Compounds > braco-19
Page last updated: 2024-12-11

braco-19

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Description

BRACO-19: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9808666
CHEMBL ID336434
CHEBI ID33534
SCHEMBL ID1101549
MeSH IDM0423574

Synonyms (33)

Synonym
9-[4-(n,n-dimethylamino)phenylamino]-3,6-bis(3-pyrrolidinopropionamido) acridine
CHEBI:33534 ,
9-[4-(n,n-dimethylamino)phenylamino]-3,6-bis(3-pyrrolodinopropionamido) acridine
n,n'-(9-{[4-(dimethylamino)phenyl]amino}acridine-3,6-diyl)bis(3-pyrrolidin-1-ylpropanamide)
braco19
braco-19
n,n''-(9-{[4-(dimethylamino)phenyl]amino}acridine-3,6-diyl)bis(3-pyrrolidin-1-ylpropanamide)
bdbm50134030
CHEMBL336434 ,
C20202
9-[4-(n,n-dimethylamino)phenylamino]-3,6-bis (3-pyrrolodino-propionamido) acridine
351351-75-2
unii-z7c5cd91wi
z7c5cd91wi ,
n,n'-(9-((4-(dimethylamino)phenyl)amino)-3,6-acridinediyl)bis(1-pyrrolidinepropanamide)
1-pyrrolidinepropanamide, n,n'-(9-((4-(dimethylamino)phenyl)amino)-3,6-acridinediyl)bis-
875923-92-5
SCHEMBL1101549
braco19 trihydrochloride
n-[9-[4-(dimethylamino)anilino]-6-(3-pyrrolidin-1-ylpropanoylamino)acridin-3-yl]-3-pyrrolidin-1-yl-propanamide
braco 19
n-(9-{[4-(dimethylamino)phenyl]amino}-6-[3-(pyrrolidin-1-yl)propanamido]acridin-3-yl)-3-(pyrrolidin-1-yl)propanamide
mfcd10574844
Q27115677
nsc847499
nsc-847499
cs0006872
n,n'-[9-[[4-(dimethylamino)phenyl]amino]-3,6-acridinediyl]bis-1-pyrrolidinepropanamide
NCGC00487231-01
CS-0006872 ,
HY-15523
n-[9-[4-(dimethylamino)anilino]-6-(3-pyrrolidin-1-ylpropanoylamino)acridin-3-yl]-3-pyrrolidin-1-ylpropanamide
AKOS040748047

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" The results demonstrate that the preparation of dosage forms and their storage conditions will have an important influence on the stability--and hence biological efficacy--of BRACO19 and related substances."( Decomposition of the telomere-targeting agent BRACO19 in physiological media results in products with decreased inhibitory potential.
Baldes, C; Boettcher, S; Kleideiter, E; Klotz, U; Lehr, CM; Mürdter, TE; Piotrowska, K; Schaefer, UF; Taetz, S; Zapp, J, 2008)		0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
acridines
N-alkylpyrrolidine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Telomerase reverse transcriptaseHomo sapiens (human)IC50 (µMol)1.08830.00062.69489.4000AID329708; AID329709; AID329710; AID393294; AID437317; AID471962
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Telomerase reverse transcriptaseHomo sapiens (human)EC50 (µMol)1.35220.11301.35226.3000AID212746; AID240076; AID257826; AID306427; AID409477
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
telomere maintenanceTelomerase reverse transcriptaseHomo sapiens (human)
RNA-templated transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
RNA-templated DNA biosynthetic processTelomerase reverse transcriptaseHomo sapiens (human)
telomere maintenance via telomeraseTelomerase reverse transcriptaseHomo sapiens (human)
mitochondrion organizationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of gene expressionTelomerase reverse transcriptaseHomo sapiens (human)
DNA strand elongationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of Wnt signaling pathwayTelomerase reverse transcriptaseHomo sapiens (human)
siRNA processingTelomerase reverse transcriptaseHomo sapiens (human)
regulation of protein stabilityTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of hair cycleTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of neuron apoptotic processTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of angiogenesisTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of glucose importTelomerase reverse transcriptaseHomo sapiens (human)
response to cadmium ionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityTelomerase reverse transcriptaseHomo sapiens (human)
establishment of protein localization to telomereTelomerase reverse transcriptaseHomo sapiens (human)
cellular response to hypoxiaTelomerase reverse transcriptaseHomo sapiens (human)
DNA biosynthetic processTelomerase reverse transcriptaseHomo sapiens (human)
replicative senescenceTelomerase reverse transcriptaseHomo sapiens (human)
siRNA transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of miRNA transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of transdifferentiationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of protein localization to nucleolusTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of endothelial cell apoptotic processTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of stem cell proliferationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of cellular senescenceTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandTelomerase reverse transcriptaseHomo sapiens (human)
telomere maintenance via telomeraseProtection of telomeres protein 1Homo sapiens (human)
telomere cappingProtection of telomeres protein 1Homo sapiens (human)
telomere assemblyProtection of telomeres protein 1Homo sapiens (human)
positive regulation of telomere maintenanceProtection of telomeres protein 1Homo sapiens (human)
regulation of telomere maintenance via telomeraseProtection of telomeres protein 1Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseProtection of telomeres protein 1Homo sapiens (human)
positive regulation of telomere maintenance via telomeraseProtection of telomeres protein 1Homo sapiens (human)
DNA duplex unwindingProtection of telomeres protein 1Homo sapiens (human)
positive regulation of helicase activityProtection of telomeres protein 1Homo sapiens (human)
positive regulation of telomerase activityProtection of telomeres protein 1Homo sapiens (human)
negative regulation of telomerase activityProtection of telomeres protein 1Homo sapiens (human)
positive regulation of DNA strand elongationProtection of telomeres protein 1Homo sapiens (human)
telomeric D-loop disassemblyProtection of telomeres protein 1Homo sapiens (human)
establishment of protein localization to telomereProtection of telomeres protein 1Homo sapiens (human)
regulation of DNA helicase activityProtection of telomeres protein 1Homo sapiens (human)
positive regulation of DNA helicase activityProtection of telomeres protein 1Homo sapiens (human)
regulation of double-strand break repair via nonhomologous end joiningProtection of telomeres protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
tRNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
transcription coactivator bindingTelomerase reverse transcriptaseHomo sapiens (human)
DNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomerase activityTelomerase reverse transcriptaseHomo sapiens (human)
telomerase RNA reverse transcriptase activityTelomerase reverse transcriptaseHomo sapiens (human)
RNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
RNA-directed DNA polymerase activityTelomerase reverse transcriptaseHomo sapiens (human)
RNA-dependent RNA polymerase activityTelomerase reverse transcriptaseHomo sapiens (human)
protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
identical protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
protein homodimerization activityTelomerase reverse transcriptaseHomo sapiens (human)
metal ion bindingTelomerase reverse transcriptaseHomo sapiens (human)
protein-folding chaperone bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomerase RNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
template-free RNA nucleotidyltransferaseTelomerase reverse transcriptaseHomo sapiens (human)
telomeric DNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomeric G-quadruplex DNA bindingProtection of telomeres protein 1Homo sapiens (human)
protein bindingProtection of telomeres protein 1Homo sapiens (human)
telomerase inhibitor activityProtection of telomeres protein 1Homo sapiens (human)
DEAD/H-box RNA helicase bindingProtection of telomeres protein 1Homo sapiens (human)
telomeric DNA bindingProtection of telomeres protein 1Homo sapiens (human)
single-stranded telomeric DNA bindingProtection of telomeres protein 1Homo sapiens (human)
telomeric D-loop bindingProtection of telomeres protein 1Homo sapiens (human)
G-rich strand telomeric DNA bindingProtection of telomeres protein 1Homo sapiens (human)
8-hydroxy-2'-deoxyguanosine DNA bindingProtection of telomeres protein 1Homo sapiens (human)
G-rich single-stranded DNA bindingProtection of telomeres protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
PML bodyTelomerase reverse transcriptaseHomo sapiens (human)
chromosome, telomeric regionTelomerase reverse transcriptaseHomo sapiens (human)
nucleusTelomerase reverse transcriptaseHomo sapiens (human)
nucleoplasmTelomerase reverse transcriptaseHomo sapiens (human)
telomerase holoenzyme complexTelomerase reverse transcriptaseHomo sapiens (human)
nucleolusTelomerase reverse transcriptaseHomo sapiens (human)
cytosolTelomerase reverse transcriptaseHomo sapiens (human)
plasma membraneTelomerase reverse transcriptaseHomo sapiens (human)
nuclear speckTelomerase reverse transcriptaseHomo sapiens (human)
mitochondrial nucleoidTelomerase reverse transcriptaseHomo sapiens (human)
TERT-RMRP complexTelomerase reverse transcriptaseHomo sapiens (human)
telomerase catalytic core complexTelomerase reverse transcriptaseHomo sapiens (human)
nuclear telomere cap complexTelomerase reverse transcriptaseHomo sapiens (human)
RNA-directed RNA polymerase complexTelomerase reverse transcriptaseHomo sapiens (human)
chromosome, telomeric regionProtection of telomeres protein 1Homo sapiens (human)
nucleoplasmProtection of telomeres protein 1Homo sapiens (human)
shelterin complexProtection of telomeres protein 1Homo sapiens (human)
nuclear telomere cap complexProtection of telomeres protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (125)

Assay IDTitleYearJournalArticle
AID1775111Displacement of 2-((E)-4-(Dimethylamino)styryl)-1-methyl-4-((Z)-(3-(3-morpholinopropyl)benzo[d]thiazol-2(3H)-ylidene)methyl)quinolin-1-ium iodide from telomeric Htg24 G4 quadruplex DNA in human U87 cells assessed as decrease in fluorescence intensity at 52021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Molecular Recognition and Imaging of Human Telomeric G-Quadruplex DNA in Live Cells: A Systematic Advancement of Thiazole Orange Scaffold To Enhance Binding Specificity and Inhibition of Gene Expression.
