Page last updated: 2024-12-04

ametantrone

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Description

ametantrone: RN given refers to parent cpd; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2134
CHEMBL ID49442
SCHEMBL ID3344151
MeSH IDM0073683

Synonyms (43)

Synonym
1,4-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-9,10-anthracenedione
brn 2791800
1,4-bis((2-((2-hydroxyethyl)amino)ethyl)amino)anthraquinone
1,4-bis(2-((2-hydroxyethyl)amino)ethylamino)-9,10-anthracenedione
nsc 196473
anthraquinone, 1,4-bis((2-((2-hydroxyethyl)amino)ethyl)amino)-
ametantrona [inn-spanish]
9,10-anthracenedione, 1,4-bis((2-(2-(hydroxyethyl)amino)ethyl)amino)-
ametantrone diacetate
ametantrone [inn]
ametantronum [inn-latin]
anthracenedione deriv.
nsc-196473
9, 1,4-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-
nsc196473
64862-96-0
ametantrone
CHEMBL49442
1,4-bis[2-(2-hydroxyethylamino)ethylamino]anthracene-9,10-dione
1,4-bis({2-[(2-hydroxyethyl)amino]ethyl}amino)anthracene-9,10-dione
AKE ,
ametantronum
ametantrona
pnt6041st1 ,
unii-pnt6041st1
SCHEMBL3344151
AC-35214
DTXSID60215153
AKOS028108437
9,10-anthracenedione, 1,4-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-
nsc 196473;ametantrone
EX-A368
1,4-bis({2-[(2-hydroxyethyl)amino]ethyl}amino)-9,10-dihydroanthracene-9,10-dione
I11677
1,4-bis((2-((2-hydroxyethyl)amino)ethyl)amino)anthracene-9,10-dione
AS-49556
BCP09323
ci881
nsc 196473; nsc 290813
Q27286653
bdbm50520631
CS-0007147
HY-13550

Research Excerpts

Overview

Amitantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylaminos at positions 1 and 4. It shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding.

ExcerptReferenceRelevance
"Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding."( Rational design, synthesis, and DNA binding properties of novel sequence-selective peptidyl congeners of ametantrone.
Basili, S; Gatto, B; Gianoncelli, A; Gresh, N; Moro, S; Palumbo, M; Scalabrin, M; Sosic, A; Zagotto, G, 2010
)
1.3
"Ametantrone acetate is an antineoplastic drug chemically described as 1,4-bis [[2-[(2-hydroxyethyl)-amino] ethyl]amino] -9,10-anthracenedione diacetate salt. "( Teratology studies of ametantrone acetate in rats and rabbits.
Anderson, JA; de la Iglesia, FA; Fitzgerald, JE; Kim, SN; Petrere, JA; Schardein, JL, 1986
)
2.03
"Ametantrone acetate is an intensely blue anthracenedione undergoing clinical trials in man. "( A phase I trial of ametantrone acetate (NSC-287513).
Bender, JF; Gams, RA; Grillo-López, AJ; Ostroy, F, 1985
)
2.04

Toxicity

ExcerptReferenceRelevance
" In mice, LD10, LD50 and LD90 values were respectively, 26, 35 and 47 mg kg-1 28 days following single intravenous injection and 22, 67 and 206 mg kg-1 14 days after single intraperitoneal injection."( Preclinical toxicity of the new antineoplastic agent, ametantrone acetate, in mice and dogs.
Anderson, JA; de la Iglesia, FA; Fitzgerald, JE; Jayasekara, U; Kim, SN; Watkins, JR, 1986
)
0.52
" 10-fold less toxic than doxorubicin and caused only minor electrocardiogram (ECG) changes."( Comparison of cardiotoxicity of two anthracenediones and doxorubicin in rats.
Beilstein, AK; Zbinden, G, 1982
)
0.26

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic parameters for ametantrone acetate (CI-881) were characterized in six patients concurrently with the phase I clinical trial."( Pharmacokinetics of ametantrone acetate (NSC-287513).
Balmer, CE; Bender, JF; Grillo-Lopez, AJ; Kuhn, JG; Loesch, DM; Ludden, TM; Von Hoff, DD, 1987
)
0.87

Dosage Studied

ExcerptRelevanceReference
" A 5-day, consecutive intraperitoneal dosing study yielded 28 day, LD10, LD50 and LD90 values of 18, 21 and 26 mg kg-1, respectively, in mice."( Preclinical toxicity of the new antineoplastic agent, ametantrone acetate, in mice and dogs.
Anderson, JA; de la Iglesia, FA; Fitzgerald, JE; Jayasekara, U; Kim, SN; Watkins, JR, 1986
)
0.52
" Dosage escalations proceeded from 15 mg/m2 to 35 mg/m2."( A phase I trial of ametantrone acetate (NSC-287513).
Bender, JF; Gams, RA; Grillo-López, AJ; Ostroy, F, 1985
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA topoisomerase 2-betaHomo sapiens (human)IC50 (µMol)0.03000.03002.77167.8000AID1584438
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (12)

Processvia Protein(s)Taxonomy
neuron migrationDNA topoisomerase 2-betaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-betaHomo sapiens (human)
axonogenesisDNA topoisomerase 2-betaHomo sapiens (human)
B cell differentiationDNA topoisomerase 2-betaHomo sapiens (human)
forebrain developmentDNA topoisomerase 2-betaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-betaHomo sapiens (human)
cellular response to hydrogen peroxideDNA topoisomerase 2-betaHomo sapiens (human)
cellular response to ATPDNA topoisomerase 2-betaHomo sapiens (human)
cellular senescenceDNA topoisomerase 2-betaHomo sapiens (human)
positive regulation of double-strand break repair via nonhomologous end joiningDNA topoisomerase 2-betaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-betaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
DNA bindingDNA topoisomerase 2-betaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-betaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-betaHomo sapiens (human)
protein bindingDNA topoisomerase 2-betaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-betaHomo sapiens (human)
ribonucleoprotein complex bindingDNA topoisomerase 2-betaHomo sapiens (human)
metal ion bindingDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
nucleolusDNA topoisomerase 2-betaHomo sapiens (human)
heterochromatinDNA topoisomerase 2-betaHomo sapiens (human)
nucleusDNA topoisomerase 2-betaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-betaHomo sapiens (human)
nucleolusDNA topoisomerase 2-betaHomo sapiens (human)
cytosolDNA topoisomerase 2-betaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-betaHomo sapiens (human)
nucleusDNA topoisomerase 2-betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (153)

Assay IDTitleYearJournalArticle
AID55805In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line DU1451999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID1130148Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse assessed as survival at 2 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID136243In vivo % T/C activity was measured against P388 leukemia1992Journal of medicinal chemistry, Jan-24, Volume: 35, Issue:2
Chromophore-modified antineoplastic imidazoacridinones. Synthesis and activity against murine leukemias.
AID1132475Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as mouse survival at 16 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID150941Ratio of medium survival time expressed as percent of untreated controls(dose 6.25 mg/kg)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID102168In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line LoVo1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID144379The capacity to stimulate NADH oxidation was determined.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones.
AID1130202Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse assessed as survival at 8 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130150Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse assessed as survival at 1 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130190Antineoplastic activity against mouse Colon 26 cells allografted in CDF1 mouse assessed as survival at 8 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID87734In vitro cytotoxicity against HeLa S3 cell lines1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity.
AID320433Cytotoxicity against human MCF7 cells at 4 ug/ml after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID1130201Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse at 16 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130195Antineoplastic activity against mouse Colon 26 cells allografted in CDF1 mouse at 2 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID54651dichroism data for visible band in the compound to DNA in ETN.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
Chromophore-modified antitumor anthracenediones: synthesis, DNA binding, and cytotoxic activity of 1,4-bis[(aminoalkyl)amino]benzo[g]-phthalazine-5,10-diones.
AID1130168Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse assessed as survival at 2 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID137871At 50 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate mean survival time1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID1130166Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse assessed as survival at 4 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID139189At 50 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate Number of toxic deaths/total number of mice; 0/61991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID1130197Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse at 16 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1132522Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as increase in survival time at 16 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID1130199Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse at 8 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130151Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse at 1 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID7502In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line A2780/Dx(RI)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID1132477Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as mouse survival at 4 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID154574Percent ratio of the medium survival time for P388 murine leukemia in CDF1 mice at 25 mg/kg1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID100682T/C in % was determined against L1210 murine leukemia cells at a dose of 12.5 x3 mg/kg1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Heterosubstituted anthracene-9,10-dione analogues. The synthesis and antitumor evaluation of 5,8-bis[(aminoalkyl)amino]naphtho[2,3-b] thiophene-4,9-diones.
AID1130169Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse at 2 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID320441Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID152743In vivo inhibitory activity against P388 murine leukemia cells and the ratio of medium survival time expressed as percent of untreated controls (%T/C) at dose of 6.25 mg/kg (6/6*)1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones.
AID154571Percent ratio of the medium survival time for P388 murine leukemia in CDF1 mice at 12.5 mg/kg1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID134929At 25 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate Long-term survivors at the end of the experiment; 0/61991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID409951Inhibition of human liver MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1130188Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse assessed as survival at 4 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130611Antitumor activity against mouse B16 cells allografted in BDF1 mouse assessed as increase of median life span at 6.2 mg/kg, ip on day 1 to 9 measured up to 80 days relative to control1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Antitumor agents. 1. 1,4-Bis[(aminoalkyl)amino]-9,10-anthracenediones.
AID320440Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID152604In vivo inhibitory activity against P388 murine leukemia cells and the ratio of medium survival time expressed as percent of untreated controls (%T/C) at dose of 12.5 mg/kg (6/6*)1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones.
AID1130186Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse assessed as survival at 8 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID320436Cytotoxicity against human PC3 cells after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID154580Percent ratio of the medium survival time for P388 murine leukemia in CDF1 mice at 6.25 mg/kg1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID1130149Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse at 2 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID100495Effective concentration against inhibition of L1210 mouse leukemia cells in tissue culture1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones.
AID1132514Antitumor activity against mouse L1210 cells allografted in BDF1 mouse assessed as increase in survival time at 12.5 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID1132521Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as increase in survival time at 32 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID222141Inhibition of cellular growth was evaluated in vitro against human colon carcinoma subline resistant to DOXO (LOVO/DOXO).1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID135056At 50 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate Long-term survivors at the end of the experiment; 0/61991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID102330Inhibitory activity against human colon adenocarcinoma cell line LoVo/Dx.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
Chromophore-modified antitumor anthracenediones: synthesis, DNA binding, and cytotoxic activity of 1,4-bis[(aminoalkyl)amino]benzo[g]-phthalazine-5,10-diones.
AID1132523Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as increase in survival time at 8 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID144491Activity of NADH dehydrogenase was determined1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID1132494Toxicity in mouse P388 cells allografted BDF1 mouse assessed as body weight difference at 16 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID137865At 12.5 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate mean survival time1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID88359Effective concentration against cell growth of HeLa cell line by 50%1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Peptidyl anthraquinones as potential antineoplastic drugs: synthesis, DNA binding, redox cycling, and biological activity.
AID232016Resistance index is the ratio of IC50 of resistant cell line/IC50 of sensitive cell line1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations.
AID100803T/C in % was determined against L1210 murine leukemia cells at a dose of 25 x3 mg/kg; 60 - day survivors =1/61990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Heterosubstituted anthracene-9,10-dione analogues. The synthesis and antitumor evaluation of 5,8-bis[(aminoalkyl)amino]naphtho[2,3-b] thiophene-4,9-diones.
AID1132513Antitumor activity against mouse L1210 cells allografted in BDF1 mouse assessed as increase in survival time at 25 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID1130187Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse at 8 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID45640Survivors of CDF1 mice on day 4 after 1st injection of compound 25 at mg/kg in six mice; 6/61989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID150937Ratio of medium survival time expressed as percent of untreated controls(dose 3.12 mg/kg)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID139184At 25 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate Number of toxic deaths/total number of mice; 0/61991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID97829Concentration of compound required to inhibit the cellular protein biosynthesis by 50%1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID1130167Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse at 4 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1132474Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as mouse survival at 32 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID1130172Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse assessed as survival at 2 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130184Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse assessed as survival at 16 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID100808T/C in % was determined against L1210 murine leukemia cells at a dose of 50 x3 mg/kg; 60 - day survivors =1/61990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Heterosubstituted anthracene-9,10-dione analogues. The synthesis and antitumor evaluation of 5,8-bis[(aminoalkyl)amino]naphtho[2,3-b] thiophene-4,9-diones.
AID1130193Antineoplastic activity against mouse Colon 26 cells allografted in CDF1 mouse at 4 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130205Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse at 4 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130204Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse assessed as survival at 4 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID144382Concentration of substrate at which the amount of total cytochrome c reduction is decreased by 10%1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID1130198Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse assessed as survival at 8 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1130192Antineoplastic activity against mouse Colon 26 cells allografted in CDF1 mouse assessed as survival at 4 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID152612In vivo inhibitory activity against P388 murine leukemia cells and the ratio of medium survival time expressed as percent of untreated controls (%T/C) at dose of 3.12 mg/kg (6/6*)1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones.
AID96950The compound was tested for its antitumor activity against L1210 cells1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID1130603Antitumor activity against mouse P388 cells allografted in mouse assessed as disease cure at 25 mg/kg, ip on day 1, 5 and 9 measured up to 60 days1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Antitumor agents. 1. 1,4-Bis[(aminoalkyl)amino]-9,10-anthracenediones.
AID1130196Antineoplastic activity against mouse L1210 cells allografted in CDF1 mouse assessed as survival at 16 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID102332Resistance index as the ratio of IC50 value against LoVo/Dx to that of LoVo cell lines.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
Chromophore-modified antitumor anthracenediones: synthesis, DNA binding, and cytotoxic activity of 1,4-bis[(aminoalkyl)amino]benzo[g]-phthalazine-5,10-diones.
AID1132496Toxicity in mouse P388 cells allografted BDF1 mouse assessed as body weight difference at 4 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID234842NADH oxidation by the compound was determined1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID153631In vivo antileukemic activity against P388 leukemia at dose 12.5 mp/kg administered intraperitoneally (30 days survivors, 3/6)1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity.
AID232801Ratio of toxic deaths/survivors 7 days after the day 5 injection as a measure of drug toxicity at the dose of 6.25 (mg/kg)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID81308Compound was tested in vitro for cytotoxicity against HL60 human leukemia cell line (72 hr exposure to compound)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID320442Cytotoxicity against human SF268 cells after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID154576Percent ratio of the medium survival time for P388 murine leukemia in CDF1 mice at 3.12 mg/kg1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID1335230Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Quinolino[3,4-b]quinoxalines and pyridazino[4,3-c]quinoline derivatives: Synthesis, inhibition of topoisomerase IIα, G-quadruplex binding and cytotoxic properties.
AID150810Survivor recorded on day 4 after day of first injection as a measure of drug toxicity(dose 3.12 mg/kg); 6/61988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID409949Inhibition of human liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1130173Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse at 2 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID134927At 12.5 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate Long-term survivors at the end of the experiment; 0/61991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID54648Ki value was measured for the binding of compound to DNA in ETN.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
Chromophore-modified antitumor anthracenediones: synthesis, DNA binding, and cytotoxic activity of 1,4-bis[(aminoalkyl)amino]benzo[g]-phthalazine-5,10-diones.
AID137868At 25 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate mean survival time1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID1449718Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Indenocinnoline derivatives as G-quadruplex binders, topoisomerase IIα inhibitors and antiproliferative agents.
AID98039Effective concentration against cell growth of L1210 cell line by 50%1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Peptidyl anthraquinones as potential antineoplastic drugs: synthesis, DNA binding, redox cycling, and biological activity.
AID1132524Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as increase in survival time at 4 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID230412It is the ratio of IC50 for LOVO tumor cell line to that of LOVO/DOXO cell line.1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID99088Tested in vitro for inhibitory activity against L1210 murine leukemia1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations.
AID102211In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line LoVo/DX(RI)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID150935Ratio of medium survival time expressed as percent of untreated controls(dose 12.5 mg/kg)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID320439Ratio of GI50 for human HL60/MX2 cells to GI50 for human HL60 cells2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID152610In vivo inhibitory activity against P388 murine leukemia cells and the ratio of medium survival time expressed as percent of untreated controls (%T/C) at dose of 25 mg/kg (6/6*)1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Synthesis, peroxidating ability, and antineoplastic evaluation of 1-[(aminoalkyl)amino]-4-hydroxy-10-imino-9-anthracenones.
AID222140Inhibition of cellular growth was evaluated in vitro against human colon carcinoma LOVO.1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID1130194Antineoplastic activity against mouse Colon 26 cells allografted in CDF1 mouse assessed as survival at 2 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID150962ratio of medium survival time of the treated to the control mice at the dose of 6.25 (mg/kg)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID1130191Antineoplastic activity against mouse Colon 26 cells allografted in CDF1 mouse at 8 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID1132493Toxicity in mouse P388 cells allografted BDF1 mouse assessed as body weight difference at 32 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID1130203Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse at 8 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID150813Survivor recorded on day 4 after day of first injection as a measure of drug toxicity(dose 6.25 mg/kg); 6/61988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID1130189Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse at 4 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID320438Cytotoxicity against DNA topoisomerase-2 deficient human HL60/MX2 cells by MTT assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID320434Cytotoxicity against human NCI-H460 cells at 4 ug/ml after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID135709Tested for antitumor activity against P388 murine leukemia1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations.
AID1132515Antitumor activity against mouse L1210 cells allografted in BDF1 mouse assessed as increase in survival time at 6.25 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID97831Effective concentration required to inhibit by 50% the growth of L1210 cells1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID97977Concentration required to inhibit the growth of L1210 leukemia cells1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID232799Ratio of toxic deaths/survivors 7 days after the day 5 injection as a measure of drug toxicity at the dose of 3.12 (mg/kg)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
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.
AID150958ratio of medium survival time of the treated to the control mice at the dose of 12.50 (mg/kg)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID1132476Antitumor activity against mouse P388 cells allografted in BDF1 mouse assessed as mouse survival at 8 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID150806Survivor recorded on day 4 after day of first injection as a measure of drug toxicity(dose 12.5 mg/kg); 6/61988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID95161Compound was tested in vitro for cytotoxicity against MDR cell line K562R (RI) (72 hr exposure to compound)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID150960ratio of medium survival time of the treated to the control mice at the dose of 3.12 (mg/kg)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID87741Effective concentration required to inhibit by 50% the growth of HeLa S3 cells1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID54649Intrinsic Binding constant of compound to DNA at pH 7 and 25 Centigrade1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Peptidyl anthraquinones as potential antineoplastic drugs: synthesis, DNA binding, redox cycling, and biological activity.
AID1584438Poison activity at recombinant human topoisomerase 2beta using pBR322 plasmid as substrate after 30 mins by ethidium bromide staining based agarose gel electrophoresis2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches.
AID45658Survivors of CDF1 mice on day 4 after 1st injection of compound at 6.25 mg/kg in six mice; 6/61989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID82830Effective concentration against cell growth of HL60 cell line by 50%1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Peptidyl anthraquinones as potential antineoplastic drugs: synthesis, DNA binding, redox cycling, and biological activity.
AID150808Survivor recorded on day 4 after day of first injection as a measure of drug toxicity(dose 25 mg/kg); 6/61988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID10019In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line A27801999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID1130200Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse assessed as survival at 16 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID156652In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line PC31999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID1130602Antitumor activity against mouse P388 cells allografted in mouse assessed as increase of median life span at 25 mg/kg, ip on day 1, 5 and 9 measured up to 60 days relative to control1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Antitumor agents. 1. 1,4-Bis[(aminoalkyl)amino]-9,10-anthracenediones.
AID102188Tested in vitro for cytotoxic activity against Human colon Adenocarcinoma sensitive cell line (LoVo)1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations.
AID320430Binding affinity to calf thymus DNA assessed as thermal denaturation temperature at 20 uM2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID320435Cytotoxicity against human SF268 cells at 4 ug/ml after 48 hrs by SRB assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID1130175Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse at 1 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID235789Ratio of toxic deaths/survivors 7 days after the day 5 injection as a measure of drug toxicity at the dose of 12.50 (mg/kg)1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
AID150936Ratio of medium survival time expressed as percent of untreated controls(dose 25 mg/kg)1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.
AID1130174Antineoplastic activity against mouse P388 cells allografted in CDF1 mouse assessed as survival at 1 mg/kg qd for 9 days1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID45648Survivors of CDF1 mice on day 4 after 1st injection of compound at 12.5 mg/kg in six mice; 6/61989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID1130185Antineoplastic activity against mouse B16 cells allografted in BDF1 mouse at 16 mg/kg qd for 9 days relative to control1979Journal of medicinal chemistry, May, Volume: 22, Issue:5
Structural modification study of bis(substituted aminoalkylamino)anthraquinones. An evaluation of the relationship of the [2-[(2-hydroxyethyl)amino]ethyl]amino side chain with antineoplastic activity.
AID134227The compound was tested for antitumor activity against P388 murine leukemia by measuring maximum tolerated dose1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations.
AID139182At 12.5 mg/kg dose CDF1 mice were injected ip on (1,5,9) days after tumor transplantation to evaluate Number of toxic deaths/total number of mice; 0/61991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Synthesis and antitumor evaluations of symmetrically and unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and 1,4-bis[(aminoalkyl)amino]-5,8-dihydroxyanthracene-9,10-diones.
AID1335229Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Quinolino[3,4-b]quinoxalines and pyridazino[4,3-c]quinoline derivatives: Synthesis, inhibition of topoisomerase IIα, G-quadruplex binding and cytotoxic properties.
AID95160Compound was tested in vitro for cytotoxicity against MDR cell line K562R (72 hr exposure to compound)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID102331Tested in vitro for cytotoxic activity against Doxorubicin resistant Human colon Adenocarcinoma sensitive cell line1994Journal of medicinal chemistry, Mar-18, Volume: 37, Issue:6
6,9-Bis[(aminoalkyl)amino]benzo[g]isoquinoline-5,10-diones. A novel class of chromophore-modified antitumor anthracene-9,10-diones: synthesis and antitumor evaluations.
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.
AID1132495Toxicity in mouse P388 cells allografted BDF1 mouse assessed as body weight difference at 8 mg/kg administered 24 hrs post challenge relative to control1978Journal of medicinal chemistry, Mar, Volume: 21, Issue:3
Antineoplastic agents. Structure-activity relationship study of bis(substituted aminoalkylamino)anthraquinones.
AID98537Compound was tested in vitro for cytotoxicity against L1210 murine cell line (48 hr exposure to compound)1999Journal of medicinal chemistry, Sep-09, Volume: 42, Issue:18
8,11-dihydroxy-6-[(aminoalkyl)amino]-7H-benzo[e]perimidin-7-ones with activity in multidrug-resistant cell lines: synthesis and antitumor evaluation.
AID26757DNA binding dissociation constant as KD; No data1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics.
AID320437Cytotoxicity against human HL60 cells after 48 hrs by MTT assay2008Bioorganic & medicinal chemistry, Jan-15, Volume: 16, Issue:2
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
AID45653Survivors of CDF1 mice on day 4 after 1st injection of compound at 3.12 mg/kg in six mice; 6/61989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
AID24662Exclusion parameter (base pairs1996Journal of medicinal chemistry, Aug-02, Volume: 39, Issue:16
Peptidyl anthraquinones as potential antineoplastic drugs: synthesis, DNA binding, redox cycling, and biological activity.
AID102184Inhibitory activity against human colon adenocarcinoma cell line LoVo.1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
Chromophore-modified antitumor anthracenediones: synthesis, DNA binding, and cytotoxic activity of 1,4-bis[(aminoalkyl)amino]benzo[g]-phthalazine-5,10-diones.
AID1449717Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Indenocinnoline derivatives as G-quadruplex binders, topoisomerase IIα inhibitors and antiproliferative agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (90)

TimeframeStudies, This Drug (%)All Drugs %
pre-199046 (51.11)18.7374
1990's28 (31.11)18.2507
2000's7 (7.78)29.6817
2010's8 (8.89)24.3611
2020's1 (1.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.48

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

MetricThis Compound (vs All)
Research Demand Index17.48 (24.57)
Research Supply Index4.55 (2.92)
Research Growth Index4.40 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.08%)5.53%
Reviews4 (4.30%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other88 (94.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]