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2,5-diaziridinyl-3-(hydroxymethyl)-6-methyl-1,4-benzoquinone

Description

2,5-diaziridinyl-3-(hydroxymethyl)-6-methyl-1,4-benzoquinone: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID129737846
SCHEMBL ID20817157
MeSH IDM0302128

Synonyms (2)

Synonym
2,5-diaziridinyl-3-(hydroxymethyl)-6-methyl-1,4-benzoquinone
SCHEMBL20817157

Toxicity

ExcerptReference
" RH1 was cytotoxic at nanomolar concentrations to all the cell lines, and was 2-3 times more toxic in the D7 cells with high DTD than in the other two cell lines."( Cytotoxicity of the bioreductive agent RH1 and its lack of interaction with radiation.
Hendry, JH; Kim, JY; Patterson, AV; Roberts, SA; Stratford, IJ; Valentine, H; Ward, TH; West, CM, 2004
)

Pharmacokinetics

ExcerptReference
" Furthermore, the pharmacokinetic and pharmacodynamic characteristics of RH1 formulated in different vehicles were measured in vivo using the validated comet-X assay in mice bearing human tumor xenografts."( Preclinical evaluation of the pharmacodynamic properties of 2,5-diaziridinyl-3-hydroxymethyl-6-methyl-1,4-benzoquinone.
Butler, J; Coe, NA; Cummings, J; Danson, S; Hargreaves, RH; Jayson, GC; McGown, AT; Ranson, M; Ward, TH, 2005
)
" Whilst it is impossible to cover all variations/conditions of a pharmacodynamic assay, we have strived to evaluate and demonstrate that this assay conforms to the three R's of validation, that is robustness, reliability and reproducibility."( Validation of the comet-X assay as a pharmacodynamic assay for measuring DNA cross-linking produced by the novel anticancer agent RH1 during a phase I clinical trial.
Cummings, J; Danson, S; Denneny, O; Ranson, M; Ward, TH, 2007
)
" It is ideally suited for the evaluation of the pharmacodynamic effects of DNA cross-linking agents undergoing early clinical trials."( Validation of the comet-X assay as a pharmacodynamic assay for measuring DNA cross-linking produced by the novel anticancer agent RH1 during a phase I clinical trial.
Cummings, J; Danson, S; Denneny, O; Ranson, M; Ward, TH, 2007
)
" Secondary objectives were assessment of toxicity, pharmacokinetic determination of RH1 and pharmacodynamic assessment of drug effect through measurement of DNA cross linking in peripheral blood mononuclear cells (PBMCs) and tumour, DTD activity in tumour and NAD(P)H:quinone oxidoreductase 1 (NQO1) polymorphism status."( Phase I pharmacokinetic and pharmacodynamic study of the bioreductive drug RH1.
Aarons, L; Cummings, J; Danson, SJ; Dawson, M; Denneny, O; Dickinson, G; Dive, C; Halbert, G; Johnson, P; Jowle, D; Ranson, M; Robson, L; Ward, TH; Watson, A, 2011
)
" Plasma pharmacokinetic analysis showed RH1 is rapidly cleared from blood (t(1/2) = 12."( Phase I pharmacokinetic and pharmacodynamic study of the bioreductive drug RH1.
Aarons, L; Cummings, J; Danson, SJ; Dawson, M; Denneny, O; Dickinson, G; Dive, C; Halbert, G; Johnson, P; Jowle, D; Ranson, M; Robson, L; Ward, TH; Watson, A, 2011
)

Dosage Studied

ExcerptReference
" Data obtained suggest a threshold for NQO1-induced toxicity above 23 nmol/min/mg and a sharp dose-response curve between the no effect level of NQO1 (23 nmol/min/mg) and the maximal effect level (>77 nmol/min/mg)."( Relationship between NAD(P)H:quinone oxidoreductase 1 (NQO1) levels in a series of stably transfected cell lines and susceptibility to antitumor quinones.
Butler, J; Dehn, DL; Hargreaves, RH; Moody, CJ; Ross, D; Swann, E; Winski, SL, 2001
)
"4 mg/kg) and daily dosing for 5 days delayed tumour growth relative to control."( Preclinical efficacy of the bioreductive alkylating agent RH1 against paediatric tumours.
Adamski, JK; Brookes, KE; Dive, C; Estlin, EJ; Hogg, A; Holt, SV; Hussein, D; Klymenko, T; Makin, GW; Ward, T, 2009
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (30)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (6.67)18.2507
2000's22 (73.33)29.6817
2010's6 (20.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (6.45%)5.53%
Reviews2 (6.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (87.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]