Etanidazole: A nitroimidazole that sensitizes hypoxic tumor cells that are normally resistant to radiation therapy.
etanidazole : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2-nitro-1H-imidazol-1-yl)acetic acid with the amino group of ethanolamine. Used as a radiosensitising agent for hypoxic tumour cells.
ID Source | ID |
---|---|
PubMed CID | 3276 |
CHEMBL ID | 47405 |
CHEBI ID | 75473 |
SCHEMBL ID | 4414 |
SCHEMBL ID | 20836613 |
SCHEMBL ID | 22493013 |
MeSH ID | M0026334 |
Synonym |
---|
KBIO1_000305 |
DIVK1C_000305 |
NCI60_002528 |
radinyl |
sp-2508 |
sr-2508 |
dup-435 |
sr 2508 |
n-(2-hydroxyethyl)-2-nitroimidazole-1-acetamide |
ethanidazole |
etanidazole [usan:inn] |
etanidazol [spanish] |
n-(2-hydroxyethyl)-2-nitro-1h-imidazole-1-acetamide |
etanidazolum [latin] |
n-(2-hydroxyethyl)-1-(2-nitro-1-imidazolyl)acetamide |
nsc 301467 |
brn 0919296 |
SPECTRUM_001574 |
BPBIO1_000723 |
PRESTWICK_1056 |
NCGC00016767-01 |
cas-22668-01-5 |
2-nitroimidazole-1-acetamide, n-(2-hydroxyethyl)- |
nsc-301467 |
1h-imidazole-1-acetamide, n-(2-hydroxyethyl)-2-nitro- |
mls003115757 , |
etanidazole (usan/inn) |
D04075 |
radinyl (tn) |
PRESTWICK3_000649 |
BSPBIO_000657 |
IDI1_000305 |
SPECTRUM5_001667 |
PRESTWICK2_000649 |
AB00052354 |
n-(2-hydroxyethyl)-2-(2-nitroimidazol-1-yl)acetamide |
radinyl(tm) |
etanidazole |
22668-01-5 |
2-(2-nitro-imidazol-1-yl)-n-2-hydroxyethylacetamide |
nsc301467 |
NCGC00095848-01 |
KBIOSS_002054 |
KBIO2_002054 |
KBIO2_007190 |
KBIOGR_001845 |
KBIO2_004622 |
PRESTWICK0_000649 |
SPBIO_000760 |
PRESTWICK1_000649 |
SPECTRUM4_001183 |
SPECTRUM2_000910 |
SPBIO_002578 |
NINDS_000305 |
SPECTRUM1503412 |
HMS2093E13 |
chebi:75473 , |
CHEMBL47405 |
smr001233273 |
HMS500P07 |
HMS1570A19 |
NCGC00016767-02 |
HMS2097A19 |
tox21_110599 |
dtxcid6025434 |
etandazole |
dtxsid8045434 , |
n-(2-hydroxyethyl)-2-(2-nitro-1h-imidazol-1-yl)acetamide |
CCG-39747 |
etanidazolum |
etanidazol |
30dka3q1hl , |
unii-30dka3q1hl |
etanidazole [mi] |
etanidazole [usan] |
etanidazole [mart.] |
etanidazole [inn] |
SCHEMBL4414 |
tox21_110599_1 |
NCGC00016767-05 |
n-(2-hydroxyethyl)-2-(2-nitro-1-imidazolyl)acetamide |
WCDWBPCFGJXFJZ-UHFFFAOYSA-N |
AKOS028109842 |
SR-05000001859-2 |
sr-05000001859 |
SR-05000001859-1 |
SBI-0051823.P002 |
HMS3714A19 |
DB12736 |
Q5402427 |
SCHEMBL20836613 |
ethylhydrocupreinehydrochloride |
SCHEMBL22493013 |
XAA66801 |
etanidazole-d4 |
Excerpt | Reference | Relevance |
---|---|---|
"01) less toxic than RK-28 at this dose, as reflected in a lower increase in the brain glucose level (0." | ( Metabolic studies and neurotoxicity in tumors and brain of mice after hypoxic cell sensitizers. Streffer, C; Tamulevicius, P, 1994) | 0.29 |
Etanidazole (Eta) was used in the RTOG randomized trial for Stage III and IV head and neck cancer. Pharmacokinetic data suggested t1/2 alpha and t1-2 beta for carboplatin were prolonged after pretreatment with etanidazoles.
The aim of the study was to evaluate the efficacy and toxicity of Etanidazole, a hypoxic cell sensitizer, combined with radiotherapy in the treatment of head and neck squamous cell carcinoma.
