug uptake in human CD4+CEM cells assessed as 3'-azido-2',3'-dideoxythymidine triphosphate half life at 200 nM | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID693586 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
| AID300146 | Antiviral activity against Rotavirus RF in human Caco-2 cells assessed as neutralization of virus in solution before its attachment after 72 hrs | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID1457058 | Antiviral activity against HIV1 harboring reverse transcriptase K103N /Y1881C double mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15
| Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
| AID1275552 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID83399 | Tested for the determination of percentage toxicity at 1 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID1720643 | Inhibition of reverse transcriptase/nucleocapsid protein 7 in wild type HIV1 NL4-3 infected in human TZM-bl cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID271059 | Antiviral activity against HIV1 PI-R replication in human MT4 cells | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Anti-AIDS agents 69. Moronic acid and other triterpene derivatives as novel potent anti-HIV agents. |
| AID647174 | Antiviral activity against HIV1 3B infected human TZM-bl cells assessed as inhibition of viral replication at 10 uM treated 8 hrs after viral infection by luciferase reporter assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 22, Issue:3
| Synthesis and antiviral activities of novel gossypol derivatives. |
| AID563943 | Antiviral activity against HIV1 pNL4-3 harboring Reverse transcriptase P119S/T165A/M184V mutant gene infected in TZM-bl cells after 72 hrs by luciferase assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
| Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile. |
| AID47432 | Inhibitory activity was evaluated on mitochondrial DNA content of CEM cells | 1999 | Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
| Synthesis and anti-HIV and anti-HBV activities of 2'-fluoro-2', 3'-unsaturated L-nucleosides. |
| AID417057 | Half life in HIV-infected human at 600 mg, po qd | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID380078 | Antiviral activity against HIV1 infected in human C8166 cells assessed as inhibition of viral-induced cytopathic effect | 2006 | Journal of natural products, Feb, Volume: 69, Issue:2
| Triterpenoids from Schisandra lancifolia with anti-HIV-1 activity. |
| AID575957 | Antiviral activity against Human immunodeficiency virus 1 subtype C BR/92/025 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID46053 | The compound was tested for anti HIV activity in CEM-SS cell lines | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
| Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents. |
| AID1710799 | Cytotoxicity against human HEL cells assessed as changes in cell morphology incubated for 3 to 6 days by light microscopy | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID1726078 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. |
| AID199851 | Reverse transcriptase activity was measured in the culture supernatant, concentration that reduces by 50% the HIV produced in the supernatant. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Preparation and anti-HIV activity of N-3-substituted thymidine nucleoside analogs. |
| AID525110 | Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID611911 | Therapeutic index, ratio of CC50 for against human C8166 cells to EC50 for HIV-1 | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Lindenane disesquiterpenoids with anti-HIV-1 activity from Chloranthus japonicus. |
| AID519960 | Selectivity ratio of EC50 for 0.01 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by MTS assay to EC50 for 0.01 MOI HIV1 NL4-3 infected in 2 hrs pretreated human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID373363 | Drug metabolism in human CEM cells assessed as radioactive 2', 3'-didehydro-3'-deoxy-4'-ethynylthymidine monophosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID341353 | Metabolic stability of the compound in human CEM cells assessed as 3'-azido-2',3'-dideoxythymidine diphosphate intracellular levels at 200 nM after 24 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID106044 | Inhibitory Effect against HIV-1 (IIIB) in CEM cells | 1995 | Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
| Design, synthesis, and structure-activity relationship of novel dinucleotide analogs as agents against herpes and human immunodeficiency viruses. |
| AID21084 | Compound was evaluated for the partition coefficient measured for 1-octanol and 0.01 M potassium phosphate buffer (pH 7.0) | 1991 | Journal of medicinal chemistry, May, Volume: 34, Issue:5
| Escherichia coli mediated biosynthesis and in vitro anti-HIV activity of lipophilic 6-halo-2',3'-dideoxypurine nucleosides. |
| AID1231847 | Selectivity index, CC50 for african green monkey Vero cells to EC50 for chikungunya virus Indian ocean strain 899 | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6
| Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID583441 | Cytotoxicity against human HepG2 cells assessed as slight increase in mitochondrial size at 50 uM after 15 days by electron microscopy relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID106633 | Inhibitory activity against the HIV-1-induced cytopathic effect in Macrophage | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID1285842 | Therapeutic index, ratio of CC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells | 2016 | Bioorganic & medicinal chemistry, May-01, Volume: 24, Issue:9
| Design, synthesis and anti-HIV-1 evaluation of hydrazide-based peptidomimetics as selective gelatinase inhibitors. |
| AID1597910 | Therapeutic index, ratio of CC50 for cat FL-4 cells to EC50 for antiviral activity against FIV infected in cat FL-4 cells | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
| Novel epidithiodiketopiperazines as anti-viral zinc ejectors of the Feline Immunodeficiency Virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID155625 | Inhibition of p24 expression in HIVD34-infected PBMC assay on day 4 at concentration of 40 nM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
| AID341998 | Antimicrobial activity against Streptococcus sp. 07686-2 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID395817 | Cytotoxicity against human PG cells after 48 hrs by MTT assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
| Simple and efficient synthesis of novel glycosyl thiourea derivatives as potential antitumor agents. |
| AID571589 | Cmax in HIV-1 infected patient on day 10 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID46845 | Antiviral activity in CEM/TK cell line infected with HIV-1 and Concentration required to inhibit the replication of HIV-1 by 50% was determined | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20
| Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate. |
| AID47311 | Cytotoxicity was determined in CEM cells, relative to RVT | 2004 | Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
| 2('),3(')-didehydro-2('),3(')-dideoxynucleosides are degraded to furfuryl alcohol under acidic conditions. |
| AID46079 | Therapeutic index value of the cpmpound against CEM-SS cells | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
| Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents. |
| AID279917 | Increase in triglyceride level in cafteria-fed Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID322393 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2008 | Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
| Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs). |
| AID214215 | inhibition of p24 core antigen synthesis in U1 cells | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and evaluation of novel ether lipid nucleoside conjugates for anti-HIV-1 activity. |
| AID614140 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
| AID79442 | Therapeutic index in H9 lymphocytes. | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14
| Anti-AIDS agents. 37. Synthesis and structure-activity relationships of (3'R,4'R)-(+)-cis-khellactone derivatives as novel potent anti-HIV agents. |
| AID1352319 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
| AID581052 | Cytotoxicity against differentiated mouse 3T3-F442A cells assessed as effect on total deoxynucleotides content at 1 uM after 2 to 10 days | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Effects of zidovudine and stavudine on mitochondrial DNA of differentiating 3T3-F442a cells are not associated with imbalanced deoxynucleotide pools. |
| AID1710801 | Cytotoxicity against cat CRFK cells assessed as reduction in cell viability incubated for 3 to 6 days by MTS assay | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones. |
| AID573995 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-708,906-resistant Human immunodeficiency virus harboring T66I, L74M and S230R mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID1304406 | Inhibition of wild type HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13
| Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
| AID484743 | Therapeutic index, ratio of CC50 for human C8166 to EC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
| Anti HIV-1 agents 5: synthesis and anti-HIV-1 activity of some N-arylsulfonyl-3-acetylindoles in vitro. |
| AID46640 | Cytotoxic concentration against CEM cells (in vitro) | 1996 | Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
| Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. |
| AID523482 | Antiviral activity against HIV1 with RT connection domain G190S/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID1589118 | Cytotoxicity in human KB cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID393073 | Antiviral activity against HIV1 3a with reverse transcriptase M184V mutation in human MT2 cells assessed as inhibition of viral-induced cytopathic effect by XTT assay relative to wild type | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors. |
| AID584610 | Inhibition of electron transport protein complex 1/3 in human subcutaneous preadipocytes at 6 uM after 30 to 60 days by photometric analysis | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID105869 | Concentration of compound required to reduce MT-4 cell viability by 50% | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID28980 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
| QSAR model for drug human oral bioavailability. |
