Page last updated: 2024-09-27

piplartine

Description

piplartine: Antineoplastic Agent, Phytogenic; alkaloid from Piper; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID637858
CHEMBL ID465843
CHEBI ID8241
CHEBI ID92424
SCHEMBL ID173092
SCHEMBL ID2465593
MeSH IDM0457216

Synonyms (82)

Synonym
sgd66v4svj ,
2(1h)-pyridinone, 5,6-dihydro-1-(1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl)-, (e)-
unii-sgd66v4svj
LS-14579
smr001233252
MLS002153903
brd2293
BRD-K24132293-001-05-3
brd-2293
BRD-K24132293-001-16-0
PRESTWICK2_000604
PRESTWICK_399
PRESTWICK3_000604
ACON1_001541
BSPBIO_000508
BPBIO1_000560
1-[3-(3,4,5-trimethoxy-phenyl)-acryloyl]-5,6-dihydro-1h-pyridin-2-one
20069-09-4
piperlongumine
piplartine
NCGC00096028-01
SPECTRUM1505135
NCGC00096028-02
NCGC00096028-03
CHEMBL465843
chebi:8241 ,
HMS1569J10
1-[(e)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one
NCGC00096028-04
HMS2096J10
ST079382
HMS2234K24
BRD-K24132293-001-09-5
5,6-dihydro-1-[(2e)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propen-1-yl]-2(1h)-pyridinone
S7551
piperlongumine [mi]
piperlongumine [inci]
2(1h)-pyridinone, 5,6-dihydro-1-(1-oxo-3-(3,4,5-trimethoxyphenyl)-2- propenyl)-, (e)-
CCG-214375
SCHEMBL173092
SCHEMBL2465593
AKOS024284776
(e)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1h)-one
A1-00162
1-[(2e)-3-(3,4,5-trimethoxyphenyl)-2-propenoyl]-5,6-dihydro-2(1h)-pyridinone #
prop-2-en-1-one, 3-(3,4,5-trimethoxyphenyl)-1-(2,3-dihydropyridin-6(1h)-one-1-yl)-
AC-32683
1-[(2e)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-1,2,5,6-tetrahydropyridin-2-one
sr-01000841248
SR-01000841248-2
CHEBI:92424
AS-74140
piperlongumine, >=97% (hplc)
J-012992
5,6-dihydro-1-(3,4,5-trimethoxycinnamoyl)-2(1h)-pyridinone
n-(3,4,5-trimethoxycinnamoyl)-d3-piperidin-2-one
5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propenyl]-2(1h)-pyridinone, 9ci
CS-0021113
HY-N2329
2(1h)-pyridinone, 5,6-dihydro-1-[(2e)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propen-1-yl]-
pplgm
(e)-1-[3-(3,4,5-trimethoxyphenyl)acryloyl]-5,6-dihydropyridin-2(1h)-one
P2361
5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl)-trans-2-propenyl]-2(1h)-pyridinone
BCP13030
piplartine;pplgm
piperlongumine; piplartine
EX-A2925
Q7197361
A14124
NCGC00096028-14
nsc794671
nsc-794671
ferrousfluoborate
5,6-dihydro-1-[1-oxo-3-(3,4,5-trimethoxyphenyl)-allyl]-2(1h)-pyridinone
A920539
bdbm50462013
1-[(2e)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-5,6-dihydropyridin-2(1h)-one
BP-25401
DTXSID801029762
1-[(2e)-3-(3,4,5-trimethoxyphenyl)-2-propenoyl]-5,6-dihydro-2(1h)-pyridinone
EN300-7424497

Research Excerpts

Overview

ExcerptReference
"Piplartine is an alkamide found in certain species of the genus"( da Fonseca, ACC; de Sousa, DP; Machado, TQ; Perez-Castillo, Y; Robbs, BK; Silva, RHN; Tejera, E, 2023)
"Piplartine (PL) is a biologically active alkaloid from long peppers that exhibits anti-inflammatory and antitumor activity."( Barbosa-Filho, JM; Bezerra, DP; Contessoto, NSA; Cornélio, ML; da Silveira, NJF; Girol, AP; Henrique, T; Oliani, SM; Silveira, ER; Stefanini, ACB; Tajara, EH; Zanon, CF, 2020)
"Piplartine (PL) is an alkaloid found in black-pepper and known for its anticancer activity, however, due to poor solubility and lack of proper formulation, its use for oral administration is a challenge. "( Fofaria, NM; Liu, X; Qhattal, HS; Srivastava, SK, 2016)
"Piplartine showed to be a more reactive substrate towards the catalysts tested."( Crotti, AE; Iamamoto, Y; Kato, MJ; Lopes, NP; Lotufo, LV; Schaab, EH, 2010)

Treatment

ExcerptReference
"Piplartine treatment induced DNA strand breaks in V79 cells, as detected by neutral and alkaline comet assay."( Bezerra, DP; Costa-Lotufo, LV; de Moraes, MO; de Vasconcellos, MC; e Silva, AC; Henriques, JA; Lima, MA; Moura, DJ; Rosa, RM; Saffi, J; Silveira, ER, 2008)

Drug Classes (2)

ClassDescription
cinnamamidesAn enamide which is cinnamamide or a derivative of cinnamamide obtained by replacement of one or more of its hydrogens.
dicarboximideAn imide in which the two acyl substituents on nitrogen are carboacyl groups.
[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 (51)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency3.98110.044717.8581100.0000AID485294
Chain A, HADH2 proteinHomo sapiens (human)Potency19.95260.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency19.95260.025120.237639.8107AID893
Nrf2Homo sapiens (human)Potency2.51190.09208.222223.1093AID624171
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency9.07940.004110.890331.5287AID504466; AID504467
TDP1 proteinHomo sapiens (human)Potency2.64940.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency9.45630.180013.557439.8107AID1460; AID1468
Smad3Homo sapiens (human)Potency14.12540.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency10.00000.011212.4002100.0000AID1030
67.9K proteinVaccinia virusPotency28.18380.00018.4406100.0000AID720580
IDH1Homo sapiens (human)Potency5.80480.005210.865235.4813AID686970
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency6.30960.01262.451825.0177AID485313
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency14.14060.316212.443531.6228AID902; AID924
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency29.09290.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency25.11893.548119.542744.6684AID743266
mitogen-activated protein kinase 1Homo sapiens (human)Potency25.11890.039816.784239.8107AID995
ras-related protein Rab-9AHomo sapiens (human)Potency6.30960.00022.621531.4954AID485297
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency39.81070.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency1.00000.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency1.00000.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency1.00000.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency5.74570.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency5.21910.004611.374133.4983AID624296; AID624297
survival motor neuron protein isoform dHomo sapiens (human)Potency35.48130.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency0.05010.031610.279239.8107AID884; AID885
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency5.01190.058010.694926.6086AID602310
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Integrin beta-3Homo sapiens (human)Potency3.16230.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency3.16230.316211.415731.6228AID924
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
TAR DNA-binding protein 43Homo sapiens (human)Potency22.38721.778316.208135.4813AID652104
GABA theta subunitRattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency0.05011.000012.224831.6228AID885
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Signal transducer and activator of transcription 3Homo sapiens (human)IC50 (µMol)7.00000.02304.13789.9800AID1392927
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)IC50 (µMol)23.84000.04322.26555.0000AID1564516; AID1677566
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PAX8Homo sapiens (human)AC5031.61000.04885.435469.1700AID687027; AID687029
Microphthalmia-associated transcription factorHomo sapiens (human)AC507.40300.015010.904946.0480AID493073; AID493102; AID493177
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (163)

Processvia Protein(s)Taxonomy
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
temperature homeostasisSignal transducer and activator of transcription 3Homo sapiens (human)
eye photoreceptor cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of DNA-templated transcriptionSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
protein import into nucleusSignal transducer and activator of transcription 3Homo sapiens (human)
inflammatory responseSignal transducer and activator of transcription 3Homo sapiens (human)
signal transductionSignal transducer and activator of transcription 3Homo sapiens (human)
transforming growth factor beta receptor signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATSignal transducer and activator of transcription 3Homo sapiens (human)
nervous system developmentSignal transducer and activator of transcription 3Homo sapiens (human)
cell population proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of cell population proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of autophagySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of gene expressionSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of gene expressionSignal transducer and activator of transcription 3Homo sapiens (human)
phosphorylationSignal transducer and activator of transcription 3Homo sapiens (human)
cytokine-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
sexual reproductionSignal transducer and activator of transcription 3Homo sapiens (human)
cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of cell migrationSignal transducer and activator of transcription 3Homo sapiens (human)
intracellular receptor signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
response to estradiolSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-1 beta productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-10 productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-6 productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of interleukin-8 productionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of tumor necrosis factor productionSignal transducer and activator of transcription 3Homo sapiens (human)
cellular response to hormone stimulusSignal transducer and activator of transcription 3Homo sapiens (human)
leptin-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
somatic stem cell population maintenanceSignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-15-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-2-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-9-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-11-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
regulation of multicellular organism growthSignal transducer and activator of transcription 3Homo sapiens (human)
glucose homeostasisSignal transducer and activator of transcription 3Homo sapiens (human)
eating behaviorSignal transducer and activator of transcription 3Homo sapiens (human)
mRNA transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionSignal transducer and activator of transcription 3Homo sapiens (human)
cellular response to leptin stimulusSignal transducer and activator of transcription 3Homo sapiens (human)
response to leptinSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of erythrocyte differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of Notch signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of angiogenesisSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of glycolytic processSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of DNA-templated transcriptionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISignal transducer and activator of transcription 3Homo sapiens (human)
astrocyte differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of inflammatory responseSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activitySignal transducer and activator of transcription 3Homo sapiens (human)
regulation of cell cycleSignal transducer and activator of transcription 3Homo sapiens (human)
radial glial cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
retinal rod cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of feeding behaviorSignal transducer and activator of transcription 3Homo sapiens (human)
growth hormone receptor signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATSignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-6-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
T-helper 17 type immune responseSignal transducer and activator of transcription 3Homo sapiens (human)
T-helper 17 cell lineage commitmentSignal transducer and activator of transcription 3Homo sapiens (human)
energy homeostasisSignal transducer and activator of transcription 3Homo sapiens (human)
cellular response to interleukin-17Signal transducer and activator of transcription 3Homo sapiens (human)
cell surface receptor signaling pathway via STATSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of inflammatory response to woundingSignal transducer and activator of transcription 3Homo sapiens (human)
interleukin-10-mediated signaling pathwaySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of miRNA transcriptionSignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of metalloendopeptidase activitySignal transducer and activator of transcription 3Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of primary miRNA processingSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of stem cell differentiationSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of neuron migrationSignal transducer and activator of transcription 3Homo sapiens (human)
regulation of cell population proliferationSignal transducer and activator of transcription 3Homo sapiens (human)
response to peptide hormoneSignal transducer and activator of transcription 3Homo sapiens (human)
defense responseSignal transducer and activator of transcription 3Homo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
mesoderm formationThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
signal transductionThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
cell population proliferationThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
cellular oxidant detoxificationThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
cell redox homeostasisThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
transcription cis-regulatory region bindingSignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificSignal transducer and activator of transcription 3Homo sapiens (human)
DNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription factor activitySignal transducer and activator of transcription 3Homo sapiens (human)
nuclear receptor activitySignal transducer and activator of transcription 3Homo sapiens (human)
signaling receptor bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein kinase bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein phosphatase bindingSignal transducer and activator of transcription 3Homo sapiens (human)
chromatin DNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
signaling adaptor activitySignal transducer and activator of transcription 3Homo sapiens (human)
identical protein bindingSignal transducer and activator of transcription 3Homo sapiens (human)
protein homodimerization activitySignal transducer and activator of transcription 3Homo sapiens (human)
protein dimerization activitySignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingSignal transducer and activator of transcription 3Homo sapiens (human)
primary miRNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
lncRNA bindingSignal transducer and activator of transcription 3Homo sapiens (human)
DNA-binding transcription factor bindingSignal transducer and activator of transcription 3Homo sapiens (human)
RNA sequestering activitySignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
thioredoxin-disulfide reductase (NADPH) activityThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
protein bindingThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
identical protein bindingThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
NADPH peroxidase activityThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
FAD bindingThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (42)