AID1473368Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for bloodstream form of Trypanosoma brucei brucei2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID374944Stabilization of human G4-KIT2 DNA quadruplex assessed as melting temperature by FRET assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID374947Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID1073186Binding affinity to HIV 1 HXB2 G-tract mutant m5/m4 FL-LTR assessed as formation of LTR G-quadruplex by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID374945Antiproliferative activity against human GIST882 cells after 96 hrs by SRB assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID471962Inhibition of telomerase in human A2780 cells by TRAP assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Prediction of telomerase inhibitory activity for acridinic derivatives based on chemical structure.
AID221795Affinity constant for binding to human 22-mer quadruplex2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.
AID409467Stabilization of d[G3(T2AG3)3] sequence of F21T telomeric G-quadruplex DNA assessed as change in melting temperature at 1 uM by FRET assay relative to BRACO-19 in presence of calf thymus DNA2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID409472Binding affinity to biotin-labeled d[CGA2T2CGTCTC2GA2T2CG] sequence of duplex DNA by surface plasmon resonance analysis2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID257831Inhibition of TAQ polymerase activity at 2 uM2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
AID409464Stabilization of d[G3(T2AG3)3] sequence of F21T telomeric G-quadruplex DNA assessed as change in melting temperature at 1 uM by FRET assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID1349266Stabilization of 3'-6FAM/5'-Dabcyl-labelled human telomeric 22 G-quadruplex DNA assessed as change in melting temperature at 0.75 uM by fluorescence assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.
AID437313Binding affinity to human telomeric DNA G-quadruplex assessed as change in melting temperature at 20 uM by FRET assay2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands.
AID1349264Stabilization of 5'6FAM/3'Dabcyl-labelled double stranded DNA (unknown origin) assessed as change in melting temperature at 0.75 uM by fluorescence assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.
AID374961Reduction in KIT protein expression in human GIST882 cells after 24 hrs by Western blot2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID1073180Binding affinity to HIV 1 HXB2 G-tract mutant m3'' FL-LTR assessed as effect on LTR G-quadruplex formation by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1073173Inhibition of wild-type HIV 1 HXB2 LTR DNA assessed as reduction in promoter activity at 6 uM after 24 hrs by GFP reporter assay in the presence of Tat2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID306430Growth inhibition of human A549 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
AID393296Inhibition of non G-quadruplex [TTAGAG]4 DNA templet extension assessed as ligand-induced polymerase stop products by Taq DNA polymerase stop assay2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID1775069Stabilization of telomeric Htg24 G-quadruplex DNA (unknown origin) assessed as inhibition of DNA amplification at 20 uM by PCR analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Molecular Recognition and Imaging of Human Telomeric G-Quadruplex DNA in Live Cells: A Systematic Advancement of Thiazole Orange Scaffold To Enhance Binding Specificity and Inhibition of Gene Expression.
AID1073195Binding affinity to HIV 1 HXB2 G-quadruplex LTR-2 DNA assessed as change in melting temperature at 16 uM after 24 hrs by circular dichroism spectropolarimeter analysis in the presence of K+2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1605723Stabilization of G4 quadruplex DNA in human U2OS cells assessed as increase in number of G4 foci at 10 uM incubated for 24 hrs by immunofluorescence microscopy2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells.
AID409463Stabilization of d[AGAG3AG2GCGCTG3AG2AG3GCT] sequence of c-kit1 G-quadruplex DNA assessed as change in melting temperature at 1 uM by FRET assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID329709Inhibition of human telomerase expressed in HEK293T cells treated after telomerase elongation by telomeric repeat amplification protocol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID374948Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID226208Affinity constant for binding to duplex DNA2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.
AID257829Cytotoxicity in human IMR90 cells by SRB assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
AID212746Inhibitory activity against human telomerase2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.
AID1349265Stabilization of 5'6FAM/3'Dabcyl-labelled double stranded DNA (unknown origin) assessed as change in melting temperature at 2.5 uM by fluorescence assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.
AID1473363Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei after 72 hrs by alamar blue assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID393288Induction of G-quadruplex structure formation in human telomeric d[5'G3(T2AG3]-3' DNA assessed as major positive band at 295 nm at 2 mole ligand concentration by CD spectroscopy2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID257827Ratio of binding constant of compound binding to human quadruplex DNA over that of duplex DNA2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
AID1775101Downregulation of hTERT mRNA expression in human HeLa cells at 5 to 20 uM by qRT-PCR analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Molecular Recognition and Imaging of Human Telomeric G-Quadruplex DNA in Live Cells: A Systematic Advancement of Thiazole Orange Scaffold To Enhance Binding Specificity and Inhibition of Gene Expression.
AID393287Inhibition of human G-quadruplex [TTAGGG]4 DNA templet extension assessed as increase in ligand-induced polymerase stop products by Taq DNA polymerase stop assay2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID1495939Antiproliferative activity against imatinib-susceptible human GIST882 cells harboring c-KIT K642E mutant after 96 hrs by SRB assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1495944Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1495942Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID257826Inhibition of telomerase activity from human A2780 cells2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
AID1073177Inhibition of wild-type HIV 1 HXB2 LTR DNA assessed as reduction in promoter activity after 24 hrs by GFP reporter assay in the presence of Tat2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1495940Antiproliferative activity against imatinib-resistant human GIST48 cells harboring c-KIT V560D/D820A double mutant after 96 hrs by SRB assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID409482Selectivity ratio of IC50 for human MCF7 cells to IC50 for human WI38 cells2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID409478Inhibition of telomerase at 50 uM by TRAP-LIG assay relative to control2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID1073175Antiviral activity against wild type HIV 1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral replication at 3 to 6 uM after 48 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1495936Stabilization of 5'-FAM/3'-TAMRA labeled duplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1473366Antimalarial activity against erythrocyte stage of Plasmodium falciparum 3D7 preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID409471Binding affinity to biotin-labeled d[(AG3TG4)2A] sequence of c-myc G-quadruplex DNA by surface plasmon resonance analysis2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID329713Decrease in telomerase processivity assessed as decrease in telomerase elongation in presence of Telo3R primer by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID374942Stabilization of synthetic duplex DNA assessed as melting temperature by FRET assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID1073182Binding affinity to HIV 1 HXB2 G-tract mutant m1 FL-LTR assessed as effect on LTR G-quadruplex formation by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID409480Cytotoxicity against human A549 cells after 96 hrs by SRB assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID253269Concentration required for G4-stabilisation in FRET assay2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis, biophysical and biological evaluation of 3,6-bis-amidoacridines with extended 9-anilino substituents as potent G-quadruplex-binding telomerase inhibitors.
AID374943Stabilization of human G4-KIT1 DNA quadruplex assessed as melting temperature by FRET assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID1073190Binding affinity to HIV 1 HXB2 G-quadruplex LTR-FL DNA assessed as change in melting temperature at 16 uM after 24 hrs by circular dichroism spectropolarimeter analysis in the presence of K+2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1073188Binding affinity to HIV 1 HXB2 G-quadruplex FL-LTR DNA assessed as blocking at G-tracts (6 and 5) after 20 mins by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1605728Stabilization of G4 quadruplex DNA in human U2OS cells assessed as TRF2 foci per cell at 10 uM incubated for 24 hrs by immunofluorescence microscopy (Rvb = 15.8 +/- 2.6%)2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells.
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.
AID437316Binding affinity to human telomeric DNA G-quadruplex assessed as change in melting temperature at 1 uM by FRET assay2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands.
AID409470Binding affinity to biotin-labeled d[(CG3)2CGCGAG3AG4] sequence of c-kit2 G-quadruplex DNA by surface plasmon resonance analysis2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID306426Effect on human G-quadruplex DNA stability by FRET assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
AID409466Stabilization of d[(TA)2GC(TA)2T6(TA)2]GC(TA)2 sequence of duplex DNA assessed as change in melting temperature at 1 uM by FRET assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID306428Growth inhibition of human DU145 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
AID1073187Binding affinity to HIV 1 HXB2 G-quadruplex FL-LTR DNA assessed as blocking sites at G-tracts (4 to 2) after 20 mins by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID409469Binding affinity to biotin-labeled d[(AG3)2CGCTG3AG2AG3] sequence of c-kit1 G-quadruplex DNA by surface plasmon resonance analysis2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID329711Inhibition of human telomerase expressed in HEK293T cells in presence of primer TS by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID1473365Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID240076Effective concentration against telomerase by TRAP2004Bioorganic & medicinal chemistry letters, Aug-16, Volume: 14, Issue:16
Synthesis, biophysical and biological evaluation of 3,6-bis-amidoacridines with extended 9-anilino substituents as potent G-quadruplex-binding telomerase inhibitors.
AID437314Binding affinity to human telomeric DNA G-quadruplex assessed as change in melting temperature at 10 uM by FRET assay2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands.
AID409481Cytotoxicity against human WI38 cells after 96 hrs by SRB assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID437317Inhibition of human telomerase in A549 cells by TRAP assay2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands.
AID437315Binding affinity to human telomeric DNA G-quadruplex assessed as change in melting temperature at 5 uM by FRET assay2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis and biological evaluation of novel 4,5-bis(dialkylaminoalkyl)-substituted acridines as potent telomeric G-quadruplex ligands.
AID409477Inhibition of telomerase by TRAP-LIG assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID1073179Inhibition of wild-type HIV 1 HXB2 LTR DNA assessed as reduction in promoter activity at 1.5 to 6 uM after 24 hrs by luciferase assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID393290Binding affinity to human telomeric d[5'G3(T2AG3]-3' DNA quadruplex assessed as major positive band at 292 nm at 2:1 drug to DNA ratio2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID1473369Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for erythrocyte stage of Plasmodium falciparum 3D72018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID306427Inhibition of human telomerase by TRAP assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
AID374941Stabilization of human G4-telomeric quadruplex assessed as melting temperature by FRET assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID1473367Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for Leishmania major MHOM/IL/80/Friedlin promastigotes2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1073178Inhibition of HIV 1 HXB2 G-tract mutant m5 LTR DNA assessed as reduction in promoter activity at 1.5 to 6 uM after 24 hrs by luciferase assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1073172Cytotoxicity against human TZM-bl cells at 0.1 to 6 uM after 48 hrs2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1495932Stabilization of 5'-FAM/3'-TAMRA labeled c-KIT1 G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1073184Binding affinity to HIV 1 HXB2 G-tract mutant m6' FL-LTR assessed as formation of LTR-2 and LTR-3 G-quadruplex by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1073191Binding affinity to HIV 1 HXB2 G-quadruplex LTR-3 DNA assessed as change in melting temperature at 16 uM after 24 hrs by circular dichroism spectropolarimeter analysis in the presence of K+2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
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.
AID1495935Stabilization of 5'-FAM/3'-TAMRA labeled 5'-UTR BCL-2 G-quadruplex RNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID329708Inhibition of human telomerase expressed in HEK293T cells treated before telomerase elongation by telomeric repeat amplification protocol assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID306429Growth inhibition of human MCF7 cells by SRB assay2007Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
AID1073185Binding affinity to HIV 1 HXB2 G-tract mutant m3 FL-LTR assessed as formation of LTR-4 G-quadruplex by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID218897Cytotoxicity against ovarian carcinoma A431 cell lines2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.
AID1073194Binding affinity to HIV 1 HXB2 G-tract mutant m6 FL-LTR DNA assessed as formation of LTR-2 G-quadruplex by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID393295Inhibition of human 35S-labeled Pot1 binding to human telomeric DNA2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID329712Inhibition of human telomerase expressed in in HEK293T cells in presence of primer (T2AG3)4 by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID1349267Stabilization of 3'-6FAM/5'-Dabcyl-labelled human telomeric 22 G-quadruplex DNA assessed as change in melting temperature at 2.5 uM by fluorescence assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.
AID1495941Antiproliferative activity against imatinib-resistant human GIST62 cells after 96 hrs by SRB assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1775102Downregulation of hTERC mRNA expression in human HeLa cells at 5 to 20 uM by qRT-PCR analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Molecular Recognition and Imaging of Human Telomeric G-Quadruplex DNA in Live Cells: A Systematic Advancement of Thiazole Orange Scaffold To Enhance Binding Specificity and Inhibition of Gene Expression.
AID1495933Stabilization of 5'-FAM/3'-TAMRA labeled c-KIT2 G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID724611Binding affinity to human telomeric sequence 5'-AGGGTTAGGGTTAGGGTTAGGGT-3' assessed as melting temperature at 10 uM by fluorescence melting assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of new DNA G-quadruplex binders selected by a combination of ligand and structure-based virtual screening approaches.
AID409468Binding affinity to biotin-labeled human telomeric d[AG3(T2AG3)3] sequence by surface plasmon resonance analysis2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID409483Selectivity ratio of IC50 for human A549 cells to IC50 for human WI38 cells2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID374953Reduction in KIT mRNA expression in human GIST882 cells after 24 hrs2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID329710Inhibition of human telomerase expressed in HEK293T cells in presence of primer (T2AG3)3 by primer extension assay2007Proceedings of the National Academy of Sciences of the United States of America, Oct-30, Volume: 104, Issue:44
Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
AID1495931Stabilization of 5'-FAM/3'-TAMRA labeled human F21T G-quadruplex DNA assessed as change in melting temperature at 0.5 uM by FRET assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1495943Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1726680Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2021RSC medicinal chemistry, Mar-26, Volume: 12, Issue:5
Synthesis and evaluation of bis(imino)anthracene derivatives as G-quadruplex ligands.
AID409479Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID1073181Binding affinity to HIV 1 HXB2 G-tract mutant m3' FL-LTR assessed as effect on LTR G-quadruplex formation by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1073174Antiviral activity against Nef-deficient HIV 1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral replication at 3 to 6 uM after 48 hrs by luciferase reporter gene assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1073193Binding affinity to HIV 1 HXB2 G-quadruplex LTR-2 DNA assessed as change in melting temperature at 16 uM after 24 hrs by circular dichroism spectropolarimeter analysis in the absence of K+2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1473364Antileishmanial activity against Leishmania major MHOM/IL/80/Friedlin promastigotes after 72 hrs by MTT assay2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID218896Cytotoxicity against ovarian carcinoma A2780 cell lines2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Trisubstituted acridine derivatives as potent and selective telomerase inhibitors.
AID409465Stabilization of d[C3G3CG3CGCGAG3AG4AG2] sequence of c-kit2 G-quadruplex DNA assessed as change in melting temperature at 1 uM by FRET assay2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
AID1775105Induction of cellular senescence in human HeLa cells assessed as positive SA-beta-Gal cells at 0.5 to 4 uM incubated for 18 days by inverted fluorescence microscopic analysis2021Journal of medicinal chemistry, 02-25, Volume: 64, Issue:4
Molecular Recognition and Imaging of Human Telomeric G-Quadruplex DNA in Live Cells: A Systematic Advancement of Thiazole Orange Scaffold To Enhance Binding Specificity and Inhibition of Gene Expression.
AID1073192Binding affinity to HIV 1 HXB2 G-quadruplex LTR-3 DNA assessed as change in melting temperature at 16 uM after 24 hrs by circular dichroism spectropolarimeter analysis in the absence of K+2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID374946Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule.
AID393294Inhibition of human telomerase assessed as unincorporated [alpha32P]dGTP2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID1717167Cytotoxicity against human U2OS cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Dimeric aryl-substituted imidazoles may inhibit ALT cancer by targeting the multimeric G-quadruplex in telomere.
AID1073189Binding affinity to HIV 1 HXB2 G-quadruplex LTR-4 DNA assessed as change in melting temperature at 16 uM after 24 hrs by circular dichroism spectropolarimeter analysis in the presence of K+2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1349268Inhibition of HDAC in human HeLa nuclear extract using Fluor de Lys as substrate by fluorimetric method2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Novel Polyamine-Naphthalene Diimide Conjugates Targeting Histone Deacetylases and DNA for Cancer Phenotype Reprogramming.
AID1073183Binding affinity to HIV 1 HXB2 G-tract mutant m2 FL-LTR assessed as formation of LTR-2 G-quadruplex by Taq polymerase stop assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID393293Stabilization of human telomeric d[5'G3(T2AG3]-3' assessed as change in melting temperature at 25 uM2009Bioorganic & medicinal chemistry, Mar-01, Volume: 17, Issue:5
BRACO19 analog dimers with improved inhibition of telomerase and hPot 1.
AID1495934Stabilization of 5'-FAM/3'-TAMRA labeled BCL-2 promoter G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line.
AID1073176Inhibition of wild-type HIV 1 HXB2 LTR DNA assessed as reduction in promoter activity after 24 hrs by GFP reporter assay in the absence of Tat2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
AID1605726Stabilization of G4 quadruplex DNA in human U2OS cells assessed as colocalization of TRF2/BGF4 foci at 10 uM incubated for 24 hrs by immunofluorescence microscopy (Rvb = 18.4 +/- 2.81%)2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (66)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's26 (39.39)29.6817
2010's30 (45.45)24.3611
2020's10 (15.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.87

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

MetricThis Compound (vs All)
Research Demand Index29.87 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index4.62 (4.65)
Search Engine Demand Index32.77 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (6.06%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other62 (93.94%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
naphthalene
[no description available]		3.1610naphthalenes;
ortho-fused bicyclic arene		apoptosis inhibitor;
carcinogenic agent;
environmental contaminant;
mouse metabolite;
plant metabolite;
volatile oil component
spermine
[no description available]		7.2110polyazaalkane;
tetramine		antioxidant;
fundamental metabolite;
immunosuppressive agent
berberine
[no description available]		2.2110alkaloid antibiotic;
berberine alkaloid;
botanical anti-fungal agent;
organic heteropentacyclic compound		antilipemic drug;
antineoplastic agent;
antioxidant;
EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor;
EC 1.21.3.3 (reticuline oxidase) inhibitor;
EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.1.4 (phospholipase A2) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
hypoglycemic agent;
metabolite;
potassium channel blocker
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		2.1710aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
stallimycin
[no description available]		3.1610
miltefosine
miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine.		2.1710phosphocholines;
phospholipid		anti-inflammatory agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
apoptosis inducer;
immunomodulator;
protein kinase inhibitor
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		2.2110dihydroxyanthraquinoneanalgesic;
antineoplastic agent
scriptaid
scriptide: provokes translocation of GLUT4 to increase glucose uptake; structure in first source		2.1510isoquinolines
imatinib
[no description available]		2.4920aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		2.2510dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
bromodeoxyuridine
Bromodeoxyuridine: A nucleoside that substitutes for thymidine in DNA and thus acts as an antimetabolite. It causes breaks in chromosomes and has been proposed as an antiviral and antineoplastic agent. It has been given orphan drug status for use in the treatment of primary brain tumors.		2.0310pyrimidine 2'-deoxyribonucleosideantimetabolite;
antineoplastic agent
tolonium chloride
Tolonium Chloride: A phenothiazine that has been used as a hemostatic, a biological stain, and a dye for wool and silk. Tolonium chloride has also been used as a diagnostic aid for oral and gastric neoplasms and in the identification of the parathyroid gland in thyroid surgery.. tolonium chloride : An organic chloride salt having 3-amino-7-(dimethylamino)-2-methylphenothiazin-5-ium (tolonium) as the counterion. It is a blue nuclear counterstain that can be used to demonstrate Nissl substance and is also useful for staining mast cell granules, both in metachromatic and orthochromatic techniques.		2.0710
perylene
Perylene: A 20-carbon dibenz(de,kl)anthracene that can be viewed as a naphthalene fused to a phenalene or as dinaphthalene. It is used as fluorescent lipid probe in the cytochemistry of membranes and is a polycyclic hydrocarbon pollutant in soil and water. Derivatives may be carcinogenic.. perylene : An ortho- and peri-fused polycyclic arene comprising of five benzene rings that is anthracene in which the d,e and k,l sides are fused to benzene rings.		2.0810ortho- and peri-fused polycyclic arene;
perylenes
acridines
Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.		12.44460acridines;
mancude organic heterotricyclic parent;
polycyclic heteroarene		genotoxin
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		3.53201,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
dequalinium chloride
dequalinium chloride : An organic chloride salt that is the dichloride salt of dequalinium.		2.0710organic chloride saltantifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor
Berberine chloride (TN)
[no description available]		2.0710organic molecular entity
daunorubicin
Daunorubicin: A very toxic anthracycline aminoglycoside antineoplastic isolated from Streptomyces peucetius and others, used in treatment of LEUKEMIA and other NEOPLASMS.. anthracycline : Anthracyclines are polyketides that have a tetrahydronaphthacenedione ring structure attached by a glycosidic linkage to the amino sugar daunosamine.. daunorubicin : A natural product found in Actinomadura roseola.		3.1610aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones		antineoplastic agent;
bacterial metabolite
acodazole
[no description available]		2.0710
lissamine rhodamine b
lissamine rhodamine B: RN given refers to parent cpd; Lissamine Rhodamine B refers to Na salt		2.0210
nsc 38280
[no description available]		2.0710
methoxy-morpholinyl-doxorubicin
methoxy-morpholinyl-doxorubicin: structure in first source		2.3110anthracycline antibiotic;
morpholines;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone
taspine
taspine: RN given refers to parent cpd; structure		2.0710
nsc 314622
NSC 314622: structure in first source		2.0710
Telomestatin
[no description available]		2.03101,3-oxazoles
alvocidib
alvocidib: structure given in first source. alvocidib : A synthetic dihydroxyflavone that is 5,7-dihydroxyflavone which is substituted by a 3-hydroxy-1-methylpiperidin-4-yl group at position 8 and by a chlorine at the 2' position (the (-)-3S,4R stereoisomer). A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic plaque formation.		2.0110dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound		antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
thiazole orange
thiazole orange: structure given in first source. thiazole orange : A cyanine dye comprising the thiazole orange cation [1-methyl-4-[(3-methyl-1,3-benzothiazol-2(3H)-ylidene)methyl]quinolinium] with the p-tosylate counterion.		7.2110cyanine dyefluorochrome
bibr 1532
[no description available]		3.8230
telomestatin
telomestatin: isolated from Spreptomyces anulatus; structure in first source		3.5320
oligonucleotides
[no description available]		3.1410
nk 5
NK 5: antioxidant containing divalent cations of iron, manganese, & cobalt		2.0710organic iodide salt;
quinolines		fluorochrome
pyridostatin
pyridostatin: binds telomeric G-quadruplexes; structure in first source		3.3150
cx 5461
CX 5461: structure in first source		2.3110diazepine;
naphthyridine derivative;
organic heterotetracyclic compound;
pyrazines;
secondary carboxamide		antineoplastic agent;
apoptosis inducer;
EC 2.7.7.6 (RNA polymerase) inhibitor
piperidines
Piperidines: A family of hexahydropyridines.		2.4420
bryostatin 1
bryostatin 1: a protein kinase C activator; macrocyclic lactone from marine Bryozoan Bugula neritina; RN given refers to (1S*-(1R*,3R*,5Z,7S*,8E,11R*,12R*(2E,4E),13E,15R*,17S*(S*),21S*,23S*,25R*))-isomer; structure given in first source; activates protein kinase c. bryostatin 1 : A member of the class of bryostatins that is (17E)-2-oxooxacyclohexacos-17-ene which is substituted by hydroxy groups at positions 4, 10, and 20; an acetoxy group at position 8; methyl groups at positions 9, 9, 18, and 19; 2-methoxy-2-oxoethylidene groups at positions 14 and 24; an (E,E)-octa-2,4-dienoyloxy group at position 21; and with oxygen bridges linking positions 6 to 10, 12 to 16, and 20 to 24. It is one of the most abundant member of the class of bryostatins.		2.2510
grn163
GRN163: inhibitor of telomerase RNA in human multiple myeloma cells.		3.1410
cyclin d1
Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.		2.0110
tetra(4-n-methylpyridyl)porphine
tetra(4-N-methylpyridyl)porphine: structure in first source		4.7680
guanine
[no description available]		2.78302-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Gastrointestinal Stromal Neoplasm
[description not available]		02.0510
Gastrointestinal Stromal Tumors
All tumors in the GASTROINTESTINAL TRACT arising from mesenchymal cells (MESODERM) except those of smooth muscle cells (LEIOMYOMA) or Schwann cells (SCHWANNOMA).		02.0510
Cancer of Gastrointestinal Tract
[description not available]		02.1710
Genome Instability
[description not available]		02.2510
Hendra Virus Infections
[description not available]		02.2510
HIV Coinfection
[description not available]		02.2510
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		02.2510
Benign Neoplasms
[description not available]		04.1430
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.		04.1430
Astrocytoma, Grade IV
[description not available]		02.1310
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		07.1310
Cancer of Colon
[description not available]		02.0110
Colonic Neoplasms
Tumors or cancer of the COLON.		02.0110
Cancer of Prostate
[description not available]		02.0210
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.0210
Cancer of the Uterus
[description not available]		02.0210
Uterine Neoplasms
Tumors or cancer of the UTERUS.		02.0210
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0210
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0110
Experimental Neoplasms
[description not available]		02.0110