| AID393069 | Inhibition on HIV1 reverse transcriptase p66/p51 | 2009 | Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
| Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors. |
| AID587745 | Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID106968 | Concentration required to inhibit replication of HIV-2 LAV-2rod strain in MT-4 cells | 1992 | Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
| Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID1172373 | Cytotoxicity against human SW620 cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Synthesis and evaluation of sulfonylethyl-containing phosphotriesters of 3'-azido-3'-deoxythymidine as anticancer prodrugs. |
| AID519863 | Antiviral activity against HIV1 subtype B-NL4-3 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID454923 | Antiviral activity against HIV1 Ba-L(R5) infected in human PBMC by p24 antigen capture assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles. |
| AID88999 | Concentration of compound required to inhibit HIV-1 replication in MT-4 cells by 50% | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine. |
| AID439729 | Cytotoxicity against human TZM-b1 cells after 2 days | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors. |
| AID380207 | Antiviral activity against HIV infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 1999 | Journal of natural products, Jul, Volume: 62, Issue:7
| Biological evaluation of proanthocyanidin dimers and related polyphenols. |
| AID105137 | Concentration of compound required to protect 50% of MT-4 cells against retroviral cytopathic effects by HIV-1 (IIIa) | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID46036 | Cytotoxic concentration against 50% survival of uninfected untreated control CEM-SS cells | 1996 | Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
| Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity. |
| AID82921 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 15 days at a concentration 5 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1572525 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | | | |
| AID587739 | Cytotoxicity against human HeLaT4 cells by WST-1 assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID1525073 | Inhibition of reverse transcriptase in HIV1 NL4.3 infected in human HeLaP4 cells assessed as reduction in formation of reverse transcribed DNA at 50 fold antiviral EC50 incubated up to 60 mins by quantitative PCR analysis | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Synthesis and Anti-HIV Profile of a Novel Tetrahydroindazolylbenzamide Derivative Obtained by Oxazolone Chemistry. |
| AID1720637 | Inhibition of reverse transcriptase/nucleocapsid protein 7 in wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Discovery of potential dual-target prodrugs of HIV-1 reverse transcriptase and nucleocapsid protein 7. |
| AID154763 | In vitro antiviral activity against PBL cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID357033 | Antiviral activity against HIV1 in human H9 cells assessed as inhibition of viral replication | 2001 | Journal of natural products, Jul, Volume: 64, Issue:7
| Anti-AIDS agents. 46. Anti-HIV activity of harman, an anti-HIV principle from Symplocos setchuensis, and its derivatives. |
| AID384989 | Selectivity index, ratio of CC50 for human C8166 cells to EC50 for HIV1 | 2008 | Journal of natural products, May, Volume: 71, Issue:5
| Periglaucines A-D, anti-HBV and -HIV-1 alkaloids from Pericampylus glaucus. |
| AID89656 | In vitro cytotoxicity in CD4+ human T-cells (c8166), using HIV-1 RT enzyme assay | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. |
| AID1754643 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID229048 | Cytotoxic effect against vero cells. | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| L-beta-(2S,4S)- and L-alpha-(2S,4R)-dioxolanyl nucleosides as potential anti-HIV agents: asymmetric synthesis and structure-activity relationships. |
| AID423787 | Antiviral activity against efavirenz-resistant HIV1 infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID519858 | Antiviral activity against HIV1 subtype B-HXB2 infected in 1 hr-pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1589123 | Selectivity index, ratio of IC50 for cytotoxicity in human NHDF cells to IC50 for cytotoxicity in human HeLa cells | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
| Synthesis and in vitro anticancer activity of new gemcitabine-nucleoside analogue dimers containing methyltriazole or ester-methyltriazole linker. |
| AID1815394 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID82129 | Compound was evaluated for anti-retrovirus activity against HIV-1 (D34) Diagen strain. | 1993 | Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
| Novel acyclonucleotides: synthesis and antiviral activity of alkenylphosphonic acid derivatives of purines and a pyrimidine. |
| AID472647 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected human CEM cells expressing GFP measured up to 8 days postinfection by p24 antigen capture ELISA | 2010 | Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
| Synthesis and anti-HIV activity of alkylated quinoline 2,4-diols. |
| AID619633 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-2 ROD infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID1729152 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV 3B infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID698294 | Antiviral activity against HIV1 IRLL98 containing reverse transcriptase K101Q, Y181C and G190A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
| New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID82283 | Tested in vitro against MT-4 cells using MTT assay | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity. |
| AID1323000 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
| AID525104 | Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID540216 | Clearance in dog after iv administration | 2005 | Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
| Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure. |
| AID104315 | Ability to block replication of HIV-1 virus in mock infected MT-4 cells | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-on e (TIBO) derivatives. 2. |
| AID1461697 | Inhibition of ABCG2 in human MCF7/FLV1000 cells assessed as increase in calcein-AM accumulation at 400 uM incubated for 10 mins by flow cytometry | 2017 | Bioorganic & medicinal chemistry, 10-01, Volume: 25, Issue:19
| Dual inhibitors of the human blood-brain barrier drug efflux transporters P-glycoprotein and ABCG2 based on the antiviral azidothymidine. |
| AID125167 | In vitro Cytotoxic concentration in mock-infected A3.01 cells. | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID1053504 | Induction of AZT-resistant HIV1 reverse transcriptase assessed as rate of ATP-mediated excision of chain-terminating nucleotides by phosphorimaging analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID1209581 | Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
| AID1610035 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 VB59 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID105692 | Inhibitory activity against resistant HIV-1 strain NevR was determined. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
| Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
| AID1693429 | Antiviral activity against HIV-1 NL4-3 in human MT-4 cells assessed as virus induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Potent leads based on CA-19L, an anti-HIV active HIV-1 capsid fragment. |
| AID154940 | Cytotoxicity against uninfected PHA-stimulated peripheral blood mononuclear (PBM) cells | 1993 | Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
| L-beta-(2S,4S)- and L-alpha-(2S,4R)-dioxolanyl nucleosides as potential anti-HIV agents: asymmetric synthesis and structure-activity relationships. |
| AID46380 | Antiviral activity against site directed resistant isolate HIV-1 V106A in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID342001 | Antimicrobial activity against Streptococcus pyogenes AP1 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID548834 | Antiviral activity against HIV1 isolate 203 harboring reverse transcriptase M41L/L210W/T215Y/M184V mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID662533 | Displacement of [125I]-CXCL12 from CXCR4 expressed in human Jurkat cells at 10 uM relative to T140 | 2012 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 22, Issue:12
| Pharmacophore-based small molecule CXCR4 ligands. |
| AID757625 | Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID583847 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K mutant infected in human SupT1 cells derived from 9 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID83418 | Effective concentration required for antiviral activity against HIV strain MN by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID105007 | cytotoxic activity in MT-4 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID644273 | Antiviral activity against X4 tropic HIV1 NL4-3 in MT4 cells assessed as protection from virus-induced cytopathogenicity after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
| Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins. |
| AID1068977 | Antiviral activity against HIV-2 ROD infected in human CEM/0 cells | 2014 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3
| Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents. |
| AID346972 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Studies on anti-HIV quinolones: new insights on the C-6 position. |
| AID417260 | Cmax in HIV-infected human assessed as zidovudine diphosphate level in PBMC at 600 mg QD for 7 days measured per 10'6 cells in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID1223467 | Ratio of Vmax to Km in non-diabetic human liver microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID320327 | Cytotoxicity against human MT2 cells | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor. |
| AID576381 | Antiviral activity against Human immunodeficiency virus 1 3B infected in AA5 cells infected with 1.56 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1223450 | Ratio of Vmax to Km in diabetic human kidney microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID548575 | Antiviral activity against HIV1 isolate 061 harboring reverse transcriptase M41L/D67N/K70R/M184V/L210W/T215Y/K219E mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID635864 | Competitive inhibition of Mycobacterium tuberculosis TMPK by Lineweaver-Burk analysis | 2011 | Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24
| Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase. |
| AID1815389 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID1447282 | Inhibition of HIV1 3B dinucleoside reverse transcriptase infected in human P4R5 MAGI cells assessed as reduction in viral infection after 2 hrs by Galacto-Star beta-galactosidase reporter gene assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
| Synthesis and anti-HIV activities of unsymmetrical long chain dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID154954 | Activity against Lamivudine-resistant virus (HIV-1M184V) in human PBM cells, expressed as EC50 | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| l-2',3'-Didehydro-2',3'-dideoxy-3'-fluoronucleosides: synthesis, anti-HIV activity, chemical and enzymatic stability, and mechanism of resistance. |
| AID1815379 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID104772 | Concentration required to reduce the viability of mock-infected MT-4 cells by 50% | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
| 2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones. |
| AID548310 | Antiviral activity against HIV1 subtype B isolate 92TH026 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1231487 | Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
| AID1884488 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against NNRTI resistant HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID1888703 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | | | |
| AID519892 | Selectivity ratio of EC50 for 0.05 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.05 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID1223447 | Uncompetitive substrate inhibition of UGT2B7 in diabetic human liver microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID1292009 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
| AID1357797 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID1220791 | Ratio of drug level in blood to plasma in monkey | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID405581 | Toxicity against human H9c2 cells assessed as inhibition of cell proliferation at 50 uM after 6 days by SRB assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID1238309 | Cytotoxicity against human MT4 cells by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID154932 | Effective conc. required to achieve 50% inhibition of HIV-1 IIIB multiplication in PBM (peripheral blood mononuclear) cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID576386 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 0.78 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID79132 | Inhibitory concentration required to inhibit uninfected H9 cell growth by 50% | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
| Anti-AIDS agents. Part 47: Synthesis and anti-HIV activity of 3-substituted 3',4'-Di-O-(S)-camphanoyl-(3'R,4'R)-(+)-cis-khellactone derivatives. |
| AID83424 | Effective concentration required for antiviral activity against HIV strain SKI by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID153100 | Cytotoxicity against human peripheral blood mononuclear cells. | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID1204141 | Cytotoxicity against human A549 cells after 48 hrs by SRB method | 2015 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
| PMA-SiO2 catalyzed synthesis of indolo[2,3-c]quinolines as potent anti cancer agents. |
| AID83420 | Effective concentration required for antiviral activity against HIV strain RF by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID218498 | Antiviral activity against HSV-1 strain F in Vero cells on day 2 | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID79307 | Compound was evaluated for cytotoxicity in H9 lymphocytes | 1998 | Bioorganic & medicinal chemistry letters, May-19, Volume: 8, Issue:10
| Anti-AIDS agents. 32. Synthesis and anti-HIV activity of betulin derivatives. |
| AID548564 | Selectivity ratio of EC50 for HIV1 7324-1 harboring reverse transcriptase 41L/67N/69N/70R/215F/219E mutant gene infected in human PBMC to EC50 for HIV1 NL 4-3 expressing wild type reverse transcriptase infected in human PBMC | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1357784 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID1504695 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
| Discovery of Thiophene[3,2- |
| AID1693431 | Cytotoxicity against in human MT-4 after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Potent leads based on CA-19L, an anti-HIV active HIV-1 capsid fragment. |
| AID397589 | Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of virus-induced cytopathic effect by formazan-based conventional colorimetric technique | 2001 | Journal of natural products, Feb, Volume: 64, Issue:2
| Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program. |
| AID548585 | Antiviral activity against HIV1 isolate 162 harboring reverse transcriptase A62V/V75I/F77L/Y115F/F116Y/Q151M/M184V mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID556527 | Antiviral activity against Human immunodeficiency virus 1 clone 14682 harboring 122E, 135V, Q145V, 200A mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility. |
| AID1231849 | Selectivity index, CC50 for african green monkey Vero cells to EC50 for HIV1 3B | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6
| Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication. |
| AID291848 | Antiviral activity against HTLV1 in human PBMC | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
| Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents. |
| AID1316804 | Antiviral activity against HIV-2 ROD infected in human MT-4 cells assessed as protection against virus induced cytopathic effect after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
| Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
| AID278016 | Cytotoxicity against C8166 cells by MTT assay | 2007 | Journal of natural products, Feb, Volume: 70, Issue:2
| Tetranorclerodanes and clerodane-type diterpene glycosides from Dicranopteris dichotoma. |
| AID78946 | Inhibitory concentration against HIV-1 infected H9 cell lines | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID199850 | Effective concentration that reduces HIV-induced cytopathic effect by 50% was determined by reverse transcriptase (RT) assay. | 1993 | Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
| Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs. |
| AID1223473 | Drug metabolism in diabetic human liver microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID1561720 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenes | | | |
| AID1265601 | Cytotoxicity against human MT4 cells by cellTiterGlo assay | 2015 | Journal of natural products, Nov-25, Volume: 78, Issue:11
| Stelleralides D-J and Anti-HIV Daphnane Diterpenes from Stellera chamaejasme. |
| AID747598 | Cytotoxicity against human CEM cells | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors. |
| AID1156486 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
| AID1410404 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4
| Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
| AID1726076 | Antiviral activity against HIV 1 NL4-3 infected in human MT4 cells assessed as reduction in viral replication and measured on day 3 post infection by Nano-glo luciferase reporter assay | 2020 | ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
| Novel Betulinic Acid-Nucleoside Hybrids with Potent Anti-HIV Activity. |
| AID548571 | Antiviral activity against HIV1 isolate 056 expressing wild type reverse transcriptase gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID548540 | Antiviral activity against HIV2 isolate CDC310319 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID738315 | Inhibition of HIV1 reverse transcriptase | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors. |
| AID548818 | Antiviral activity against HIV1 isolate 069 harboring reverse transcriptase D67E/T69SSG/V75M/M184V/L210W/T215Y mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1763900 | Antiviral activity against HIV-1 IIIB harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID1165077 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
| AID341351 | Metabolic stability of the compound in human CD4+ CEM cells assessed as 3'-azido-2',3'-dideoxythymidine triphosphate intracellular levels at 200 nM after 8 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosine. |
| AID779527 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
| Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
| AID1238313 | Antiviral activity against T-cell line-tropic HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID105159 | Effective concentration required to achieve 50% protection of MT-4 cells against cytopathic effect of HIV-2 (8 days) | 1994 | Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
| Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs. |
| AID1221969 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID79297 | Anti-HIV activity in acutely infected H9 lymphocytes. | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
| Anti-AIDS agents. 15. Synthesis and anti-HIV activity of dihydroseselins and related analogs. |
| AID104440 | Average antiviral activity against HIV-1 in MT-4 cells using cell-protection assay | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17
| 3'-Azido-3',5'-dideoxythymidine-5'-methylphosphonic acid diphosphate: synthesis and HIV-1 reverse transcriptase inhibition. |
| AID1632126 | Cytotoxicity against HDF assessed as reduction in cell survival after 72 hrs by sulforhodamine B assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis, Antibacterial, and Anticancer Evaluation of Novel Spiramycin-Like Conjugates Containing C(5) Triazole Arm. |
| AID571593 | Ratio of AUC (0 to 12 hrs) in HIV-1 infected patient on day 10 to AUC ( 0 to 12 hrs) in HIV-1 infected patient on day 1 | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID222388 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 24 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID333023 | Antiviral activity against HIV1 3B in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2
| Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. |
| AID664466 | Antiviral activity against HIV1 3B infected in HeLa P4/R5 cells assessed as reduction of viral infection incubated for 2 hrs followed by incubated in drug-free medium for 46 hrs by single round infection beta-galactosidase reporter gene assay | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
| Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors. |