Excerpt | Reference | Relevance |
---|---|---|
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
Excerpt | Relevance | Reference |
---|---|---|
") was administered just prior to an alkylating agent, the combination treatment produced significantly more tumor cell killing across the dosage range of each alkylating agent tested compared with the alkylating agent alone." | ( Modulation of alkylating agents by etanidazole and Fluosol-DA/carbogen in the FSaIIC fibrosarcoma and EMT6 mammary carcinoma. Bubley, G; Coleman, CN; Eder, JP; Frei, E; Herman, TS; Holden, SA; Tanaka, J; Teicher, BA, 1991) | 0.56 |
" There remains the possibility that, on the basis of the combined drug dosage achieved, an increased therapeutic efficacy can be reached with either drug alone." | ( The combination of multiple doses of etanidazole and pimonidazole in 48 patients: a toxicity and pharmacokinetic study. Bleehen, NM; Maughan, TS; Newman, HF; Stenning, S; Ward, R; Workman, P, 1991) | 0.55 |
"To develop dosing criteria for the use of L-buthionine-S-sulfoximine (active diastereoisomer) as a glutathione depletor in the clinic, using a pharmacodynamic and pharmacokinetic in vitro-in vivo approach." | ( Pharmacodynamics of prolonged treatment with L,S-buthionine sulfoximine. Bump, EA; Coleman, CN; Griffith, OW; Hurwitz, SJ; Lai, LL; Malaker, K; Riese, N, 1994) | 0.29 |
" In the present study, the in vivo radiosensitizing activity of KU-2285 in combination with radiation dose fractionation, and the pharmacokinetics of cumulative dosing of KU-2285 in the peripheral nerves were examined." | ( Radiosensitizing activity and pharmacokinetics of multiple dose administered KU-2285 in peripheral nerve tissue in mice. Abe, M; Iwai, H; Matsuno, E; Sasai, K; Shibamoto, Y, 1994) | 0.29 |
" At low, therapeutically relevant radiation doses, where 2-nitroimidazoles are less efficient sensitizers, the preincubation effect may be even more important, but thiol depletion still minimizes its impact in this region of the dose-response curve." | ( Enhanced radiation-sensitivity by preincubation with nitroimidazoles: effect of glutathione depletion. Koch, CJ; Skov, KA, 1994) | 0.29 |
" We observed the release characteristics of etanidazole in the dosage forms of microspheres and discs, subjected to different preparation conditions." | ( PEG modulated release of etanidazole from implantable PLGA/PDLA discs. Lee, T; Wang, CH; Wang, F, 2002) | 0.88 |
" At a dosage of 50 Gy (total dosage during a radiotherapy treatment period) showed no apparent effects on the tri-phase release profile." | ( Sustained release system for highly water-soluble radiosensitizer drug etanidazole: irradiation and degradation studies. Wang, CH; Wang, J; Yip, EY, 2003) | 0.55 |
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
prodrug | A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug. |
alkylating agent | Highly reactive chemical that introduces alkyl radicals into biologically active molecules and thereby prevents their proper functioning. It could be used as an antineoplastic agent, but it might be very toxic, with carcinogenic, mutagenic, teratogenic, and immunosuppressant actions. It could also be used as a component of poison gases. |
radiosensitizing agent | A drug that makes increases the sensitivity of tumour cells to radiation therapy. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
imidazoles | A five-membered organic heterocycle containing two nitrogen atoms at positions 1 and 3, or any of its derivatives; compounds containing an imidazole skeleton. |
C-nitro compound | A nitro compound having the nitro group (-NO2) attached to a carbon atom. |
monocarboxylic acid amide | A carboxamide derived from a monocarboxylic acid. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 0.2371 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 0.2131 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 5.0119 | 0.0025 | 5.8400 | 31.6228 | AID899 |
thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 1.2589 | 0.0100 | 39.5371 | 1,122.0200 | AID1479 |
histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 0.5012 | 0.2512 | 15.8432 | 39.8107 | AID504327 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 14.1254 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1454814 | Hypoxia radiosensitization activity in human HCT116 cells assessed as sensitizer enhancement ratio by measuring ratio of radiation dose for 1% survival in absence to presence of compound at 1 mM preincubated for 1 hr followed by irradiation measured after | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454865 | Drug level in NIH-III mouse assessed as maximum achievable dose at 10 ml/kg, iv | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454878 | Tmax in tumor of NIH-III mouse xenografted with human HCT116 cells at 2.20 mmol/kg, iv administered as single dose by HPLC analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID408779 | Radiosensitizing activity in mouse EMT6/KU cells assessed as enhancement ratio reducing surviving fraction of cells at 1 mM after 5 to 7 days | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Design of antiangiogenic hypoxic cell radiosensitizers: 2-nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety. |
