Page last updated: 2024-11-12

di-2-pyridylketone-4,4-dimethyl-3-thiosemicarbazone

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Cross-References

ID SourceID
PubMed CID10334137
CHEMBL ID385064
SCHEMBL ID1025308
MeSH IDM0533925

Synonyms (35)

Synonym
iron chelator, dp44mt
CHEMBL385064 ,
nsc744381
nsc-744381
2,n-dimethylsemicarbazone
dp44mt
152095-12-0
di-2-pyridylketone-4,4,-dimethyl-3-thiosemicarbazone
3-[bis(2-pyridyl)methyleneamino]-1,1-dimethyl-thiourea
2-[di(pyridin-2-yl)methylidene]-n,n-dimethylhydrazinecarbothioamide
S7909
hydrazinecarbothioamide, 2-(di-2-pyridinylmethylene)-n,n-dimethyl-
SCHEMBL1025308
DTXSID80438322
mfcd20527329
di-2-pyridyl ketone 4,4-dimethylthiosemicarbazone
dp44mt, >=98% (hplc)
J-008883
HY-18973
CS-0014820
AKOS030603691
BCP15939
iron chelator
ams_cnc_id-343098670
smssf-0625533
EX-A2542
BS-15546
2-(di(pyridin-2-yl)methylene)-n,n-dimethylhydrazinecarbothioamide
3-(dipyridin-2-ylmethylideneamino)-1,1-dimethylthiourea
CCG-267326
A921110
C72884
bdbm50554640
CGA09512
2-(di(pyridin-2-yl)methylene)-n,n-dimethylhydrazine-1-carbothioamide
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histone deacetylase 1Homo sapiens (human)IC50 (µMol)5.00000.00010.55439.9000AID1699972
Histone deacetylase 8Homo sapiens (human)IC50 (µMol)5.00000.00070.99479.9000AID1699974
Histone deacetylase 6Homo sapiens (human)IC50 (µMol)5.00000.00000.53769.9000AID1699973
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (103)

Processvia Protein(s)Taxonomy
negative regulation of myotube differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
chromatin organizationHistone deacetylase 1Homo sapiens (human)
chromatin remodelingHistone deacetylase 1Homo sapiens (human)
DNA methylation-dependent heterochromatin formationHistone deacetylase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
protein deacetylationHistone deacetylase 1Homo sapiens (human)
endoderm developmentHistone deacetylase 1Homo sapiens (human)
positive regulation of cell population proliferationHistone deacetylase 1Homo sapiens (human)
epidermal cell differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
hippocampus developmentHistone deacetylase 1Homo sapiens (human)
neuron differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of cell migrationHistone deacetylase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
circadian regulation of gene expressionHistone deacetylase 1Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusHistone deacetylase 1Homo sapiens (human)
odontogenesis of dentin-containing toothHistone deacetylase 1Homo sapiens (human)
regulation of cell fate specificationHistone deacetylase 1Homo sapiens (human)
embryonic digit morphogenesisHistone deacetylase 1Homo sapiens (human)
negative regulation of apoptotic processHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionHistone deacetylase 1Homo sapiens (human)
negative regulation by host of viral transcriptionHistone deacetylase 1Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionHistone deacetylase 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIHistone deacetylase 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationHistone deacetylase 1Homo sapiens (human)
oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
positive regulation of oligodendrocyte differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of androgen receptor signaling pathwayHistone deacetylase 1Homo sapiens (human)
hair follicle placode formationHistone deacetylase 1Homo sapiens (human)
eyelid development in camera-type eyeHistone deacetylase 1Homo sapiens (human)
fungiform papilla formationHistone deacetylase 1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayHistone deacetylase 1Homo sapiens (human)
negative regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
positive regulation of stem cell population maintenanceHistone deacetylase 1Homo sapiens (human)
regulation of stem cell differentiationHistone deacetylase 1Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayHistone deacetylase 1Homo sapiens (human)
heterochromatin formationHistone deacetylase 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIHistone deacetylase 8Homo sapiens (human)
chromatin organizationHistone deacetylase 8Homo sapiens (human)
mitotic sister chromatid cohesionHistone deacetylase 8Homo sapiens (human)
negative regulation of protein ubiquitinationHistone deacetylase 8Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 8Homo sapiens (human)
regulation of telomere maintenanceHistone deacetylase 8Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 8Homo sapiens (human)
polyamine deacetylationHistone deacetylase 6Homo sapiens (human)