| AID718522 | Antiviral activity against HIV-1 3B infected in MT4 cells assessed as inhibition of virus-induced cytopathicity | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| POMA analyses as new efficient bioinformatics' platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues. |
| AID1174085 | Cytotoxicity against human PBMC | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Synthesis and antiviral evaluation of 2-amino-6-carbamoylpurine dioxolane nucleoside derivatives and their phosphoramidates prodrugs. |
| AID747599 | Cytotoxicity against human PBMC | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors. |
| AID576385 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 1.56 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID153105 | Inhibition of HIV-1 (BaL) cytopathicity in human peripheral blood mononuclear cells. | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID152794 | Tested in vitro for cytotoxicity against PBM cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID46047 | Inhibitory activity against the cytopathic effect of HIV-2 G910-6(AZT-res) strain in CEM-SS cells | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
| Unusual single-stranded polyribonucleotides as potent anti-HIV agents. |
| AID81411 | Inhibition of HIV-1 replication in human peripheral blood mononuclear cells. | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
| Synthesis and antiviral activity of various 3'-azido analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1, HTLV-III/LAV). |
| AID373367 | Drug metabolism in human CEM cells assessed as radioactive stavudine diphosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID551465 | Cytotoxicity against human C1866 cells after 72 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents. |
| AID1221956 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID82927 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 26 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1443668 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID45808 | Antiviral activity in HIV-2 infected CEM cells which are deficient in Thymidine Kinase | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID548803 | Antiviral activity against HIV1 isolate 201 harboring reverse transcriptase M41L/L210W/T215Y mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1610054 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 NARI-DR infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID1604015 | Cytotoxicity against human C8166 cells assessed as reduction in cell viability | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review. |
| AID548544 | Antiviral activity against HIV1 subtype A isolate 92UG029 infected in human MDM after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID576390 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human H9 cells infected with 25 uL of virus stock assessed as expression of p24 antigen after 6 days postinfection by ELISA | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID717448 | Antiviral activity against HCV assessed as inhibition of viral replication at 10 uM | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Synthesis, evaluation of anti-HIV-1 and anti-HCV activity of novel 2',3'-dideoxy-2',2'-difluoro-4'-azanucleosides. |
| AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
| Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
| AID679158 | TP_TRANSPORTER: uptake in OCT2-expressing HEK293 cells | 2002 | Journal of the American Society of Nephrology : JASN, Jul, Volume: 13, Issue:7
| cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. |
| AID1466377 | Antiviral activity against HIV-1 assessed as inhibition of virus-induced syncytia formation | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | Indoles as therapeutics of interest in medicinal chemistry: Bird's eye view. |
| AID747601 | Cytotoxicity against human HuH7 cells assessed as reduction in rRNA levels at 120 hrs by RT-PCR analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors. |
| AID354615 | Cytotoxicity against mock-infected human H9 cells after 4 days | 1996 | Journal of natural products, Nov, Volume: 59, Issue:11
| Two new lignans, interiotherins A and B, as anti-HIV principles from Kadsura interior. |
| AID576380 | Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 0.78 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID1763902 | Antiviral activity against HIV-1 IIIB harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
| AID14573 | Pharmacokinetic parameter AUC in mice following a single dose intravenous administration of the compound | 1996 | Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
| Nucleoside conjugates. 15. Synthesis and biological activity of anti-HIV nucleoside conjugates of ether and thioether phospholipids. |
| AID152631 | The compound was tested for antiviral activity against AZT sensitive 10 HIV in PBM cells. | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID1203628 | Downregulation of Bcl2 mRNA expression in human 5637 cells at 100 uM after 48 hrs by real-time PCR analysis relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID1594065 | Cytotoxicity against cat FL-4 cells measured after 7 days by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Synthesis and comparison of substituted 1,2,3-dithiazole and 1,2,3-thiaselenazole as inhibitors of the feline immunodeficiency virus (FIV) nucleocapsid protein as a model for HIV infection. |
| AID523357 | Antiviral activity against HIV1 with RT connection domain G190A mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID83229 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1267612 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-2 ROD | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity. |
| AID576200 | Antiviral activity against of Human immunodeficiency virus 1 3B infected in AA5 cells infected with 3.13 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID675189 | Cytotoxicity against human CEM-SS cells by XTT method | 2012 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
| Synthesis and anti-HIV activities of symmetrical dicarboxylate esters of dinucleoside reverse transcriptase inhibitors. |
| AID569567 | Therapeutic index, ratio of CC50 for human C1866 cells to EC50 for HIV1-3B | 2011 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
| Compounds from Kadsura angustifolia with anti-HIV activity. |
| AID222498 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT after 1 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID228862 | Antioxidant activity was evaluated by measuring the inhibition of oxidation of ABTS to ABTS+ by metmyoglobin in the presence of H2O2. | 2000 | Bioorganic & medicinal chemistry letters, Jan-03, Volume: 10, Issue:1
| Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity. |
| AID635302 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
| AID1223468 | Uncompetitive substrate inhibition of UGT2B7 in non-diabetic human liver microsomes assessed as reduction in enzyme-mediated zidovudine glucuronide formation by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID471325 | Antiviral activity against HIV-1 NL4-3 expressing VSV-G envelope infected in human 293T cells assessed as inhibition of viral replication after 48 hrs by Luciferase reporter gene assay | 2009 | Journal of natural products, Sep, Volume: 72, Issue:9
| Chemical Constituents of the Roots of Euphorbia micractina. |
| AID83066 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID153101 | Cytotoxicity against human peripheral blood mononuclear cells. | 2001 | Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
| New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID572974 | Ratio of IC50 for HIV1 harboring reverse transcriptase M41L/D67N/K70R/T215F/K219Q mutant infected in human HeLa P4/R5 cells to wild type HIV1 infected in human HeLa P4/R5 cells | 2009 | Antimicrobial 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. |
| AID604023 | Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID152649 | Cytotoxicity in peripheral blood mononuclear cells (PBM). | 1992 | Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
| Asymmetric synthesis of 1,3-dioxolane-pyrimidine nucleosides and their anti-HIV activity. |
| AID525109 | Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137. |
| AID519891 | Selectivity ratio of EC50 for 0.02 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.02 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID279915 | Increase in body weight in cafteria-fed Wistar rat at 70 mg/kg/day after 4 weeks | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID1316331 | Antiviral activity against HIV2 ROD harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID102615 | Tested in vitro for anticancer activity against MCF-7 cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID106587 | Concentration of compound required to reduce the viability of mock infected MT-4 cells against HIV-1 by 50% | 1991 | Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
| Specific anti-HIV-1 "acyclonucleosides" which cannot be phosphorylated: synthesis of some deoxy analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID1316328 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID46818 | The cytotoxicity was measured on wild type CEM/O cells. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| cycloSal-2',3'-dideoxy-2',3'-didehydrothymidine monophosphate (cycloSal-d4TMP): synthesis and antiviral evaluation of a new d4TMP delivery system. |
| AID51036 | Drug concentration which inhibits 50% of growth of cord blood mononuclear cells (CBMCs) | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID104997 | Effective concentration required to protect MT-2 cells against cytopathogenicity of HIV-1 LAI | 2003 | Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
| A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude. |
| AID548323 | Antiviral activity against HIV1 subtype G isolate JV1038 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID542940 | Cytotoxicity against mouse 3T3-F442A cells at 6 uM after 24 hrs by trypan blue staining | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Zidovudine impairs adipogenic differentiation through inhibition of clonal expansion. |
| AID15242 | Percentage of total protein recovered in S3 which is the soluble fraction in mouse brain after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID230127 | Tested for the ratio between CC50 (MT-4) to EC50 (MT-4) | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| 1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity. |
| AID1884221 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
| AID449424 | Inhibition of HIV1 reverse transcriptase SSGR/T215Y mutant-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| The nucleoside analogue D-carba T blocks HIV-1 reverse transcription. |
| AID79277 | Anti-HIV activity was evaluated as the concentration required to inhibit the growth of uninfected H9 lymphocyte cells by 50% | 1998 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
| Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs. |
| AID373381 | Stability in human CEM cells assessed as intracellular radioactive phosphorylated metabolite accumulation at 2 uM incubated for 24 hrs measured after 8 hrs of compound removal assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID610676 | Cytotoxicity against human C8166 cells by MTT assay | 2011 | Journal of natural products, Jun-24, Volume: 74, Issue:6
| Tigliane-type diterpenoid glycosides from Euphorbia fischeriana. |
| AID1320866 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
| AID1053506 | Ratio of EC50 for NNRTI-resistant Human immunodeficiency virus 1 to EC50 for wild type Human immunodeficiency virus 1 expressing p24 | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID492522 | Antiviral activity against HIV1 3B infected in H9 cells assessed as inhibition of viral replication by p24 antigen ELISA | 2010 | Journal of natural products, Mar-26, Volume: 73, Issue:3
| Discovery and development of natural product-derived chemotherapeutic agents based on a medicinal chemistry approach. |
| AID83065 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 7 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID300153 | Selectivity index, ratio of CC50 for rhesus monkey MA104 cells to IC50 for Rotavirus RF after attachment to Caco-2 cells | 2007 | Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
| Exomethylene pyranonucleosides: efficient synthesis and biological evaluation of 1-(2,3,4-trideoxy-2-methylene-beta-d-glycero-hex-3-enopyranosyl)thymine. |
| AID619643 | Ratio of EC50 for HIV-1 3B harboring RT L100I mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID538997 | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs | 2010 | Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23
| Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds. |
| AID523356 | Antiviral activity against HIV1 with RT connection domain Y181C/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID382985 | Cytotoxicity against human Caco-2 cells after 72 hrs | 2008 | European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
| Unsaturated fluoro-ketopyranosyl nucleosides: synthesis and biological evaluation of 3-fluoro-4-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine and N(6)-benzoyl adenine. |
| AID587740 | Selectivity index, ratio of CC50 for human HeLa-T4 cells to EC50 for single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
| Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
| AID279914 | Increase in body weight in lean Wistar rat at 70 mg/kg/day after 4 weeks | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID357410 | Inhibition of HIV1 delta env/VSV-G replication in human sup T1 T-lymphoid H9 cells assessed as inhibition of total viral DNA at 2 uM after 2 hrs by RT-PCR | 2007 | The Journal of biological chemistry, May-25, Volume: 282, Issue:21
| Interaction between HIV-1 Rev and integrase proteins: a basis for the development of anti-HIV peptides. |
| AID154773 | Antiviral activity against TEKI virus strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID8002 | Observed volume of distribution | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
| Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID515880 | Antimalarial activity against Plasmodium falciparum 3D7 after 48 hrs by SYBR green assay | 2010 | Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
| Potential application of thymidylate kinase in nucleoside analogue activation in Plasmodium falciparum. |
| AID571594 | Tmax in HIV-1 infected patient at 200 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID105376 | Cytotoxic dose in MT-4 cells | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
| 3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues. |
| AID278017 | Antiviral activity against HIV1 | 2007 | Journal of natural products, Feb, Volume: 70, Issue:2
| Tetranorclerodanes and clerodane-type diterpene glycosides from Dicranopteris dichotoma. |
| AID47476 | Total viral index (TAI) is the area between the cytotoxicity and the antiviral activity curve for CEM cells. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID1223465 | Drug metabolism in non-diabetic human liver microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID45197 | Compound was evaluated for the effect of Order of Addition on Cytoprotection against HIV-1RF at dilution 1000, Pretreat with 100 uM | 1999 | Journal of medicinal chemistry, Apr-22, Volume: 42, Issue:8
| Chicoric acid analogues as HIV-1 integrase inhibitors. |
| AID548321 | Antiviral activity against HIV1 subtype F isolate 93BR020 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1193108 | Antiviral activity against Feline immunodeficiency virus infected in cat FL-4 cells assessed as inhibition of viral replication after 7 days by quantitative RT-PCR analysis | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Novel fused tetrathiocines as antivirals that target the nucleocapsid zinc finger containing protein of the feline immunodeficiency virus (FIV) as a model of HIV infection. |
| AID584081 | Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, H221Y, F227F/L, M230M/I mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
| Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
| AID1460944 | Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 harboring reverse transcriptase K103N mutant infected in MAGI-CCR5 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID105180 | Effective concentration of compound against HIV-1 IIIB strain in MT-4 cells | 2004 | Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
| New bicyclam-GalCer analogue conjugates: synthesis and in vitro anti-HIV activity. |
| AID155274 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain A17 (Y181C) in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
| N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1. |
| AID91481 | Binding constant against human serum albumin (HSA) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
| Cheminformatic models to predict binding affinities to human serum albumin. |
| AID235678 | Selectivity Index measured as ratio of CC50 to that of EC50. | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15
| Synthesis and anti-HIV-1 activity of a series of 1-alkoxy-5-alkyl-6-(arylthio)uracils. |
| AID105515 | The effective concentration required to achieve 50% protection of MT-4 cells against the cytopathic effect of HIV-2 virus LAV-2ROD | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID46819 | Antiviral activity was measured on HIV-1 in wild-type CEM/O cells | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
| cycloSal-2',3'-dideoxy-2',3'-didehydrothymidine monophosphate (cycloSal-d4TMP): synthesis and antiviral evaluation of a new d4TMP delivery system. |
| AID79107 | In vitro Cytotoxic concentration which destroyed HIV-1 LAV infected H9 cells completely | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID666135 | Selectivity index, ratio of CC50 for human MOLT3 cells to IC50 for HIV1 | 2012 | Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
| Truncated phosphonated C-1'-branched N,O-nucleosides: a new class of antiviral agents. |
| AID665275 | Selectivity index ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID106410 | Number of infected cells at 10e-4 concentration of compound was tested on MT-4 cells infected by HIV-1/IIB | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| HIV-1 reverse transcriptase inhibitor design using artificial neural networks. |
| AID79634 | Antiviral activity against Hepatitis-B virus 2.2.15(HBV) | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22
| Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides. |
| AID619641 | Ratio of EC50 for HIV-1 3B harboring RT K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
| AID1565096 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | | | |
| AID244675 | Therapeutic index expressed as ratio of IC50 for 50% toxicity to EC50 for 50% inhibition | 2004 | Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
| 3-O-Glutaryl-dihydrobetulin and related monoacyl derivatives as potent anti-HIV agents. |
| AID394137 | Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
| Synthesis, HIV-RT inhibitory activity and SAR of 1-benzyl-1H-1,2,3-triazole derivatives of carbohydrates. |
| AID1754640 | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
| AID1316330 | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
| AID154956 | Anti-HIV-1 activity against human peripheral blood mononuclear (PBM) cells infected with HIV-1 strain LAV | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
| Asymmetric synthesis and biological evaluation of beta-L-(2R,5S)- and alpha-L-(2R,5R)-1,3-oxathiolane-pyrimidine and -purine nucleosides as potential anti-HIV agents. |
| AID571619 | Drug level in HIV-1 infected patient urine on day 10 by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID1460928 | Cytotoxicity against human MAGI-CCR5 cells assessed as reduction in cell viability after 48 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
| An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
| AID1053513 | Cytotoxicity against human CEM-SS cells assessed as cell viability after 6 days by MTS assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. |
| AID279919 | Increase in total cholesterol level in cafteria-fed Wistar rat at 70 mg/kg/day relative to control | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Site-specific reduction of oxidative and lipid metabolism in adipose tissue of 3'-azido-3'-deoxythymidine-treated rats. |
| AID548320 | Antiviral activity against HIV1 subtype F isolate 93BR019 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1884493 | Antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID1226480 | Antiviral activity against Dengue virus infected in BHK pD2-hRucPac-2ATG cells assessed as inhibition of viral replication at 10 uM after 3 days by luciferase reporter gene assay relative to control | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| 5'-Silylated 3'-1,2,3-triazolyl Thymidine Analogues as Inhibitors of West Nile Virus and Dengue Virus. |
