Compounds > nsc 706744
Page last updated: 2024-11-08

nsc 706744

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Cross-References

ID SourceID
PubMed CID397888
CHEMBL ID126159
SCHEMBL ID4162998
MeSH IDM0459014

Synonyms (31)

Synonym
nsc-706744
NCI60_037977 ,
nsc-706743
6-[3-(2-hydroxyethyl)aminopropyl]-5,11-diketo-2,3-dimethoxy-8,9-(methylenedioxy)- 11h-indeno[1,2-c]isoquinoline
5h-[1,6]indeno[1,2-c]isoquinoline- 5,12(6h)-dione,6-[3-[(2-hydroxyethyl)amino]propyl]-2,3-dimethoxy-
nsc706743
308246-52-8
lmp744
topoisomerase-1 inhibitor lmp744
mj-iii-65
CHEMBL126159 ,
lmp-744
SCHEMBL4162998
bdbm50237809
DTXSID30327954
29by7hqv0t ,
5h-(1,3)dioxolo(5,6)indeno(1,2-c)isoquinoline-5,12(6h)-dione, 6-(3-((2-hydroxyethyl)amino)propyl)-2,3-dimethoxy-
unii-29by7hqv0t
863126-39-0
CS-7432
HY-U00248
Q27894415
EX-A3021
BCP34017
6-(3-((2-hydroxyethyl)amino)propyl)-2,3-dimethoxy-5h-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6h)-dione
308246-52-8 (free base)
lmp744 free base
20-[3-(2-hydroxyethylamino)propyl]-15,16-dimethoxy-5,7-dioxa-20-azapentacyclo[10.8.0.02,10.04,8.013,18]icosa-1(12),2,4(8),9,13,15,17-heptaene-11,19-dione
MS-28221
AC-35733
AKOS040733616
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency5.86820.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency5.86820.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Tyrosyl-DNA phosphodiesterase 2Homo sapiens (human)IC50 (µMol)1.00000.97002.21604.1000AID1443969
Tyrosyl-DNA phosphodiesterase 1Homo sapiens (human)IC50 (µMol)12.00000.01203.32138.4300AID1443968
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (35)

Processvia Protein(s)Taxonomy
double-strand break repairTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
cell surface receptor signaling pathwayTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
neuron developmentTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
single strand break repairTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
DNA repairTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
double-strand break repairTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
magnesium ion bindingTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
single-stranded DNA bindingTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
transcription corepressor activityTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
nuclease activityTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
protein bindingTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
manganese ion bindingTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
tyrosyl-RNA phosphodiesterase activityTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
5'-tyrosyl-DNA phosphodiesterase activityTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
double-stranded DNA bindingTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
single-stranded DNA bindingTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
exonuclease activityTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
protein bindingTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
3'-tyrosyl-DNA phosphodiesterase activityTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
nucleusTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
nucleoplasmTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
nucleolusTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
cytoplasmTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
aggresomeTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
nuclear bodyTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
PML bodyTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
PML bodyTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
cytoplasmTyrosyl-DNA phosphodiesterase 2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
nucleoplasmTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
cytoplasmTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
plasma membraneTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
intracellular membrane-bounded organelleTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
nucleusTyrosyl-DNA phosphodiesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (80)

Assay IDTitleYearJournalArticle
AID1457589Induction of DNA damage in human PBMC assessed as gamma-H2AX foci formation at 0.1 to 1 uM after 2 hrs by confocal microscopy2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.
AID80518Antiproliferative activity was determined for 50% growth inhibition against human colon HCT116 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID497150Cytotoxicity against human MCF7 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID366202Antiproliferative activity against human SF539 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID1457588Induction of DNA damage in human CCRF-CEM cells assessed as gamma-H2AX foci formation at 0.1 to 1 uM after 2 hrs by confocal microscopy2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Design and Synthesis of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer Agents That Inhibit Topoisomerase I.
AID453802Cytotoxicity against human OVCAR-3 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID615990Antiproliferative activity against human HOP62 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID1279120Cytotoxicity against human DU145 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID771323Inhibition of recombinant DNA topoisomerase 1 (unknown origin) assessed as inhibition of topoisomerase 1-mediated DNA cleavage at 1 uM after 20 mins by SDS-PAGE analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.
AID497144Cytotoxicity against human OVCAR-3 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID1443971Cytotoxicity against human SF539 cells after 48 hrs by SRB assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID214742Antiproliferative activity was determined for 50% growth inhibition against human melanoma UACC-62 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID366208Inhibition of human recombinant topoisomerase 1 assessed as DNA cleavage relative to 1 uM camptothecin2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID615991Antiproliferative activity against human HCT116 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID1443968Inhibition of recombinant Tdp1 (unknown origin) assessed as decrease in hydrolysis of phosphodiester linkage between tyrosine residue and the 3' end of 5'-[32P]-DNA after 15 mins by PAGE analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID1279113Activity at recombinant Top1 (unknown origin) using 3'-[32P]-labeled double-stranded DNA (117 bp) as substrate assessed as suppression of DNA cleavage at 0.1 to 100 uM incubated for 20 mins by electrophoretic assay relative to 1 uM camptothecin2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID1279121Cytotoxicity against human MCF7 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID615994Antiproliferative activity against human OVCAR3 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID1279118Cytotoxicity against human OVCAR3 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID615992Antiproliferative activity against human SF539 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID1443972Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID366206Antiproliferative activity against human DU145 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID1143111Growth inhibition of human SN12C cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID56865Inhibitory activity of compound against human recombinant DNA topoisomerase I mediated DNA cleavage; Greater activity2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID497146Cytotoxicity against human SN12C cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID1279114Cytotoxicity against human HOP62 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID1143110Growth inhibition of human DU145 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID453800Cytotoxicity against human SF539 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID1443973Cytotoxicity against human OVCAR3 cells after 48 hrs by SRB assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID200451Antiproliferative activity was determined for 50% growth inhibition against human renal SN12C cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID366207Antiproliferative activity against human MDA-MB-435 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID1443969Inhibition of recombinant human Tdp2 assessed as decrease in alpha 32P-cordycepin-3'-labeled DNA breaks after 15 mins by PAGE analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID1363340Inhibition of recombinant TOP1 (unknown origin)-mediated 3'-[32P]-labeled 117-bp DNA oligonucleotide cleavage assessed as induction of protein-DNA covalent cleavage complex formation at 1 uM after 20 mins by PAGE analysis relative to camptothecin2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Discovery, Synthesis, and Evaluation of Oxynitidine Derivatives as Dual Inhibitors of DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1), and Potential Antitumor Agents.
AID366200Antiproliferative activity against human HOP62 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID145413Antiproliferative activity was determined for 50% growth inhibition against human ovarian OVCAR-3 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID1143114Growth inhibition of human SF539 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID453799Cytotoxicity against human HCT116 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID453803Cytotoxicity against human SN12C cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID497152Inhibition of human recombinant Top1-mediated DNA cleavage at 1 uM after 20 mins relative to camptothecin2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID615989Inhibition of recombinant human TOP1 mediated DNA cleavage after 20 mins by gel electrophoresis relative to camptothecin2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID1279119Cytotoxicity against human SN12C cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID57720Antiproliferative activity was determined for 50% growth inhibition against human Prostate DU-145 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID497138Cytotoxicity against human HCT116 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID366201Antiproliferative activity against human HCT116 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID1143117Growth inhibition of human MCF7 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID497140Cytotoxicity against human SF539 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID45948Antiproliferative activity was determined for 50% growth inhibition against human CNS SF-539 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID1279117Cytotoxicity against human UACC62 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID1566778Inhibition of recombinant TOP1 (unknown origin) using 3'-[32P]-labeled 117 bp DNA oligonucleotide assessed as TOP1-mediated DNA cleavage by measuring induction and stabilization of cleavage sites 17, 35 and 79 at 1 uM incubated for 20 mins by PAGE analysi2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and biological evaluation of 5-aminoethyl benzophenanthridone derivatives as DNA topoisomerase IB inhibitors.
AID453806Inhibition of human DNA topoisomerase 1 assessed as induction of enzyme-dependent DNA cleavage relative to 1 uM camptothecin2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID615993Antiproliferative activity against human UACC62 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID102143Antiproliferative activity was determined for 50% growth inhibition against human breast MDA-MB-435 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID1279116Cytotoxicity against human SF539 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID615996Antiproliferative activity against human DU145 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID1443974Cytotoxicity against human SN12C cells after 48 hrs by SRB assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID1284067Poisoning activity at topoisomerase 1 (unknown origin) using 3'-[32P]dGTP labelled 117bp oligonucleotide assessed as induction of DNA cleavage at 1 uM incubated for 20 mins by SDS-PAGE analysis2016European journal of medicinal chemistry, Apr-13, Volume: 112Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties.
AID366203Antiproliferative activity against human UACC62 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID1279115Cytotoxicity against human HCT116 cells by MTT assay2016Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.
AID453801Cytotoxicity against human UACC62 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID1143112Growth inhibition of human UACC62 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID1143115Growth inhibition of human HCT116 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID453805Cytotoxicity against human MDA-MB-435 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID615995Antiproliferative activity against human SN12C cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID453804Cytotoxicity against human DU145 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID497136Cytotoxicity against human HOP62 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID497148Cytotoxicity against human DU145 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID615997Antiproliferative activity against human MCF7 cells by SRB assay2011Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
AID222121Mean graph midpoint for growth inhibition of all human cancer cell lines2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID453798Cytotoxicity against human HOP62 cells2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
AID1443978Inhibition of recombinant Top1 (unknown origin) assessed as increase in [32P]-DNA breaks at 1 uM after 20 mins by PAGE analysis2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID1443975Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID1443970Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay2017Journal of medicinal chemistry, 04-27, Volume: 60, Issue:8
Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2).
AID366204Antiproliferative activity against human OVCAR-3 cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID1143116Growth inhibition of human HOP62 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID366205Antiproliferative activity against human SN12C cells2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
AID497142Cytotoxicity against human UACC62 cells2010Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
AID81499Antiproliferative activity was determined for 50% growth inhibition against human lung HOP-62 cell line2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
AID1143113Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Design, synthesis, and biological evaluation of O-2-modified indenoisoquinolines as dual topoisomerase I-tyrosyl-DNA phosphodiesterase I inhibitors.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (21.43)29.6817
2010's10 (71.43)24.3611
2020's1 (7.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
ethidium bromide
[no description available]		2.1710organic bromide saltgeroprotector;
intercalator;
trypanocidal drug
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		3.95120delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
etoposide
[no description available]		2.1310beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
oxynitidine
oxynitidine: structure in frist source		2.5920
nsc 314622
NSC 314622: structure in first source		3.1450
22-hydroxyacuminatine
22-hydroxyacuminatine: cytotoxic; isolated from Camptotheca acuminata; structure in first source		2.0410
n'-(10h-indolo(3,2-b)quinolin-11-yl)-n,n-dimethylpropane-1,3-diamine
[no description available]		2.1710
nsc 725776
NSC 725776: inhibits topoisomerase I; structure in first source		2.4620
nsc 724998
[no description available]		2.4620
rosettacin
rosettacin: structure in first source		2.7430
ConditionIndicatedRelationship StrengthStudiesTrials
Leucocythaemia
[description not available]		02.1310
Benign Neoplasms
[description not available]		02.1310
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)		02.1310
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.		02.1310
Breast Cancer
[description not available]		02.2110
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.2110