spermidine deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of signaling receptor activityHistone deacetylase 6Homo sapiens (human)
protein polyubiquitinationHistone deacetylase 6Homo sapiens (human)
response to amphetamineHistone deacetylase 6Homo sapiens (human)
protein deacetylationHistone deacetylase 6Homo sapiens (human)
protein quality control for misfolded or incompletely synthesized proteinsHistone deacetylase 6Homo sapiens (human)
intracellular protein transportHistone deacetylase 6Homo sapiens (human)
autophagyHistone deacetylase 6Homo sapiens (human)
actin filament organizationHistone deacetylase 6Homo sapiens (human)
negative regulation of microtubule depolymerizationHistone deacetylase 6Homo sapiens (human)
regulation of autophagyHistone deacetylase 6Homo sapiens (human)
positive regulation of epithelial cell migrationHistone deacetylase 6Homo sapiens (human)
negative regulation of hydrogen peroxide metabolic processHistone deacetylase 6Homo sapiens (human)
regulation of macroautophagyHistone deacetylase 6Homo sapiens (human)
axonal transport of mitochondrionHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex assemblyHistone deacetylase 6Homo sapiens (human)
regulation of protein stabilityHistone deacetylase 6Homo sapiens (human)
protein destabilizationHistone deacetylase 6Homo sapiens (human)
lysosome localizationHistone deacetylase 6Homo sapiens (human)
protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationHistone deacetylase 6Homo sapiens (human)
cellular response to heatHistone deacetylase 6Homo sapiens (human)
peptidyl-lysine deacetylationHistone deacetylase 6Homo sapiens (human)
response to immobilization stressHistone deacetylase 6Homo sapiens (human)
cellular response to topologically incorrect proteinHistone deacetylase 6Homo sapiens (human)
erythrocyte enucleationHistone deacetylase 6Homo sapiens (human)
ubiquitin-dependent protein catabolic process via the multivesicular body sorting pathwayHistone deacetylase 6Homo sapiens (human)
negative regulation of protein-containing complex disassemblyHistone deacetylase 6Homo sapiens (human)
regulation of fat cell differentiationHistone deacetylase 6Homo sapiens (human)
negative regulation of gene expression, epigeneticHistone deacetylase 6Homo sapiens (human)
negative regulation of proteolysisHistone deacetylase 6Homo sapiens (human)
negative regulation of DNA-templated transcriptionHistone deacetylase 6Homo sapiens (human)
collateral sproutingHistone deacetylase 6Homo sapiens (human)
negative regulation of axon extension involved in axon guidanceHistone deacetylase 6Homo sapiens (human)
positive regulation of dendrite morphogenesisHistone deacetylase 6Homo sapiens (human)
negative regulation of oxidoreductase activityHistone deacetylase 6Homo sapiens (human)
response to corticosteroneHistone deacetylase 6Homo sapiens (human)
response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicHistone deacetylase 6Homo sapiens (human)
cilium assemblyHistone deacetylase 6Homo sapiens (human)
regulation of microtubule-based movementHistone deacetylase 6Homo sapiens (human)
regulation of androgen receptor signaling pathwayHistone deacetylase 6Homo sapiens (human)
dendritic spine morphogenesisHistone deacetylase 6Homo sapiens (human)
cilium disassemblyHistone deacetylase 6Homo sapiens (human)
parkin-mediated stimulation of mitophagy in response to mitochondrial depolarizationHistone deacetylase 6Homo sapiens (human)
regulation of establishment of protein localizationHistone deacetylase 6Homo sapiens (human)
cellular response to hydrogen peroxideHistone deacetylase 6Homo sapiens (human)
aggresome assemblyHistone deacetylase 6Homo sapiens (human)
polyubiquitinated misfolded protein transportHistone deacetylase 6Homo sapiens (human)
response to growth factorHistone deacetylase 6Homo sapiens (human)
cellular response to misfolded proteinHistone deacetylase 6Homo sapiens (human)
cellular response to parathyroid hormone stimulusHistone deacetylase 6Homo sapiens (human)
response to dexamethasoneHistone deacetylase 6Homo sapiens (human)
tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of tubulin deacetylationHistone deacetylase 6Homo sapiens (human)
positive regulation of cellular response to oxidative stressHistone deacetylase 6Homo sapiens (human)
negative regulation of protein acetylationHistone deacetylase 6Homo sapiens (human)
regulation of autophagy of mitochondrionHistone deacetylase 6Homo sapiens (human)
positive regulation of cholangiocyte proliferationHistone deacetylase 6Homo sapiens (human)
negative regulation of aggrephagyHistone deacetylase 6Homo sapiens (human)
epigenetic regulation of gene expressionHistone deacetylase 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (37)

Processvia Protein(s)Taxonomy
nucleosomal DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
core promoter sequence-specific DNA bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 1Homo sapiens (human)
p53 bindingHistone deacetylase 1Homo sapiens (human)
transcription corepressor activityHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 1Homo sapiens (human)
protein bindingHistone deacetylase 1Homo sapiens (human)
enzyme bindingHistone deacetylase 1Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 1Homo sapiens (human)
Krueppel-associated box domain bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 1Homo sapiens (human)
NF-kappaB bindingHistone deacetylase 1Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
E-box bindingHistone deacetylase 1Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 1Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 1Homo sapiens (human)
promoter-specific chromatin bindingHistone deacetylase 1Homo sapiens (human)
histone deacetylase activityHistone deacetylase 8Homo sapiens (human)
protein bindingHistone deacetylase 8Homo sapiens (human)
Hsp70 protein bindingHistone deacetylase 8Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 8Homo sapiens (human)
metal ion bindingHistone deacetylase 8Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 8Homo sapiens (human)
DNA-binding transcription factor bindingHistone deacetylase 8Homo sapiens (human)
histone decrotonylase activityHistone deacetylase 8Homo sapiens (human)
acetylspermidine deacetylase activityHistone deacetylase 6Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHistone deacetylase 6Homo sapiens (human)
transcription corepressor bindingHistone deacetylase 6Homo sapiens (human)
actin bindingHistone deacetylase 6Homo sapiens (human)
histone deacetylase activityHistone deacetylase 6Homo sapiens (human)
protein bindingHistone deacetylase 6Homo sapiens (human)
beta-catenin bindingHistone deacetylase 6Homo sapiens (human)
microtubule bindingHistone deacetylase 6Homo sapiens (human)
zinc ion bindingHistone deacetylase 6Homo sapiens (human)
enzyme bindingHistone deacetylase 6Homo sapiens (human)
polyubiquitin modification-dependent protein bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin protein ligase bindingHistone deacetylase 6Homo sapiens (human)
protein lysine deacetylase activityHistone deacetylase 6Homo sapiens (human)
histone deacetylase bindingHistone deacetylase 6Homo sapiens (human)
tubulin deacetylase activityHistone deacetylase 6Homo sapiens (human)
alpha-tubulin bindingHistone deacetylase 6Homo sapiens (human)
ubiquitin bindingHistone deacetylase 6Homo sapiens (human)
tau protein bindingHistone deacetylase 6Homo sapiens (human)
beta-tubulin bindingHistone deacetylase 6Homo sapiens (human)
misfolded protein bindingHistone deacetylase 6Homo sapiens (human)
Hsp90 protein bindingHistone deacetylase 6Homo sapiens (human)
dynein complex bindingHistone deacetylase 6Homo sapiens (human)
transcription factor bindingHistone deacetylase 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (27)

Processvia Protein(s)Taxonomy
nucleusHistone deacetylase 1Homo sapiens (human)
nucleoplasmHistone deacetylase 1Homo sapiens (human)
cytoplasmHistone deacetylase 1Homo sapiens (human)
cytosolHistone deacetylase 1Homo sapiens (human)
NuRD complexHistone deacetylase 1Homo sapiens (human)
neuronal cell bodyHistone deacetylase 1Homo sapiens (human)
Sin3-type complexHistone deacetylase 1Homo sapiens (human)
histone deacetylase complexHistone deacetylase 1Homo sapiens (human)
chromatinHistone deacetylase 1Homo sapiens (human)
heterochromatinHistone deacetylase 1Homo sapiens (human)
transcription repressor complexHistone deacetylase 1Homo sapiens (human)
protein-containing complexHistone deacetylase 1Homo sapiens (human)
nucleusHistone deacetylase 1Homo sapiens (human)
nuclear chromosomeHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleoplasmHistone deacetylase 8Homo sapiens (human)
cytoplasmHistone deacetylase 8Homo sapiens (human)
histone deacetylase complexHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 8Homo sapiens (human)
nucleusHistone deacetylase 6Homo sapiens (human)
nucleoplasmHistone deacetylase 6Homo sapiens (human)
cytoplasmHistone deacetylase 6Homo sapiens (human)
multivesicular bodyHistone deacetylase 6Homo sapiens (human)
centrosomeHistone deacetylase 6Homo sapiens (human)
cytosolHistone deacetylase 6Homo sapiens (human)
microtubuleHistone deacetylase 6Homo sapiens (human)
caveolaHistone deacetylase 6Homo sapiens (human)