| AID46840 | Cytotoxic concentration required to reduce viability of uninfected cells in CEM/TK cell line | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
| S-acyl-2-thioethyl phosphoramidate diester derivatives as mononucleotide prodrugs. |
| AID519876 | Antiviral activity against 0.02 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID82931 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of CEM-CL13 on at 7 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID105126 | Compound was evaluated for its inhibitory effect on the replication of HIV-2 (ROD) in MT-4 cells | 2003 | Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
| Synthesis and biological evaluation of thymine nucleosides fused with 3',4'-tetrahydrofuran ring. |
| AID658566 | Resistance factor, ratio of EC50 for multidrug-resistant HIV1 695-RT infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
| AID548538 | Antiviral activity against HIV1 group O isolate BCF02 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1729158 | Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
| AID79287 | Concentration that inhibits uninfected H9 cell growth by 50%. | 2003 | Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
| Anti-AIDS agents 54. A potent anti-HIV chalcone and flavonoids from genus Desmos. |
| AID423785 | Antiviral activity against non-nucleoside reverse transcriptase inhibitor-resistant HIV1 bearing reverse transcriptase N119 (Y181C) mutation infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID378446 | Cytotoxicity against mock-infected human H9 lymphocytes | 2006 | Journal of natural products, Sep, Volume: 69, Issue:9
| Tripfordines A-C, sesquiterpene pyridine alkaloids from Tripterygium wilfordii, and structure anti-HIV activity relationships of Tripterygium alkaloids. |
| AID222678 | In Vivo detection of total AZT in Mice brains after oral administration of 20 mg/kg after 2 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID222496 | In Vivo detection in Mice brains after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 8 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID105008 | Anti HIV-1 activity in human lymphocyte MT-4 cell line | 1993 | Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
| Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT. |
| AID217731 | Cytotoxicity was determined in the vero cells infected with HIV-I | 1993 | Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
| Asymmetric synthesis and biological evaluation of beta-L-(2R,5S)- and alpha-L-(2R,5R)-1,3-oxathiolane-pyrimidine and -purine nucleosides as potential anti-HIV agents. |
| AID1237700 | Antiviral activity against HIV2 ROD infected in human CEM/0 cells assessed as reduction in virus-induced giant cell formation incubated for 4 to 5 days | 2015 | Journal of medicinal chemistry, Aug-13, Volume: 58, Issue:15
| Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides. |
| AID1357794 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID548573 | Antiviral activity against HIV1 isolate 058 harboring reverse transcriptase M41L/D67N/K70R/L210W/T215F/K219Q mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID573996 | Ratio of EC50 for Human immunodeficiency virus 1 3B to EC50 for L-870,810-resistant Human immunodeficiency virus harboring L74M, E92Q and S230N mutations in integrase | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID355255 | Selectivity index, ratio of IC50 for human PBMC to EC50 for HIV1 LAV-1 | 1997 | Journal of natural products, Sep, Volume: 60, Issue:9
| In vitro anti-HIV activity of biflavonoids isolated from Rhus succedanea and Garcinia multiflora. |
| AID19826 | Partition coefficient (logP) | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
| Lipophilic, acid-stable, adenosine deaminase-activated anti-HIV prodrugs for central nervous system delivery. 2. 6-Halo and 6-alkoxy prodrugs of 2'-beta-fluoro-2',3'-dideoxyinosine. |
| AID56389 | Selective index is the ratio of inhibitory concentrations of cellular DNA polymerase delta to HIV-1 reverse transcriptase | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Discovery, synthesis, and bioactivity of bis(heteroaryl)piperazines. 1. A novel class of non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID326390 | Cytotoxicity against human C8166 cells after 72 hrs by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 18, Issue:7
| 1-Aryl-tetrahydroisoquinoline analogs as active anti-HIV agents in vitro. |
| AID232764 | Selectivity index of HIV-1 and HIV-2 with respect to CEM cells | 1997 | Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
| Novel 3'-C/N-substituted 2',3'-beta-D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties. |
| AID154809 | Cytotoxic concentration which reduces the cell viability of HIV-1 IIIB infected PBM (peripheral blood mononuclear) cells | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| Synthesis and evaluation of "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase. |
| AID1610053 | Antiviral activity against HIV1 NARI-DR infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
| AID46937 | In vitro antiviral activity against CEM cell lines | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV activity of several 2'-fluoro-containing pyrimidine nucleosides. |
| AID1383896 | Antiviral activity against HIV1 Lai infected in human MOLT4 cells after 7 days by WST8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Polypharmacology in HIV inhibition: can a drug with simultaneous action against two relevant targets be an alternative to combination therapy? |
| AID222390 | In Vivo detection in Mice plasma after oral administration of 20 mg/kg detected in the form of AZT 5`-P after 48 hr | 1992 | Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
| Improved brain delivery of AZT using a glycosyl phosphotriester prodrug. |
| AID423786 | Antiviral activity against non-nucleoside reverse transcriptase inhibitor-resistant HIV1 bearing reverse transcriptase A17 (K103N, Y181C) mutation infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT | 2009 | Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
| Aryl nucleoside H-phosphonates. Part 16: synthesis and anti-HIV-1 activity of di-aryl nucleoside phosphotriesters. |
| AID571600 | Tmax in HIV-1 infected patient at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID635301 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
| Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
| AID681687 | TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.010? uM, AZT: 500 uM) in OCTN2-expressing HEK293 cells | 1999 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 291, Issue:2
| Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. |
| AID548806 | Antiviral activity against HIV1 isolate 206 harboring reverse transcriptase D67N/K70R mutant gene by phenosense assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID1483274 | Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
| AID1815378 | Anti-HIV activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
| AID452270 | Cytotoxicity against human PBMC after 5 days | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus. |
| AID584639 | Toxicity in human subcutaneous preadipocytes assessed as decrease of adiponectin expression at 6 uM after 30 days by ELISA | 2010 | Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
| Mitochondrial DNA depletion and respiratory chain activity in primary human subcutaneous adipocytes treated with nucleoside analogue reverse transcriptase inhibitors. |
| AID717449 | Cytotoxicity against african green monkey Vero cells | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Synthesis, evaluation of anti-HIV-1 and anti-HCV activity of novel 2',3'-dideoxy-2',2'-difluoro-4'-azanucleosides. |
| AID235028 | Therapeutic index (IC50/EC50) was determined | 2004 | Journal of medicinal chemistry, Jan-29, Volume: 47, Issue:3
| Anti-AIDS agents. 52. Synthesis and anti-HIV activity of hydroxymethyl (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone derivatives. |
| AID405337 | Toxicity against human HepG2/C3A cells assessed as inhibition of cell proliferation at 50 uM after 6 days by SRB assay | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID1238312 | Cytotoxicity against human MT4 cells by MTT assay in presence of 10 uM of chloroquine | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
| Anti-HIV screening for cell-penetrating peptides using chloroquine and identification of anti-HIV peptides derived from matrix proteins. |
| AID106892 | Anti-HIV activity against HIV-I H112-2 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID152632 | Tested in vitro for anti HIV-1 activity against PBM cells | 1999 | Journal of medicinal chemistry, Mar-11, Volume: 42, Issue:5
| Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase. |
| AID553574 | Antiviral activity against HIV1 ERS104pre infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID105590 | Cytotoxicity was tested in MT-4 cells by the XTT-microculture tetrazolium assay. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
| Synthesis and anti-HIV-1 activity of 2'-"up"-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC). |
| AID583457 | Cytotoxicity against human HepG2 cells assessed as inhibition of mitochondrial respiratory chain complex II activity at 50 uM after 15 days relative to control | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| In vitro mitochondrial toxicity of metacavir, a new nucleoside reverse transcriptase inhibitor for treatment of hepatitis B virus. |
| AID81263 | Effective concentration against cytopathicity of HIV-1 strain (HTLV IIIB) in CEM cell line | 2003 | Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
| Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription. |
| AID46377 | Antiviral activity against site directed resistant isolate HIV-1 K103N in CEM cells | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
| Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1203617 | Toxicity in rat liver assessed as effect on cell viability at 50 to 200 uM after 2 hrs by MTT reduction assay relative to control | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| New organochalcogen multitarget drug: synthesis and antioxidant and antitumoral activities of chalcogenozidovudine derivatives. |
| AID235631 | Selectivity index determined for CC50 (test II) to EC50 x 10e3; Not tested | 2001 | Bioorganic & medicinal chemistry letters, Jul-23, Volume: 11, Issue:14
| Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. |
| AID341999 | Antimicrobial activity against Staphylococcus aureus ATCC 29213 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID1357791 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
| AID104237 | Therapeutic index is the ratio between IC50/EC50 of HIV-I H112-2 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID333024 | Inhibition of PKC beta2 | 1994 | Journal of natural products, Feb, Volume: 57, Issue:2
| Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. |
| AID275090 | Cytotoxicity against MAGI-CCR5 cells | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
| Synthesis, in vitro antiviral evaluation, and stability studies of novel alpha-borano-nucleotide analogues of 9-[2-(phosphonomethoxy)ethyl]adenine and (R)-9-[2-(phosphonomethoxy)propyl]adenine. |
| AID680771 | TP_TRANSPORTER: uptake in OAT2-expressing S2 cells | 2002 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 300, Issue:3
| Human organic anion transporters and human organic cation transporters mediate renal antiviral transport. |
| AID426891 | Selectivity index, ratio of CC50 for human PBMC cells to EC50 for HIV1 | 2009 | Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
| Synthesis, antiviral activity and molecular modeling of oxoquinoline derivatives. |
| AID519864 | Antiviral activity against HIV1 subtype B-NL4-3 infected in 2 hrs pretreated human MT2 cells assessed as inhibition of multicycle replication measured on day 5 postinfection by RT SPA | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID676998 | Selectivity index, ratio of CC50 for human HeLa cells to IC50 for VSV-G pseudotyped HIV1 lentiviral particles | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
| Synthesis and evaluation of hybrid drugs for a potential HIV/AIDS-malaria combination therapy. |
| AID105530 | Effective dose of compound required to inhibit 50% of HIV-1 antigen production in MT-4 cultures. | 1996 | Journal of medicinal chemistry, Jun-07, Volume: 39, Issue:12
| Synthesis and potent anti-HIV-1 activity of novel 6-benzyluracil analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. |
| AID104262 | In vitro Cytotoxic concentration which reduced HIV-1 LAV infected MT-2 cells by 50 percent | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
| Synthesis and anti-HIV activity of 4'-azido- and 4'-methoxynucleosides. |
| AID449351 | Inhibition of HIV1 reverse transcriptase M184V mutant-mediated viral DNA synthesis in human HOS cells assessed as luciferase activity treated 3 hrs before infection measured after 48 hrs by luminescence assay | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| The nucleoside analogue D-carba T blocks HIV-1 reverse transcription. |
| AID157405 | The effective concentration required to achieve 50% protection of human peripheral blood lymphocytes against the cytopathic effect of HIV-1 virus HTLV-IIIB strain | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
| Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. |
| AID81085 | Anti HIV-1 activity against the virus NL4-3 using MAGI assay | 2002 | Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
| Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid. |
| AID519885 | Antiviral activity against 0.005 MOI wild type HIV1 NL4-3 infected in 2 hr-pretreated human MT2 cells measured after 5 days by MTS assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID44827 | Concentration which produces a 50% survival of HIV-1 infected cells relative to uninfected control C8166 cells | 2001 | Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
| Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. |
| AID576150 | Cytotoxicity against human PBMC assessed as cell viability at 1 uM by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID377971 | Antiviral activity against HIV1 3B infected in human H9 T cells after 4 days by ELISA | 1999 | Journal of natural products, Jan, Volume: 62, Issue:1
| Novel anti-HIV lancilactone C and related triterpenes from Kadsura lancilimba. |
| AID47612 | Minimum compound concentration that reduced cell viability by 25% for HIV replication in CEM cells. | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3
| Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides. |
| AID83563 | Tested for the determination of percentage protection at 20 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID548318 | Antiviral activity against HIV1 subtype E isolate CMU06 infected in human PBMC after 48 to 72 hrs by MTS assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID573985 | Antiviral activity against Reverse transcriptase inhibitor-resistant Human immunodeficiency virus 1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
| Preclinical evaluation of 1H-benzylindole derivatives as novel human immunodeficiency virus integrase strand transfer inhibitors. |
| AID1446815 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID1443661 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
| Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
| AID104427 | Conc. required to inhibit the cytopathicity on HIV-1 by 50% on MT-4 cells | 2001 | Journal of medicinal chemistry, Aug-30, Volume: 44, Issue:18
| New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation. |
| AID157571 | Antiviral activity against human peripheral blood mononuclear cells, infected with HIV-2(strain ROD-2) | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
| Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes. |
| AID1884539 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID1223471 | Ratio of Vmax to Km in non-diabetic human kidney microsomes assessed as UGT2B7-mediated zidovudine glucuronide formation per pmol protein by HPLC and LC-MS/MS method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
| Diabetes mellitus reduces activity of human UDP-glucuronosyltransferase 2B7 in liver and kidney leading to decreased formation of mycophenolic acid acyl-glucuronide metabolite. |
| AID405347 | Toxicity against human H9c2 cells assessed as effect on mitochondrial DNA copy numbers after 12 days | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
| Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs. |
| AID47426 | Evaluated in vitro for their potential toxic effects human CEM cells | 2003 | Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
| Synthesis, anti-HIV activity, and molecular mechanism of drug resistance of L-2',3'-didehydro-2',3'-dideoxy-2'-fluoro-4'-thionucleosides. |
| AID551042 | Inhibition of HIV1 reverse transcriptase activity after 1 hr by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
| Synthesis and biological activity of novel 5'-arylamino-nucleosides by microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction. |
| AID607875 | Cytotoxic activity against human MT4 cells assessed as viability of mock-infected cells after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors. |
| AID607806 | Antiviral activity against 0.06 MOI Human immunodeficiency virus 1 IIIB infected in C8166 cells assessed as reduction in virus-induced cytopathic effect after 3 days by syncytium reduction assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
| Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors. |
| AID571624 | Drug level in HIV-1 infected patient urine assessed as zidovudine-5-O-glucoronide level at 300 mg, po bid on day 10 coadministered with 500 mg, po bid amdoxovir by LC-MS/MS analysis | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Lack of pharmacokinetic interaction between amdoxovir and reduced- and standard-dose zidovudine in HIV-1-infected individuals. |
| AID252633 | Mean retention time in reversed phase HPLC (RP-18) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| Synthesis and biological evaluation of neutral and zwitterionic 3-carboranyl thymidine analogues for boron neutron capture therapy. |
| AID576383 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human CEM-SS cells infected with 1.56 uL of virus stock assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID154941 | Antiviral activity against HIV-1 strain LAI in PBM cells on day 6 | 1994 | Journal of medicinal chemistry, Aug-05, Volume: 37, Issue:16
| Synthesis and biological properties of 5-o-carboranyl-1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil. |
| AID491830 | Selectivity index, ratio of CC50 for human H9 cells to EC50 for HIV1 3B | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
| Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
| AID595596 | Selectivity index, ratio of CC50 for human PBMC infected with Human immunodeficiency virus 1 LAV1 to EC50 for Human immunodeficiency virus 1 LAV1 | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5
| Broad-spectrum antiviral activity including human immunodeficiency and hepatitis C viruses mediated by a novel retinoid thiosemicarbazone derivative. |
| AID154640 | Effective concentration required for antiviral activity against lymphocyte cell line of PBL cells of Human by XTT assay | 1994 | Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
| Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction. |
| AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID417262 | Cmax in HIV-infected human assessed as zidovudine monophosphate level in PBMC at 600 mg QD for 7 days measured per 10'6 cells in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID133199 | Quantity of anylate in P2 subregion in mouse brain that contains myelin fragments, synaptosomes (pinched-nerve endings), and mitochondria after Jugular Vein Injection | 1996 | Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
| In vivo biodistribution, pharmacokinetic parameters, and brain uptake of 5-halo-y-methoxy(or ethoxy)-5,6-dihydro-3'-azido-3'-deoxythymidine diastereomers as potential prodrugs of 3'-azido-3'-deoxythymidine. |
| AID245918 | Cytotoxic concentration against the mock infected MT-4 cells | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2
| Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. |
| AID614139 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 IIIB infected in human MT4 cells | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17
| Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
| AID373383 | Stability in human CEM cells assessed as intracellular radioactive triphosphate metabolite remaining at 2 uM incubated for 24 hrs measured after 4 hrs of compound removal assessed per 10'6 cells relative to 0 hrs after compound removal | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID83224 | Percent inhibition measured as the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 14 days at a concentration 1 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID1220796 | Drug metabolism in bile duct-cannulated rat assessed as glucuronide concentration in bile and urine at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
| Human pharmacokinetic prediction of UDP-glucuronosyltransferase substrates with an animal scale-up approach. |
| AID1743639 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L/V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
| AID42386 | Protection of C8166 cells against the cytopathic effect of HIV isolate CBL-1 | 1989 | Journal of medicinal chemistry, Mar, Volume: 32, Issue:3
| 1-(3-cyano-2,3-dideoxy-beta-D-erythro-pentofuranosyl)thymine (cyanothymidine): synthesis and antiviral evaluation against human immunodeficiency virus. |
| AID575956 | Antiviral activity against Human immunodeficiency virus 1 subtype B 302056 infected in phytohemagglutininin and interleukin-2-stimulated PBMC assessed as inhibition of viral Reverse transcriptase by [3H]TTP incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
| Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. |
| AID586317 | Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of gag gene expression at 0.27 ug/ml after 5 days post infection by quantitative real time RT-PCR | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
| Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
| AID1166453 | Antiviral activity against HIV1 infected in human A3.01 cells assessed as complete inhibition of viral replication at 20 uM | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
| Altertoxins with potent anti-HIV activity from Alternaria tenuissima QUE1Se, a fungal endophyte of Quercus emoryi. |
| AID83557 | Tested for the determination of percentage protection at 100 uM concentrations against HIV-1 in ATH8 Cells | 1990 | Journal of medicinal chemistry, May, Volume: 33, Issue:5
| Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS. |
| AID235319 | Selective index as the ratio of CC50 to that of IC50 value against CEM cells. | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
| Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro. |
| AID559939 | Antiviral activity against HIV1 JRCSF infected in human PBMC assessed as inhibition of viral p24 antigen production after 7 to 10 days by ELISA | 2009 | Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
| The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100. |
| AID548838 | Antiviral activity against HIV1 isolate 212 harboring reverse transcriptase L210W/T215Y mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID548836 | Antiviral activity against HIV1 isolate 206 harboring reverse transcriptase D67N/K70R mutant gene by phenosense assay relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. |
| AID617764 | Antiviral activity against HIV1 HxB2 infected in human TZM-bl cells assessed as inhibition of virus neutralization after 48 hrs by luciferase assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Synthesis and biological evaluation of 2',4'- and 3',4'-bridged nucleoside analogues. |
| AID23239 | Partition coefficient (logP) | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
| S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs. |
| AID417248 | Tmax in HIV-infected human assessed as zidovudine diphosphate level in PBMC at 600 mg QD for 7 days in presence of Lamivudine | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Intracellular pharmacokinetics of once versus twice daily zidovudine and lamivudine in adolescents. |
| AID104800 | Dose required to reduce the viability of mock-infected cells by 50%, determined by MTT method. | 1998 | Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
| Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication. |
| AID1197831 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
| AID718369 | Selectivity index, ratio of CC50 for HIV1 3B infected in human MT4 cells to EC50 for HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
| Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach. |
| AID523486 | Antiviral activity against HIV1 with RT connection domain L100I/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
| Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance. |
| AID45902 | Compounds were tested for cytotoxicity against CEM-SS cells in terms of incorporation of [3H]dThd | 1998 | Journal of medicinal chemistry, Apr-09, Volume: 41, Issue:8
| Design, synthesis, and antiviral evaluations of 1-(substituted benzyl)-2-substituted-5,6-dichlorobenzimidazoles as nonnucleoside analogues of 2,5,6-trichloro-1-(beta-D-ribofuranosyl)benzimidazole. |
| AID1298243 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
| 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
| AID747597 | Cytotoxicity against African green monkey Vero cells | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors. |
| AID487831 | Therapeutic index, ratio of IC50 for human MT2 cells to EC50 for HIV1 3B infected in human MT2 cells | 2010 | Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
| Anti-AIDS agents 82: synthesis of seco-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents. |
| AID83057 | Compound ability to inhibit the production of HIV reverse transcriptase (RT) in culture supernatant of monocytic U937 on at 11 days at a concentration 25 uM | 1991 | Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
| Lipophilic glycosyl phosphotriester derivatives of AZT: synthesis, NMR transmembrane transport study, and antiviral activity. |
| AID519889 | Selectivity ratio of EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by MTS assay to EC50 for 0.005 MOI HIV1 NL4-3 infected in human MT2 cells by RT assay | 2008 | Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
| Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. |
| AID373368 | Drug metabolism in human CEM cells assessed as radioactive stavudine triphosphate accumulation at 2 uM assessed per 10'6 cells | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4
| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1275546 | Antiviral activity against HIV1 3B expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
| AID154782 | Antiviral activity against subtype isolate C strain in PBLs (peripheral blood lymphocytes) | 2001 | Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
| The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID155624 | Inhibition of p24 expression in HIVD34-infected PBMC assay on day 4 at concentration of 4 nM | 1994 | Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
| Evaluation of a vitamin-cloaking strategy for oligopeptide therapeutics: biotinylated HIV-1 protease inhibitors. |
| AID718519 | Antiviral activity against HIV-2 ROD infected in MT4 cells assessed as protection against virus-induced cytopathicity relative to control | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| POMA analyses as new efficient bioinformatics' platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues. |
| AID153133 | Intracellular of AZT-TP concentrations in LAI/HIV-1 infected PMBCs was determined at a conc of 10 uM) | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
| Amino acid phosphoramidate monoesters of 3'-azido-3'-deoxythymidine: relationship between antiviral potency and intracellular metabolism. |
| AID355253 | Antiviral activity against HIV1 LAV-1 in PHA-stimulated human PBMC after 6 days | 1997 | Journal of natural products, Sep, Volume: 60, Issue:9
| In vitro anti-HIV activity of biflavonoids isolated from Rhus succedanea and Garcinia multiflora. |
| AID606415 | Antiviral activity against HIV1 harboring vesicular stomatitis virus glycoprotein infected in human 293T cells assessed as inhibition of viral replication after 48 hrs by luciferase activity based luminometer analysis | 2011 | Journal of natural products, May-27, Volume: 74, Issue:5
| Lathyrane diterpenoids from the roots of Euphorbia micractina and their biological activities. |
| AID1446814 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
| AID106890 | Anti-HIV activity against HIV-I A17 strain in MT2 cell line | 1996 | Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
| Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers. |
| AID342000 | Antimicrobial activity against Staphylococcus aureus CCM 885 after 20 hrs | 2007 | Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
| Deoxyribonucleoside kinases activate nucleoside antibiotics in severely pathogenic bacteria. |
| AID1761006 | Antiviral activity against wild type HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in viral infection measured after 1 day by luciferase reporter gene assay based luminiscence assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
| AID581053 | Cytotoxicity against differentiated mouse 3T3-F442A cells assessed as effect on total deoxynucleotides content at 10 uM after 2 to 10 days | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Effects of zidovudine and stavudine on mitochondrial DNA of differentiating 3T3-F442a cells are not associated with imbalanced deoxynucleotide pools. |
| AID229051 | Cytotoxicity against uninfected PHA-stimulated vero cells was determined. | 1993 | Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
| 1,3-dioxolanylpurine nucleosides (2R,4R) and (2R,4S) with selective anti-HIV-1 activity in human lymphocytes. |
| AID104944 | Concentration which reduced the viability of the HIV-1 infected MT-4 cells to 50% compared to untreated control cells | 1995 | Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
| Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs. |
| AID376301 | Antiviral activity against HIV1 3B in human C8166 cells assessed as inhibition of virus-induced cytopathic effect | 2006 | Journal of natural products, Apr, Volume: 69, Issue:4
| Nortriterpenoids from Schisandra lancifolia. |
| AID630372 | Cytotoxicity against human MCF7 cells assessed as cell survival after 72 hrs by sulforhodamine B colorimetric assay | 2011 | Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
| Synthesis and anticancer activity of 5'-chloromethylphosphonates of 3'-azido-3'-deoxythymidine (AZT). |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2014 | Acta crystallographica. Section D, Biological crystallography, Apr, Volume: 70, Issue:Pt 4
| 3'-Azidothymidine in the active site of Escherichia coli thymidine phosphorylase: the peculiarity of the binding on the basis of X-ray study. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3
| High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
| AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
| Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10
| Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |