Compounds > c 1311
Page last updated: 2024-12-07

c 1311

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

Description

C 1311: an imidazoacridinone; arrests cell-cycle progression in the G2 phase of L1210 cells; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132127
CHEMBL ID338604
SCHEMBL ID2442405
MeSH IDM0259901

Synonyms (30)

Synonym
mz4y5h4oab ,
unii-mz4y5h4oab
NCI60_015698
imidazoacridinone
symadex
c-1311 ,
xls-002
NEURO_000342 ,
5-((2-(diethylamino)ethyl)amino)-8-hydroxy-6h-imidazo(4,5,1-de)acridin-6-one
ccris 7541
c 1311
6h-imidazo(4,5,1-de)acridin-6-one, 5-((2-(diethylamino)ethyl)amino)-8-hydroxy-
CHEMBL338604 ,
5-(2-diethylamino-ethylamino)-8-hydroxy-2,10b-diaza-aceanthrylen-6-one(2.0mhcl.1.0mh2o)
bdbm50008347
5-(2-(diethylamino)ethylamino)-8-hydroxy-6h-imidazo[4,5,1-de]acridin-6-one
138154-39-9
5-((2-(diethylamino)ethyl)amino)-8-hydroxy-6h-imidazo[4,5,1-de]acridin-6-one
imidazoacridone
SCHEMBL2442405
DTXSID10160508
CUNDRHORZHFPLY-UHFFFAOYSA-N
symadex, >=98% (hplc)
138154-39-9 (free base)
symadex free base
5-((2-diethylamino)ethyl)amino)-8-hydroxy-6h-imidazo(4,5,1-de)acridin-6-one
NCGC00487207-01
Q27284307
6h-imidazo[4,5,1-de]acridin-6-one, 5-[[2-(diethylamino)ethyl]amino]-8-hydroxy-
10-[2-(diethylamino)ethylamino]-5-hydroxy-1,14-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-2(7),3,5,9,11,13(16),14-heptaen-8-one

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" All subjects experienced one or more treatment-related adverse events (AEs)."( Evaluation of the safety of C-1311 (SYMADEX) administered in a phase 1 dose escalation trial as a weekly infusion for 3 consecutive weeks in patients with advanced solid tumours.
Bourbouloux, E; Campone, M; Capizzi, R; Drouin, M; Fumoleau, P; Grieshaber, C; Isambert, N; Loadman, P; Major, A; Yin, W, 2010)		0.36

Pharmacokinetics

ExcerptReferenceRelevance
" Data are not available on the pharmacokinetic properties of this compound; therefore, the main aim of this project was to study the plasma pharmacokinetics and tissue and tumour distribution of C1311 in mice and to assess, prior to potential clinical application, whether these pharmacokinetics were linear with respect to the dose."( Pharmacokinetics and tissue distribution of the imidazoacridinone C1311 in tumour-bearing mice.
Bibby, MC; Calabrese, CR; Double, JA; Loadman, PM, 1998)		0.3
" Following treatment with an intraperitoneal injection, fibres were excised and cells retrieved for pharmacodynamic analysis using the comet assay/fluorescence microscopy."( The hollow fibre model--facilitating anti-cancer pre-clinical pharmacodynamics and improving animal welfare.
Bibby, MC; Cooper, PA; Shnyder, SD; Suggitt, M, 2006)		0.33

Bioavailability

ExcerptReferenceRelevance
"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

Dosage Studied

ExcerptRelevanceReference
" The pharmaceutical development of C1311 necessitated the availability of an assay for the quantification and purity determination of C1311 active pharmaceutical ingredient (API) and its pharmaceutical dosage form."( Development and validation of an LC-UV method for the quantification and purity determination of the novel anticancer agent C1311 and its pharmaceutical dosage form.
Beijnen, JH; den Brok, MW; Grieshaber, CK; Harvey, MD; Hillebrand, MJ; Nuijen, B, 2005)		0.33
" The compound is pharmaceutically formulated as a lyophilized product containing 100 mg C1311 (anhydrous free base) per dosage unit and requires reconstitution before intravenous administration."( Compatibility and stability of the novel anti-cancer agent C1311 in infusion devices and its in vitro biocompatibility.
Beijnen, JH; Buluran, JN; den Brok, MW; Grieshaber, CK; Harms, R; Harvey, MD; Nuijen, B, 2005)		0.33
" Continuous low C-1311 dosing (8 mg/kg/day for 5 days) gave similar inhibition of angiogenesis (80%), suggesting that low-dose, frequent C-1311 administration may be more effective in terms of reducing toxicity."( Anticancer imidazoacridinone C-1311 inhibits hypoxia-inducible factor-1α (HIF-1α), vascular endothelial growth factor (VEGF) and angiogenesis.
Brillowska-Dąbrowska, A; Konopa, J; Paradziej-Łukowicz, J; Peszyńska-Sularz, G; Skwarska, A, 2011)		0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC50 (µMol)0.13700.00271.62879.9000AID479979; AID621612
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km63.30005.00006.830010.0000AID1215438
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km28.90004.49006.51339.0000AID1215432
UDP-glucuronosyltransferase 1A10Homo sapiens (human)Km62.23332.74004.21005.6800AID1215415; AID1215416; AID1215441
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A9Homo sapiens (human)
quinone catabolic processRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 1A10Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A10Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A10Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A10Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
retinoic acid bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
dihydronicotinamide riboside quinone reductase activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
protein bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
zinc ion bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
electron transfer activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
oxidoreductase activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
oxidoreductase activity, acting on other nitrogenous compounds as donorsRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
chloride ion bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
protein homodimerization activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
FAD bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
melatonin bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
resveratrol bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
NAD(P)H dehydrogenase (quinone) activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A10Homo sapiens (human)
protein kinase C bindingUDP-glucuronosyltransferase 1A10Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A10Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A10Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A10Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
nucleoplasmRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
cytosolRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
extracellular exosomeRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
cytosolRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A10Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A10Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A10Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID621614Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2): crystal structures, biochemical activity, and intracellular effects of imidazoacridin-6-ones.
AID1215446Drug metabolism in human intestinal microsomes assessed as ratio of Vmax to Km for glucuronidation per mg of protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215435Activity of human recombinant UGT1A7 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1682833Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Structure-activity relationship of novel acridone derivatives as antiproliferative agents.
AID1215438Activity of human recombinant UGT1A9 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215411Drug metabolism in human jejunum microsomes assessed as glucuronidation activity at 0.1 mM for 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215443Ratio Vmax to Km for human recombinant UGT1A10 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215413Drug metabolism in human ileum microsomes assessed as glucuronidation activity at 0.1 mM for 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215433Activity of human recombinant UGT1A1 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID100464In vitro inhibitory activity against murine L1210 leukemia1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias.
AID1215451Activity of human recombinant UGT1A9 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein at 235 uM after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215429Activity of human recombinant UGT1A10 expressed in baculovirus-infected Sf9 cells assessed as metabolite formation at 200 uM after 60 mins by HPLC analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215426Activity of human recombinant UGT1A8 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID479980Toxicity in human HCT116 cells after 96 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2.
AID1096392Binding affinity to Bos taurus (calf) thymus DNA assessed as change in melting temperature at drug to DNA base pair ratio 0.25 M2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Nov, Volume: 20, Issue:8
Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies.
AID1215431Drug metabolism in human intestinal microsomes assessed as glucuronidation activity at 0.2 mM for 60 mins by ESI-MS analysis in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215417Activity of human recombinant UGT1A10 D396A mutant expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg of protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215439Activity of human recombinant UGT1A9 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215427Activity of human recombinant UGT1A9 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215440Ratio Vmax to Km for human recombinant UGT1A9 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215430Drug metabolism in human liver microsomes assessed as glucuronidation activity at 0.2 mM for 60 mins by ESI-MS analysis in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID621613Cytotoxicity against human HCT116 cells after 24 hrs by MTT assay2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2): crystal structures, biochemical activity, and intracellular effects of imidazoacridin-6-ones.
AID1215415Activity of human recombinant UGT1A10 D396A mutant expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215414Drug metabolism in human colon microsomes assessed as glucuronidation activity at 0.1 mM for 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215402Drug metabolism assessed as human recombinant UGT1A1-mediated compound formation treated with C-1311 for 60 mins by ESI-MS/UV-vis spectroscopy in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215428Activity of human recombinant UGT1A10 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215453Drug metabolism in human stomach microsomes assessed as glucuronidation activity at 0.1 mM for 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID479979Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2.
AID1215444Drug metabolism in human intestinal microsomes assessed as glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215447Drug metabolism in human liver microsomes assessed as glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215445Drug metabolism in human intestinal microsomes assessed as glucuronidation per mg of protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215410Drug metabolism in human duodenum microsomes assessed as glucuronidation activity at 0.1 mM for 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215423Activity of human recombinant UGT1A1 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215436Activity of human recombinant UGT1A7 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215441Activity of human recombinant UGT1A10 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215434Ratio Vmax to Km for human recombinant UGT1A1 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215416Activity of human recombinant UGT1A10 V92A mutant expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215452Inhibition of human recombinant UGT1A9 activity expressed in baculovirus-infected Sf9 cells2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215442Activity of human recombinant UGT1A10 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215419Drug metabolism in human intestinal microsomes assessed as metabolite formation treated with C-1311 for 60 mins by ESI-MS/UV-vis spectroscopy in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID479981Binding affinity to calf thymus DNA assessed as change in melting temperature at 10 uM relative to control2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2.
AID134763Toxicity in CDF1 male mice following a single intraperitoneal administration1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias.
AID1215422Drug metabolism assessed as human recombinant UGT1A7-mediated compound formation treated with C-1311 for 60 mins by ESI-MS/UV-vis spectroscopy in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215432Activity of human recombinant UGT1A1 expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215425Activity of human recombinant UGT1A7 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID139781Antineoplastic activity was evaluated in vivo against murine leukemia P388 (i.p./i.p.; days 1-5) and optimum dose was reported1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias.
AID1215421Drug metabolism assessed as human recombinant UGT1A9-mediated compound formation treated with C-1311 for 60 mins by ESI-MS/UV-vis spectroscopy in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215449Drug metabolism in human liver microsomes assessed as ratio of Vmax to Km for glucuronidation per mg of protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215412Drug metabolism in human small intestine microsomes assessed as glucuronidation activity at 0.1 mM for 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215448Drug metabolism in human liver microsomes assessed as glucuronidation per mg of protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1682832Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Structure-activity relationship of novel acridone derivatives as antiproliferative agents.
AID1215418Activity of human recombinant UGT1A10 V92A mutant expressed in baculovirus-infected Sf9 cells assessed as enzyme-mediated glucuronidation per mg of protein after 60 mins by Michaelis-Menten equation in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1215409Drug metabolism in human liver microsomes assessed as metabolite formation treated with C-1311 for 60 mins by ESI-MS/UV-vis spectroscopy in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID136246In vivo % T/C activity was measured against P388 leukemia; 1751992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias.
AID1215424Activity of human recombinant UGT1A3 expressed in baculovirus-infected Sf9 cells assessed as glucuronidation activity per mg of protein at 100 to 200 uM after 60 mins in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
AID1096393Antitumor activity against Mus musculus (mouse) P388 cells xenografted in Mus musculus (mouse) assessed as increase in survival time relative to control2011Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, Nov, Volume: 20, Issue:8
Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies.
AID621612Inhibition of human recombinant NQO2 assessed as reduction of DCPIP by spectrophotometry2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2): crystal structures, biochemical activity, and intracellular effects of imidazoacridin-6-ones.
AID1215420Drug metabolism assessed as human recombinant UGT1A10-mediated compound formation treated with C-1311 for 60 mins by ESI-MS/UV-vis spectroscopy in presence of 3 mM UDP-GlcUA2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (17.65)18.2507
2000's17 (33.33)29.6817
2010's22 (43.14)24.3611
2020's3 (5.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.87

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

MetricThis Compound (vs All)
Research Demand Index29.87 (24.57)
Research Supply Index3.99 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index35.06 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.92%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other51 (98.08%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ametantrone
ametantrone: RN given refers to parent cpd; structure		1.9810
bisbenzimidazole
Bisbenzimidazole: A benzimidazole antifilarial agent; it is fluorescent when it binds to certain nucleotides in DNA, thus providing a tool for the study of DNA replication; it also interferes with mitosis.		2.0710bibenzimidazole;
N-methylpiperazine		anthelminthic drug;
fluorochrome
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		2.0310nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		2.520dihydroxyanthraquinoneanalgesic;
antineoplastic agent
mitomycin
Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.		2.0310mitomycinalkylating agent;
antineoplastic agent
cytarabine
[no description available]		2.1110beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside		antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.0310pyrrole;
secondary amine
acridines
Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.		3.6890acridines;
mancude organic heterotricyclic parent;
polycyclic heteroarene		genotoxin
deoxycytidine
[no description available]		2.0310pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.7530delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.7330taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
etoposide
[no description available]		2.3110beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
irinotecan
[no description available]		2.7530carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug
capecitabine
Capecitabine: A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER.. capecitabine : A carbamate ester that is cytidine in which the hydrogen at position 5 is replaced by fluorine and in which the amino group attached to position 4 is converted into its N-(penyloxy)carbonyl derivative. Capecitabine is a antineoplastic agent used in the treatment of cancers.		2.0310carbamate ester;
cytidines;
organofluorine compound		antimetabolite;
antineoplastic agent;
prodrug
acridine orange
Acridine Orange: A cationic cytochemical stain specific for cell nuclei, especially DNA. It is used as a supravital stain and in fluorescence cytochemistry. It may cause mutations in microorganisms.. acridine orange : Fluorescent dye useful for cell cycle determination. It is cell-permeable, and interacts with DNA and RNA by intercalation or electrostatic attractions respectively.. acridine orange free base : A member of the class of aminoacridines that is acridine carrying two dimethylamino substituents at positions 3 and 6. The hydrochloride salt is the fluorescent dye 'acridine orange', used for cell cycle determination.		2.0810aminoacridines;
aromatic amine;
tertiary amino compound		fluorochrome;
histological dye
lissamine rhodamine b
lissamine rhodamine B: RN given refers to parent cpd; Lissamine Rhodamine B refers to Na salt		2.0310
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		3.47701,2,3-triazole
tryptoquivaline
tryptoquivaline: tremor-producing metabolite from Aspergillus clavatus; tetrapeptide derived from tryptophan, anthranilic acid, valine, & methylalanine; structure & N1 names previously assigned to tryptoquivaline C & tryptoquivaline D found to be incorrect & are revised in third source; see also record for tryptoquivalone; structure in third source		2.0310
c 1303
C 1303: DNa-binding drug; structure given indicates that the cpd should be the dimethylamino cpd, but it is named as the diethylamino cpd		2.0610
c 1310
C 1310: an imidazoacridinone; arrests cell-cycle progression in the G2 phase of L1210 cells; structure given in first source		3.2660
sjg 136
1,1'-((propane-1,3-diyl)dioxy)bis(7-methoxy-2-methylidene-1,2,3,10,11,11a-hexahydro-5H-pyrrolo(2,1-c)(1,4)benzodiazepin-5,11-dione): structure in first source		2.0310
resveratrol
trans-resveratrol : A resveratrol in which the double bond has E configuration.		2.0510resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger
mocetinostat
mocetinostat: undergoing phase II clinical trials for treatment of cancer. mocetinostat : A benzamide obtained by formal condensation of the carboxy group of 4-({[4-(pyridin-3-yl)pyrimidin-2-yl]amino}methyl)benzoic acid with one of the amino groups of benzene-1,2-diamine. It is an orally active and isotype-selective HDAC inhibitor which exhibits antitumour activity (IC50 = 0.15, 0.29, 1.66 and 0.59 muM for HDAC1, HDAC2, HDAC3 and HDAC11).		2.0110aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline		antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent
acid phosphatase
Acid Phosphatase: An enzyme that catalyzes the conversion of an orthophosphoric monoester and water to an alcohol and orthophosphate. EC 3.1.3.2.		210
octaarginine
octaarginine: structure in first source		2.3110
ConditionIndicatedRelationship StrengthStudiesTrials
Leukemia L 1210
[description not available]		02.6830
Leukemia P388
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.		01.9810
Experimental Leukemia
[description not available]		01.9810
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		02.5420
Cancer of Lung
[description not available]		02.0810
Lung Neoplasms
Tumors or cancer of the LUNG.		02.0810
Acute Myelogenous Leukemia
[description not available]		02.1110
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.1110
Benign Neoplasms
[description not available]		03.8321
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.8321
Neutropenia
A decrease in the number of NEUTROPHILS found in the blood.		03.4411
Bladder Cancer
[description not available]		02.0610
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		02.0610
Cancer of Colon
[description not available]		03.1150
Malignant Melanoma
[description not available]		02.0610
Angiogenesis, Pathologic
[description not available]		02.0610
Colonic Neoplasms
Tumors or cancer of the COLON.		03.1150
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		02.0610
Cancer of Cervix
[description not available]		02.0810
Uterine Cervical Neoplasms
Tumors or cancer of the UTERINE CERVIX.		02.0810
Hepatocellular Carcinoma
[description not available]		02.0810
Cancer of Liver
[description not available]		02.0810
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		02.0810
Liver Neoplasms
Tumors or cancer of the LIVER.		02.0810
Extravascular Hemolysis
[description not available]		02.4120
Hemolysis
The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.		02.4120
Carcinoma, Non-Small Cell Lung
[description not available]		02.0310
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		02.0310
Leucocythaemia
[description not available]		02.0310
Leukemia
A progressive, malignant disease of the blood-forming organs, characterized by distorted proliferation and development of leukocytes and their precursors in the blood and bone marrow. Leukemias were originally termed acute or chronic based on life expectancy but now are classified according to cellular maturity. Acute leukemias consist of predominately immature cells; chronic leukemias are composed of more mature cells. (From The Merck Manual, 2006)		02.0310
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		01.9910
Adenocarcinoma, Basal Cell
[description not available]		01.9910
Experimental Neoplasms
[description not available]		02.3920
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		01.9910
Bone Cancer
[description not available]		0210
Cancer of Ovary
[description not available]		0210
Osteogenic Sarcoma
[description not available]		0210
Bone Neoplasms
Tumors or cancer located in bone tissue or specific BONES.		0210
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		0210
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		0210