AID1454887 | Cytotoxicity against human HCT116 cells at anoxic IC50 incubated for 1 hr at 21 degC by sulforhodamine B assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454862 | Toxicity in NIH-III mouse xenografted with human HCT116 cells assessed as change in body weight with 15 Gy radiation at 2.20 mmol/kg, iv administered as single dose | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454882 | In vivo hypoxia radiosensitization activity in human HCT116 cells xenografted in NIH-III mouse assessed as survival ratio by measuring ratio of cell survival with 12.5 Gy radiation in absence to presence of compound at 2.20 mmol/kg, iv pretreated as singl | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
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. |
AID1454801 | Hypoxia radiosensitization activity in human HCT116 cells assessed as survival ratio by measuring ratio of cell survival with 15 Gy radiation in absence to presence of compound at anoxic IC50 preincubated for 1 hr followed by 15 Gy irradiation measured af | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454866 | Cmax in plasma of NIH-III mouse xenografted with human HCT116 cells at 2.20 mmol/kg, iv administered as single dose by HPLC analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
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. |
AID1454845 | Hypoxia radiosensitization activity in human HCT116 cells assessed as survival ratio by measuring ratio of cell survival with radiation in absence to presence of compound at 1 mM preincubated for 1 hr followed by 6 to 29 Gy irradiation measured after 10 d | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454797 | Solubility of the compound in alphaMEM containing 5% FCS and 1% DMSO by HPLC analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID689771 | Antitubercular activity against Mycobacterium tuberculosis H37Rv isolate ITR after 7 days by luminescence spectrometry | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis. |
AID1454888 | Electrophilicity of the compound in pH 7 phosphate buffer assessed as one-electron reduction potential | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454827 | Hypoxia radiosensitization activity in human HCT116 cells assessed as survival ratio by measuring ratio of cell survival with radiation in absence to presence of compound at 1 mM preincubated for 1 hr followed by 6 to 29 Gy irradiation measured after 10 d | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID689770 | Antitubercular activity against Mycobacterium tuberculosis H37Rv isolate SRI after 5 days by resazurin-based microplate assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis. |
AID1454798 | Cytotoxicity against human HCT116 cells incubated for 4 hrs under anaerobic condition measured after 5 days by sulforhodamine B assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454800 | Hypoxia radiosensitization activity in human HCT116 cells assessed as sensitizer enhancement ratio by measuring ratio of radiation dose for 1% survival in absence to presence of compound at 1 mM preincubated for 1 hr followed by irradiation measured after | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454874 | Cmax in tumor of NIH-III mouse xenografted with human HCT116 cells at 2.20 mmol/kg, iv administered as single dose by HPLC analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID689773 | Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiterGlo assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis. |
AID1454870 | Tmax in plasma of NIH-III mouse xenografted with human HCT116 cells at 2.20 mmol/kg, iv administered as single dose by HPLC analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID1454799 | Hypoxic cytotoxicity ratio of IC50 for human HCT116 cells under oxic condition to IC50 for human HCT116 cells under anoxic condition | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Next-Generation Hypoxic Cell Radiosensitizers: Nitroimidazole Alkylsulfonamides. |
AID689772 | Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 10 days in anaerobic condition followed by 48 hrs incubation in aerobic condition by LORA assay | 2012 | Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13 | Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 82 (26.11) | 18.7374 |
1990's | 111 (35.35) | 18.2507 |
2000's | 71 (22.61) | 29.6817 |
2010's | 41 (13.06) | 24.3611 |
2020's | 9 (2.87) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.79) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 49 (15.03%) | 5.53% |
Reviews | 18 (5.52%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 259 (79.45%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Assessment of Hypoxia in Malignant Gliomas Using EF5 [NCT00430079] | 48 participants (Actual) | Interventional | 2001-07-31 | Terminated(stopped due to Administratively complete.) | |||
Microenvironment: Imaging/Implications in Brain Tumors; A Preliminary Investigation of the Biodistribution of [F-18]-EF5 in Patients With Brain Tumors [NCT00110032] | Phase 1 | 46 participants (Actual) | Interventional | 2005-06-30 | Terminated(stopped due to Administratively complete.) | ||
The Detection of Tumor Hypoxia and Vascularity in Patients Undergoing Intraperitoneal Photodynamic Therapy [NCT00028782] | 80 participants (Actual) | Interventional | 2001-10-31 | Terminated(stopped due to Administratively complete.) | |||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |