Page last updated: 2024-12-08

nsc 314622

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

Description

NSC 314622: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID329826
CHEMBL ID79513
SCHEMBL ID14147251
MeSH IDM0293091

Synonyms (22)

Synonym
smr001565399
nsc-341622
CHEMBL79513
2,3-dimethoxy-6-methyl-5h-[1,3]dioxolo[4',5':5,6]indeno[1,2-c]isoquinoline-5,12(6h)-dione
{5h-[1,3]dioxolo[5,6]indeno[1,2-c]isoquinoline-5,12-dione,} 2, 3-dimethoxy-6-methyl-
NCIMECH_000446
NCI60_002710
mls002701805 ,
66358-49-4
NSC314622 ,
nsc-314622
5h-[1,6]indeno[1,2-c]isoquinoline-5,12-dione, 2,3-dimethoxy-6-methyl-
nsc 314622
2,3-dimethoxy-6-methyl-5h-(1,3)dioxolo(4',5':5,6)indeno(1,2-c)isoquinoline-5,12(6h)-dione
unii-q1g3fj6tls
5,6-dihydro-5,11-diketo-2,3-dimethoxy-6-methyl-8,9-methylenedioxy-11h-indeno(1,2-c)isoquinoline
q1g3fj6tls ,
CCG-35623
SCHEMBL14147251
DTXSID40216582
2,3-dimethoxy-6-methyl-5h-(1,3)dioxolo(5,6)indeno(1,2-c)isoquinoline-5,12(6h)-dione
5h-(1,3)dioxolo(5,6)indeno(1,2-c)isoquinoline-5,12(6h)-dione, 2,3-dimethoxy-6-methyl-

Research Excerpts

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glp-1 receptor, partialHomo sapiens (human)Potency5.62340.01846.806014.1254AID624417
TDP1 proteinHomo sapiens (human)Potency5.39180.000811.382244.6684AID686978; AID686979
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency1.63600.00419.984825.9290AID504444
flap endonuclease 1Homo sapiens (human)Potency89.12510.133725.412989.1251AID588795
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency84.92140.425612.059128.1838AID504891
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency6.51310.004611.374133.4983AID624297
DNA polymerase kappa isoform 1Homo sapiens (human)Potency89.12510.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (11)

Processvia Protein(s)Taxonomy
DNA topological changeDNA topoisomerase 1Homo sapiens (human)
chromatin remodelingDNA topoisomerase 1Homo sapiens (human)
circadian rhythmDNA topoisomerase 1Homo sapiens (human)
response to xenobiotic stimulusDNA topoisomerase 1Homo sapiens (human)
programmed cell deathDNA topoisomerase 1Homo sapiens (human)
phosphorylationDNA topoisomerase 1Homo sapiens (human)
peptidyl-serine phosphorylationDNA topoisomerase 1Homo sapiens (human)
circadian regulation of gene expressionDNA topoisomerase 1Homo sapiens (human)
embryonic cleavageDNA topoisomerase 1Homo sapiens (human)
chromosome segregationDNA topoisomerase 1Homo sapiens (human)
DNA replicationDNA topoisomerase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingDNA topoisomerase 1Homo sapiens (human)
DNA bindingDNA topoisomerase 1Homo sapiens (human)
chromatin bindingDNA topoisomerase 1Homo sapiens (human)
double-stranded DNA bindingDNA topoisomerase 1Homo sapiens (human)
single-stranded DNA bindingDNA topoisomerase 1Homo sapiens (human)
RNA bindingDNA topoisomerase 1Homo sapiens (human)
DNA topoisomerase type I (single strand cut, ATP-independent) activityDNA topoisomerase 1Homo sapiens (human)
protein serine/threonine kinase activityDNA topoisomerase 1Homo sapiens (human)
protein bindingDNA topoisomerase 1Homo sapiens (human)
ATP bindingDNA topoisomerase 1Homo sapiens (human)
DNA binding, bendingDNA topoisomerase 1Homo sapiens (human)
protein domain specific bindingDNA topoisomerase 1Homo sapiens (human)
supercoiled DNA bindingDNA topoisomerase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
nuclear chromosomeDNA topoisomerase 1Homo sapiens (human)
P-bodyDNA topoisomerase 1Homo sapiens (human)
fibrillar centerDNA topoisomerase 1Homo sapiens (human)
male germ cell nucleusDNA topoisomerase 1Homo sapiens (human)
nucleusDNA topoisomerase 1Homo sapiens (human)
nucleoplasmDNA topoisomerase 1Homo sapiens (human)
nucleolusDNA topoisomerase 1Homo sapiens (human)
perikaryonDNA topoisomerase 1Homo sapiens (human)
protein-DNA complexDNA topoisomerase 1Homo sapiens (human)
nucleolusDNA topoisomerase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (218)

Assay IDTitleYearJournalArticle
AID658162Stabilization of human G-quadruplex F21T assessed as change in melting temperature at 1 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries.
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.
AID247266Growth inhibitory activity against human breast MDA-MB-435 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID46746Mean graph midpoint for growth inhibition of all human cancer cell lines2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID458049Antiproliferative activity against human SN12C cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID145418Cytotoxic concentration against human ovarian OVCAR-3 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID273195Cytotoxicity against human HCT116 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
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.
AID297404Cytotoxicity against human MDA-MB-435 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID57727Cytotoxicity against DU-145 human prostate cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID297652Cytotoxicity against human MDA-MB-435 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
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.
AID547387Antiproliferative activity against human DU145 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID620803Cytotoxicity against human UACC62 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
AID458050Antiproliferative activity against human DU145 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
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.
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.
AID547379Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID286258Cytotoxicity against human OVCAR-3 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID620805Cytotoxicity against human SN12C cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
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.
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.
AID547378Antiproliferative activity against human HOP62 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID219007Cytotoxicity in breast MDA-MB-435 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID1075787Cytotoxicity against human MCF7 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID80526Cytotoxic concentration against human colon HCT116 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID247243Growth inhibitory activity against human renal SN12C cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID547385Antiproliferative activity against human SN12C cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
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.
AID657920Growth inhibition of human HCT116 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID90293Mean graph midpoint for growth inhibition of all human cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID620801Cytotoxicity against human HCT116 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
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.
AID286261Cytotoxicity against human MDA-MA-435 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID657923Growth inhibition of human OVCAR3 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID458047Antiproliferative activity against human SF539 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID286256Cytotoxicity against human SF268 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID247234Growth inhibitory activity against human CNSSF-539 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID81500Cytotoxicity against lung HOP-62 human cancer cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
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.
AID547381Antiproliferative activity against human COLO205 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID243386Topoisomerase-I mediated DNA Cleavage activity at 30 degree C for 30 min relative to NSC 314622; Range = 25-75%2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
AID547377Antiproliferative activity against human K562 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID247161Growth inhibition against ProstateDU-145 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID244264Induction of topoisomerase I mediated DNA cleavage; Activity similar to parent compound 12004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
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.
AID200450Cytotoxicity against human renal SN12C cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
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.
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.
AID88924Mean graph mid point for growth inhibition of all human cancer cell lines tested.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID286260Cytotoxicity against human DU145 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID80521Cytotoxicity against colon HCT116 human cancer cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID45945Cytotoxicity in CNS SF-539 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
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.
AID273197Cytotoxicity against human UACC62 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
AID657926Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
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.
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.
AID273196Cytotoxicity against human SF539 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
AID297402Cytotoxicity against human SN12C cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID547375Antiproliferative activity against human RPMI18226 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID244798Mean graph midpoint for growth inhibition of all human cancer cell lines2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
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.
AID253090Mean graph mid point for growth inhibition of human cancer cell lines2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID247261Growth inhibitory activity against human melanoma UACC-62 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID547382Antiproliferative activity against human UACC62 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
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.
AID297403Cytotoxicity against human DU145 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID657919Growth inhibition of human HOP62 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID102150Cytotoxicity against MDA-MB-435 human breast cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID252291Concentration tested for Top1-mediated DNA cleavage (concentration taken upto 100 uM); ++: similar activity as the parent compound 3a2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID547384Antiproliferative activity against human IGROV1 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID55795Cytotoxicity against prostate DU-145 human cancer cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID214746Cytotoxic concentration against human melanoma UACC-62 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID247162Growth inhibition against Melanoma UACC-62 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID200928Cytotoxicity against SF-268 human CNS cancer cell line was determined; NT- Not tested2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
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.
AID145417Cytotoxicity against ovarian OVCAR-3 human cancer cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID1075791Cytotoxicity against human SF539 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID547383Antiproliferative activity against human OVACR3 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID657917Inhibition of human recombinant topoisomerase 1-mediated DNA cleavage using [32P]-3'-end-labeled 117-bp DNA fragment as substrate at 100 uM after 20 mins by SDS-PAGE analysis2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID247283Concentration required to inhibit the growth of human Renal SN12C cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
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.
AID247282Concentration required to inhibit the growth of human Lung HOP-62 cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
AID620802Cytotoxicity against human SF539 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
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.
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.
AID297645Cytotoxicity against human HOP62 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
AID273198Cytotoxicity against human OVCAR-3 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
AID247165Growth inhibition against Breast MDA-MB-435 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID297399Cytotoxicity against human SF539 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID297398Cytotoxicity against human HCT116 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID1075786Cytotoxicity against human DU145 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID286257Cytotoxicity against human UACC62 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID458051Antiproliferative activity against human MDA-MB-435 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID223656Cytotoxicity in prostate DU-145 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
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.
AID46131Cytotoxicity against human CNSSF-539 cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID547380Antiproliferative activity against human SF539 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID56716Activity to produce DNA topoisomerase I-mediated DNA cleavage at concentration up to 10 uM; ++, indicates similar activity as the parent compound 22003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
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.
AID56867Inhibitory activity against human DNA topoisomerase I mediated DNA cleavage; Weak activity2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
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.
AID214741Cytotoxicity against human melanoma UACC-62 cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID297400Cytotoxicity against human UACC62 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID81501Cytotoxic concentration against human lung HOP-62 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID45949Compound was tested for its cytotoxicity against CNS SF-539 Human cancer cell line1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID297397Cytotoxicity against human HOP62 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID57725Cytotoxic concentration against human prostate DU-145 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID145412Cytotoxicity against human ovarian OVCAR-3 cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID1075796Inhibition of human recombinant topoisomerase 1 using radiolabeled DNA as substrate at 100 uM after 20 mins by SDS-PAGE2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID219867Cytotoxicity in colon HCT116 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID273194Cytotoxicity against human HOP62 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
AID145419Cytotoxicity against OVCAR-3 human ovarian cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID102144In vitro cytotoxicity against MDA-MB-435 (Human breast cancer) cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID286254Cytotoxicity against human HOP62 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID247155Growth inhibition against Renal SN12C cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
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.
AID247158Growth inhibition against ColonHCT-116 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID46084Cytotoxic concentration against human CNS SF-539 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID268887Antiproliferative activity against human NCI60 cell line measured as mean graph midpoint2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
AID657925Growth inhibition of human DU145 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
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.
AID214748Cytotoxicity against UACC-62 human melanoma cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID57718Cytotoxicity against human prostate DU-145 cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID1075793Cytotoxicity against human HOP62 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID247309Concentration required to inhibit the growth of human Prostate DU-145 cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
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.
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.
AID620804Cytotoxicity against human OVCAR3 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
AID297651Cytotoxicity against human DU145 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
AID657921Growth inhibition of human SF539 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID106678Cytotoxicity against human breast MIDA-MB-435 cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID657922Growth inhibition of human UACC62 cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID458062Inhibition of human recombinant topoisomerase-1-mediated 117bp DNA oligonucleotide cleavage at 10 uM by PAGE2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID286259Cytotoxicity against human SN12C cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID247257Growth inhibitory activity against human ovarian OVCAR-3 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID547388Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
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.
AID56887Inhibitory activity against DNA topoisomerase I cleavage was determined at a concentration ranging up to 10 uM; ''++'' indicates similar activity as the parent compound 252004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID458048Antiproliferative activity against human OVCAR-3 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID620747Inhibition of human topoisomerase 1 assessed as inhibition of radiolabeled DNA fragment cleavage 0.1 to 100 uM after 20 mins by gel-based phosphoimaging relative to control2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
AID200453Cytotoxic concentration against human renal SN12C cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID247296Concentration required to inhibit the growth of human Ovarian OVCAR cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
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.
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.
AID80394Cytotoxicity against human colon HCT116 cancer cell lines.2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID458044Antiproliferative activity against human UACC62 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID223626Cytotoxicity in ovarian OVCAR-3 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
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.
AID222024Cytotoxicity in melanoma UACC-62 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID247319Concentration required to inhibit the growth of human Breast MDA-MB-435 cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
AID1075788Cytotoxicity against human SN12C cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
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.
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.
AID228386Cytotoxicity in renal SN12C cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID56732DNA topoisomerase I mediated cleavage activity tested up to a concentration of 100 uM; Same activity as compound 12002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID273199Cytotoxicity against human SN12C cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
AID620806Cytotoxicity against human DU145 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
AID214743In vitro cytotoxicity against UACC-62 (Human melanoma) cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID297648Cytotoxicity against human UACC62 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
AID458046Antiproliferative activity against human HOP62 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID273201Cytotoxicity against human MDA-MB-435 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
AID273200Cytotoxicity against human DU145 cell line2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
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.
AID200457Cytotoxicity against SN12C human renal cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID247160Growth inhibition against OvarianOVCAR-3 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
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.
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.
AID297647Cytotoxicity against human SF539 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
AID297650Cytotoxicity against human SN12C cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
AID247153Growth inhibition against CNSSF-539 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID297401Cytotoxicity against human OVCAR-3 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
AID80392Cytotoxicity against HCT116 human colon cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
AID286255Cytotoxicity against human HCT116 cells2007Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
AID297646Cytotoxicity against human HCT116 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
AID297649Cytotoxicity against human OVCAR-3 cells2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
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.
AID247156Growth inhibition against Lung HOP-62 cell line2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
AID221331Cytotoxicity in lung HOP-62 cell line.2002Journal of medicinal chemistry, Jan-03, Volume: 45, Issue:1
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
AID247269Concentration required to inhibit the growth of human CNSSF-539 cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
AID620800Cytotoxicity against human HOP62 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
AID657924Growth inhibition of human SN12C cells after 48 hrs by sulforhodamine B assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
AID247242Growth inhibitory activity against human lung HOP-62 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID81498Cytotoxicity was determined in human lung HOP-62 cancer cell lines2003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
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.
AID247289Concentration required to inhibit the growth of human Colon HCT-11 cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
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.
AID620807Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
AID658164Stabilization of human G-quadruplex F21T assessed as change in melting temperature at 5 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries.
AID200452In vitro cytotoxicity against SN12C (Human renal cancer) cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID102147Cytotoxic concentration against human breast MDA-MB-435 cell line growth inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
AID458045Antiproliferative activity against human HCT116 cells2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
AID81502Cytotoxicity against HOP-62 human lung cancer cell line was determined2004Bioorganic & medicinal chemistry letters, Jul-16, Volume: 14, Issue:14
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
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.
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.
AID658163Stabilization of DNA duplex hairpin structure assessed as change in melting temperature at 1 uM by FRET assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries.
AID1075789Cytotoxicity against human OVCAR3 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID1075790Cytotoxicity against human UACC62 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
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.
AID547386Antiproliferative activity against human UO31 cells after 48 hrs by SRB assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
AID56724Compound was tested for its inhibitory activity against DNA topoisomerase I; similar activity as parent compound 12003Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
AID247316Concentration required to inhibit the growth of human Melanoma UACC-62 cells2005Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
AID57038The activity was examined against DNA topoisomerase I mediated DNA cleavage using 3''-End-labelled 161 BP plasmid DNA.++ indicates greater than 50% of the activity of 1 uM camptothecin1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
AID1075792Cytotoxicity against human HCT116 cells by SRB assay2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID247250Growth inhibitory activity against human colon HCT116 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID247258Growth inhibitory activity against human prostate DU-145 cell line2004Journal of medicinal chemistry, Nov-04, Volume: 47, Issue:23
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (31)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (6.45)18.2507
2000's18 (58.06)29.6817
2010's10 (32.26)24.3611
2020's1 (3.23)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%
Reviews1 (3.23%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other30 (96.77%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]