inclusion bodyHistone deacetylase 6Homo sapiens (human)
aggresomeHistone deacetylase 6Homo sapiens (human)
axonHistone deacetylase 6Homo sapiens (human)
dendriteHistone deacetylase 6Homo sapiens (human)
cell leading edgeHistone deacetylase 6Homo sapiens (human)
ciliary basal bodyHistone deacetylase 6Homo sapiens (human)
perikaryonHistone deacetylase 6Homo sapiens (human)
perinuclear region of cytoplasmHistone deacetylase 6Homo sapiens (human)
axon cytoplasmHistone deacetylase 6Homo sapiens (human)
histone deacetylase complexHistone deacetylase 6Homo sapiens (human)
microtubule associated complexHistone deacetylase 6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (130)

Assay IDTitleYearJournalArticle
AID715990Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in RBC count at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1699970Antiproliferative activity against human K562/A02 cells overexpressing P-gp by MTT assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID716228Inhibition to 59Fe uptake from 59Fe-transferrin in human SK-N-MC cells at 25 uM after 3 hrs2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1501300Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID716220Antiproliferative activity at human A549 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1626658Cytotoxicity against human A2780 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID303516Effect on iron efflux in human SK-N-MC cells assessed as cellular iron release2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and characterization of new iron chelators with anti-proliferative activity: structure-activity relationships of novel thiohydrazone analogues.
AID439767Antitumor activity against human SK-MEL-28 cells implanted in nude mouse assessed as reduction in tumor growth at 0.4 mg/kg/day measured up to 7 weeks relative to control2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID370489Reduction of cellular iron uptake from 59Fe]transferrin in human SK-N-MC cells at 25 uM after 3 hrs relative to control2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
2-Acetylpyridine thiosemicarbazones are potent iron chelators and antiproliferative agents: redox activity, iron complexation and characterization of their antitumor activity.
AID1550741Antiproliferative activity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID439768Octanol-water partition coefficient, log P of the compound2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID271691Antiproliferative activity against human SK-N-MC cells after 96 hrs by MTT assay2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Dipyridyl thiosemicarbazone chelators with potent and selective antitumor activity form iron complexes with redox activity.
AID1626663Cytotoxicity against human KBC1 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID715975Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in WBC count at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID716219Antiproliferative activity at human MRC5 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID716003Toxicity in human DMS53 cells xenografted BALB/c nu/nu mouse assessed as body weight change at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID671699Potentiation of theophylline transdermal permeation in pig ear skin assessed as enhancement ratio at 20 mg after 24 hrs by Franz diffusion cell method2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Investigation of substituted 6-aminohexanoates as skin penetration enhancers.
AID1319028Induction of ROS accumulation in human KBV1 cells over expressing P-gp at 10 uM after 30 mins by DCF-DA staining based flow cytometry2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID677923Antiproliferative activity against human HCT116 cells expressing p53 assessed as cell survival at 5 nM after 9 days by clonogenic assay relative to control2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID722572Induction of 59Fe efflux in human SK-N-MC cells prelabeled with 59Fe2-Tf at 25 uM after 3 hrs by gamma-scintillation counting analysis (Rvb = 5 +/- 1%)2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID370485Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
2-Acetylpyridine thiosemicarbazones are potent iron chelators and antiproliferative agents: redox activity, iron complexation and characterization of their antitumor activity.
AID677908Antiproliferative activity against human NHDF cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID1550510Cytotoxicity against human CFPAC-1 cells incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, May-15, Volume: 170Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues.
AID716229Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as cardiac fibrosis at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1319033Induction of P-gp-mediated lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as increase in LAMP2 fluorescence at 10 uM after 24 hrs in presence of P-gp inhibitor elacridar by TexasRed staining based immunofluorescence 2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID1626661Resistance factor, ratio of IC50 for triapine-resistant human SW480 cells to IC50 for human SW480 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID715985Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in hemoglobin level at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID370490Induction of iron removal from 59Fe]transferrin assessed as iron release after 3 hrs relative to control2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
2-Acetylpyridine thiosemicarbazones are potent iron chelators and antiproliferative agents: redox activity, iron complexation and characterization of their antitumor activity.
AID715743Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as hepatocellular fibrosis at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1550747Selectivity index, ratio of IC50 for human NHDF cells to IC50 for human HCT116 cells expressing wild type p532019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID271700Increase in Fe(2+)-mediated hydroxyl radical production measured as hydroxylation of benzoate at IBE of 3 relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Dipyridyl thiosemicarbazone chelators with potent and selective antitumor activity form iron complexes with redox activity.
AID370487Induction of iron mobilization in 59Fe]transferrin labeled human SK-N-MC cells assessed as iron release at 25 uM after 3 hrs by gamma scintillation counter2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
2-Acetylpyridine thiosemicarbazones are potent iron chelators and antiproliferative agents: redox activity, iron complexation and characterization of their antitumor activity.
AID539493Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Investigating the activity of 2-substituted alkyl-6-(2,5-dioxopyrrolidin-1-yl)hexanoates as skin penetration enhancers.
AID1501301Binding affinity to 59Fe2+ in human SK-N-MC cells labeled with 59Fe2-transferrin assessed as Fe release at 25 uM after 3 hrs by gamma scintillation counting method relative to total cellular 59Fe2+ (Rvb = 6%)2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID716222Induction of 59Fe mobilization in human SK-N-MC cells at 25 uM after 3 hrs by gamma-scintillation counter2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID271694Increase in Fe(3+)-mediated ascorbate oxidation at IBE of 1 relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Dipyridyl thiosemicarbazone chelators with potent and selective antitumor activity form iron complexes with redox activity.
AID411003Partition coefficient, log P of the compound2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Iron chelators of the dipyridylketone thiosemicarbazone class: precomplexation and transmetalation effects on anticancer activity.
AID715996Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in organ weight at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1501308Metal chelating activity assessed as inhibition of Cu2+ mediated amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 2 hrs by turbidity assay2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID1550745Antiproliferative activity against human Hs683 cells incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID619952Toxicity in human SK-N-MC cells assessed as cell viability after 3 hrs by trypan blue staining2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Halogenated 2'-benzoylpyridine thiosemicarbazone (XBpT) chelators with potent and selective anti-neoplastic activity: relationship to intracellular redox activity.
AID1319044Induction of oxidative stress-dependent lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as decrease in cathepsin D and LAMP2 lysosomal colocalization at 10 uM after 24 hrs in presence of antioxidant N-acetyl-L-cystein2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID439770Effect on iron metabolism in human SK-N-MC cells assessed as cellular iron uptake from transferrin at 25 uM after 3 hrs in presence of pronase relative to control2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID715747Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as hepatocellular necrosis at 3 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID722571Reduction of cellular 59Fe uptake from 59Fe-Transferrin in human SK-N-MC cells assessed as 59Fe level prelabeled with 59Fe2-Tf at 25 uM after 3 hrs relative to control2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID370486Octanol-water partition coefficient, log P of the compound2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
2-Acetylpyridine thiosemicarbazones are potent iron chelators and antiproliferative agents: redox activity, iron complexation and characterization of their antitumor activity.
AID292406Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Design, synthesis, and characterization of novel iron chelators: structure-activity relationships of the 2-benzoylpyridine thiosemicarbazone series and their 3-nitrobenzoyl analogues as potent antitumor agents.
AID271695Increase in Fe(3+)-mediated ascorbate oxidation at IBE of 3 relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Dipyridyl thiosemicarbazone chelators with potent and selective antitumor activity form iron complexes with redox activity.
AID1319030Induction of P-gp-mediated lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as cathepsin D release from lysosome to cytosol at 10 uM after 24 hrs by TexasRed staining based immunofluorescence microscopic analysis2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID735438Antiproliferative activity against human SK-N-MC cells measured after 72 hrs at 37 degC by MTT assay2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
Synthesis and biological evaluation of substituted 2-benzoylpyridine thiosemicarbazones: novel structure-activity relationships underpinning their anti-proliferative and chelation efficacy.
AID1319023Substrate activity at P-gp (unknown origin) in P-gp enriched membranes assessed as increase in ATPase activity at 50 uM in presence of Mg2-ATP after 40 mins by luciferase reporter gen assay relative to control2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID1699973Inhibition of recombinant human HDAC6 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1319042Induction of oxidative stress-dependent lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as decrease in cathepsin D and LAMP2 lysosomal colocalization at 10 uM after 24 hrs by TexasRed staining based immunofluorescence2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID619948Induction of Fe efflux in human SK-N-MC cells assessed as release of intracellular 59Fe up to 25 uM after 3 hrs by gamma-scintillation counting2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Halogenated 2'-benzoylpyridine thiosemicarbazone (XBpT) chelators with potent and selective anti-neoplastic activity: relationship to intracellular redox activity.
AID1550783Binding affinity to calf thymus DNA assessed as hypochromism incubated for 1.5 hrs by spectrophotometric method2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID1550748Selectivity index, ratio of IC50 for human NHDF cells to IC50 for human HCT116 cells deficient in p532019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID439769Iron chelating activity in human SK-N-MC cells assessed as cellular iron efflux at 25 uM after 3 hrs relative to control2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID677922Antiproliferative activity against human HCT116 cells expressing p53 assessed as cell survival at 1 nM after 9 days by clonogenic assay relative to control2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID439764Toxicity in iv dosed CD2F1 hybrid mouse assessed as maximum tolerated dose administered BID at an interval of 6 hrs for 5 days a week over 2 weeks2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID1626659Cytotoxicity against human SW480 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID715748Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as hepatocellular necrosis at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID460409Toxicity in MDCK cells by MTT method2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID1550749Selectivity index, ratio of IC50 for human NHDF cells to IC50 for human MCF7 cells2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID715733Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in lungs histology at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1550751Selectivity index, ratio of IC50 for human NHDF cells to IC50 for human Hs683 cells2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID671697Lipophilicity, log K of the compound by RP-HPLC analysis2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Investigation of substituted 6-aminohexanoates as skin penetration enhancers.
AID1699974Inhibition of recombinant human HDAC8 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1626660Cytotoxicity against triapine-resistant human SW480 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID722575Cytotoxicity against human SK-N-MC cells assessed as growth inhibition after 72 hrs by MTT assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID1626664Resistance factor, ratio of IC50 for human KBC1 cells to IC50 for human KB-3-1 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID411004Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay2009Journal of medicinal chemistry, Jan-22, Volume: 52, Issue:2
Iron chelators of the dipyridylketone thiosemicarbazone class: precomplexation and transmetalation effects on anticancer activity.
AID619945Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTS assay2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Halogenated 2'-benzoylpyridine thiosemicarbazone (XBpT) chelators with potent and selective anti-neoplastic activity: relationship to intracellular redox activity.
AID1319019Antiproliferative activity against human KB3-1 cells after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID439762Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID1550746Antiproliferative activity against human NHDF cells incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID303517Inhibition of cellular iron uptake from 59Fe]transferrin in human SK-N-MC cells at 50 uM relative to control2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and characterization of new iron chelators with anti-proliferative activity: structure-activity relationships of novel thiohydrazone analogues.
AID677924Antiproliferative activity against human HCT116 cells expressing p53 assessed as cell survival at 0.5 nM after 9 days by clonogenic assay relative to control2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID716214Antitumor activity against human DMS53 cells xenografted BALB/c nu/nu mouse assessed as reduction of tumor volume at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days (RVb = 922 94 mm'3)2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1626662Cytotoxicity against human KB-3-1 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID292410Partition coefficient, log P of the compound2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Design, synthesis, and characterization of novel iron chelators: structure-activity relationships of the 2-benzoylpyridine thiosemicarbazone series and their 3-nitrobenzoyl analogues as potent antitumor agents.
AID1550744Antiproliferative activity against human U251 cells incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID677905Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID715738Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in brain histology at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID722565Toxicity in intact human RBC assessed as methemoglobin formation at 25 uM after 3 hrs relative to untreated control2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID1319032Induction of P-gp-mediated lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as cathepsin D release from lysosome to cytosol at 10 uM after 24 hrs in presence of P-gp inhibitor elacridar by TexasRed staining based immun2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID1501306Induction of autophagy in human SK-N-MC cells assessed as decrease in p62 level at 25 uM after 24 hrs by Western blot analysis2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID271690Partition coefficient, log P of the compound2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Dipyridyl thiosemicarbazone chelators with potent and selective antitumor activity form iron complexes with redox activity.
AID1319038Induction of copper-dependent lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as decrease in cathepsin D and LAMP2 lysosomal colocalization at 10 uM after 24 hrs by TexasRed staining based immunofluorescence microscop2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID1550742Antiproliferative activity against human HCT116 cells deficient in p53 incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID1319021Antiproliferative activity against human KBV1 cells over expressing P-gp after 24 hrs in presence of P-gp inhibitor elacridar by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID1626665Cytotoxicity against human WI38 cells incubated for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID1550743Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTS assay2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID715970Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in platelet count at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID722570Induction of ascorbate oxidation in citrate buffer in presence of 10 uM Fe3+ at 1 to 60 uM2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID715753Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as vacuolation at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID722568Toxicity in human RBC lysates assessed as methemoglobin formation at 25 uM after 3 hrs (Rvb = 1.2 +/- 8%)2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID1319031Induction of P-gp-mediated lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as increase in LAMP2 fluorescence at 10 uM after 24 hrs by TexasRed staining based immunofluorescence microscopic analysis2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID439765Antitumor activity against mouse M109 cells implanted in CD2F1 hybrid mouse assessed as reduction of tumor weight at 0.4 mg/kg, iv administered 4 days after implantation BID for 5 days measured on day 12 after implantation relative to control2009Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
Thiosemicarbazones from the old to new: iron chelators that are more than just ribonucleotide reductase inhibitors.
AID1699972Inhibition of recombinant human HDAC1 using Boc-Lys(Ac)-AMC as substrate incubated for 60 mins by fluorimetric assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID1699971Resistance index, ratio of of IC50 for human K562/A02 cells to IC50 for human K562 cells2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID619949Inhibition of 59Fe uptake from transferrin in human SK-N-MC cells at 25 uM after 3 hrs relative to control2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Halogenated 2'-benzoylpyridine thiosemicarbazone (XBpT) chelators with potent and selective anti-neoplastic activity: relationship to intracellular redox activity.
AID460410Toxicity in human SK-N-MC cells by MTT method2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID671698Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Investigation of substituted 6-aminohexanoates as skin penetration enhancers.
AID1501307Induction of autophagy in human SK-N-MC cells assessed as increase in LC3 accumulation at 25 uM after 24 hrs in presence of autophagy inhibitor Baf1 by Western blot analysis2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID1319040Induction of copper-dependent lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp assessed as decrease in cathepsin D and LAMP2 lysosomal colocalization at 10 uM after 24 hrs in presence of Cu chelator tetrathiomolybdate by TexasR2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID1550508Cytotoxicity against human PANC1 cells incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, May-15, Volume: 170Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues.
AID1626669Cytotoxicity against human A2780 cells pre-incubated with CuCl2 for 60 mins followed by compound addition for for 72 hrs by MTT assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Impact of Stepwise NH2-Methylation of Triapine on the Physicochemical Properties, Anticancer Activity, and Resistance Circumvention.
AID619944Anticancer activity against mouse M109 cells xenografted in iv dosed CD2F1 mouse assessed as reduction in tumor growth after 5 days2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Halogenated 2'-benzoylpyridine thiosemicarbazone (XBpT) chelators with potent and selective anti-neoplastic activity: relationship to intracellular redox activity.
AID715960Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in hematopoetic cells in splenic red pulp at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days by hematoxylin and eosin staining method2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID715965Cardiotoxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID716225Antiproliferative activity at human SK-N-MC cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID735441Inhibition of cellular iron uptake in human SK-N-MC cells assessed as iron uptake at 25 uM for 3 hrs at 37 degC relative to control2013Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4
Synthesis and biological evaluation of substituted 2-benzoylpyridine thiosemicarbazones: novel structure-activity relationships underpinning their anti-proliferative and chelation efficacy.
AID722566Toxicity in intact human RBC assessed as methemoglobin formation using Fe(compound)2 complex at 25 uM after 3 hrs relative to untreated control2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Alkyl substituted 2'-benzoylpyridine thiosemicarbazone chelators with potent and selective anti-neoplastic activity: novel ligands that limit methemoglobin formation.
AID1319027Induction of lysosomal membrane permeabilization in human KBV1 cells over expressing P-gp at 10 uM after 30 mins by acridine orange staining based fluorescence microscopic analysis2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID312544Antiproliferative activity against human SK-MN-C cells by MTT assay2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of novel iron chelators for the treatment of iron overload disease: the methyl pyrazinylketone isonicotinoyl hydrazone series.
AID1319018Antiproliferative activity against human KB3-1 cells after 24 hrs by MTT assay2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID677907Antiproliferative activity against human HCT116 cells expressing p53 after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID715980Toxicity in BALB/c nu/nu mouse xenografted with human DMS53 cells assessed as change in reticulocyte count at 0.75 mg/kg, iv administered for 5 days a week measured after 21 days2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1501299Metal chelating activity assessed as inhibition of Cu2+ mediated human amyloid beta (1 to 40) aggregation at 25 uM after 2 hrs by turbidity assay2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID677906Antiproliferative activity against p53-deficient human HCT116 cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
AID1699969Antiproliferative activity against human K562 cells by MTT assay2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.
AID271693Increase in Fe(3+)-mediated ascorbate oxidation at IBE of 0.1 relative to control2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
Dipyridyl thiosemicarbazone chelators with potent and selective antitumor activity form iron complexes with redox activity.
AID460413Inhibition of [59Fe] uptake from [59Fe]transferrin in human SK-N-MC cells assessed as at 50 uM after 3 hrs relative to untreated control2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Conjugates of desferrioxamine B (DFOB) with derivatives of adamantane or with orally available chelators as potential agents for treating iron overload.
AID1501302Inhibition of 59Fe2+ uptake from transferrin in human SK-N-MC cells labeled with 59Fe2-Tf assessed as 59Fe uptake level at 25 uM after 3 hrs by gamma scintillation counting method relative to untreated control2017European journal of medicinal chemistry, Oct-20, Volume: 139A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease.
AID1550507Cytotoxicity against human MIAPaCa2 cells incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, May-15, Volume: 170Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues.
AID1319026Induction of lysosomal membrane permeabilization in human KB3-1 cells at 10 uM after 30 mins by acridine orange staining based fluorescence microscopic analysis2016Journal of medicinal chemistry, Sep-22, Volume: 59, Issue:18
Structure-Activity Relationships of Di-2-pyridylketone, 2-Benzoylpyridine, and 2-Acetylpyridine Thiosemicarbazones for Overcoming Pgp-Mediated Drug Resistance.
AID716221Antiproliferative activity at human DMS53 cells after 72 hrs by MTT assay2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Novel second-generation di-2-pyridylketone thiosemicarbazones show synergism with standard chemotherapeutics and demonstrate potent activity against lung cancer xenografts after oral and intravenous administration in vivo.
AID1550750Selectivity index, ratio of IC50 for human NHDF cells to IC50 for human U251 cells2019European journal of medicinal chemistry, Jun-01, Volume: 171Anticancer activity of the thiosemicarbazones that are based on di-2-pyridine ketone and quinoline moiety.
AID1550509Cytotoxicity against human Capan2 cells incubated for 24 hrs by MTT assay2019European journal of medicinal chemistry, May-15, Volume: 170Multi-target compounds acting in cancer progression: Focus on thiosemicarbazone, thiazole and thiazolidinone analogues.
AID303514Antiproliferative activity against human SK-N-MC cells by MTT assay2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Design, synthesis, and characterization of new iron chelators with anti-proliferative activity: structure-activity relationships of novel thiohydrazone analogues.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (33.33)29.6817
2010's13 (61.90)24.3611
2020's1 (4.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.50

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.50 (24.57)
Research Supply Index3.09 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (9.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (90.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]