Processvia Protein(s)Taxonomy
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleusSignal transducer and activator of transcription 3Homo sapiens (human)
nucleusSignal transducer and activator of transcription 3Homo sapiens (human)
nucleoplasmSignal transducer and activator of transcription 3Homo sapiens (human)
cytoplasmSignal transducer and activator of transcription 3Homo sapiens (human)
cytosolSignal transducer and activator of transcription 3Homo sapiens (human)
plasma membraneSignal transducer and activator of transcription 3Homo sapiens (human)
RNA polymerase II transcription regulator complexSignal transducer and activator of transcription 3Homo sapiens (human)
chromatinSignal transducer and activator of transcription 3Homo sapiens (human)
transcription regulator complexSignal transducer and activator of transcription 3Homo sapiens (human)
cytoplasmSignal transducer and activator of transcription 3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
fibrillar centerThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
nucleoplasmThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
cytosolThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
extracellular exosomeThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
mitochondrionThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
cytosolThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
cytoplasmThioredoxin reductase 1, cytoplasmicHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (302)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1741898Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c nude mouse assessed as reduction in tumor weight at 10 mg/kg, ip measured at 2 days interval for 21 days relative to control2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1430073Lipophilicity, log D of compound at pH 7.42017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1564517Inhibition of rat TrxR1 using DTNB as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by Ellman's method2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1741863Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1392921Growth inhibition of human DU145 cells after 48 hrs by WST-1 assay2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1433268Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1455312Cytotoxicity against human HCT116 cells at 2 to 50 nM after 24 to 48 hrs in presence of TGF-beta1 by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1392923Growth inhibition of human LNCAP cells after 48 hrs by WST-1 assay2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1741864Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1433254Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1392946Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 3 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1474919Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1173277Cytotoxicity against mouse RAW264.7 cells assessed as cell proliferation at 10 uM2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
AID1206053Induction of ROS production in human A549 cells after 3 hrs by APF staining-based fluorescence assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1158951Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1677560Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1396583Toxicity in po dosed mouse2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
AID1474915Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1459286Induction of bovine tubulin depolymerization at 25 uM measured every 30 secs for 60 mins by spectrophotometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1392947Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 7 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1455335Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455310Antimigratory activity in human HCT116 cells assessed as inhibition of TGF-beta1-induced cell migration at 50 nM after 48 hrs by trans-well assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1564518Inhibition of TrxR1 (unknown origin) using DTNB as substrate preincubated for 30 mins in presence of insulin followed by substrate addition by colorimetry2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1564522Cytotoxicity against human PBMC assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1433260Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1206058Reduction in reduced GSH level in human A549 cells at 10 uM after 4 hrs by luminescence assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1377676Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1426165Inhibition of equine liver GST assessed as decrease in conjugation of CDNB to GSH at 100 uM preincubated with GSH for 30 mins followed by CDNB addition measured for 3 mins relative to control2017European journal of medicinal chemistry, Jan-27, Volume: 126Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy.
AID1455323Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1168752Selectivity ratio of IC50 for human HaCaT cells to IC50 for human PANC1 cells2014European journal of medicinal chemistry, Nov-24, Volume: 87A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness.
AID1741881Induction of autophagy in human MDA-MB-231 cells transfected with mRFP-eGFP-LC3 assessed as accumulation of autophagosomes by measuring increase in red fluorescence at 1.8 uM measured after 24 hrs by confocal laser scanning microscopy2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1392949Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 3 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1229943Cytotoxicity against rat PC12 cells assessed as reduction in cell viability at 20 uM to 100 uM incubated for 24 hrs by MTT assay2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Synthesis of piperlongumine analogues and discovery of nuclear factor erythroid 2-related factor 2 (Nrf2) activators as potential neuroprotective agents.
AID1433250Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433233Induction of apoptosis in p53 null human U937 cells assessed as PARP-1 cleavage at 2 uM after 24 hrs in presence of SAHA by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1677584Inhibition of mTOR phosphorylation in human BEL-7402/5-FU cells at 2 uM incubated for 72 hrs by Western blot analysis
AID1677557Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1206041Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1433306Effect on SAHA-induced apoptosis in p53 null human U937 cells assessed as decrease in XIAP expression level by measuring ratio of XIAP to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1206045Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1455321Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1459266Induction of apoptosis in human MCF7 cells assessed as downregulation of Bcl2 expression at 10 uM after 48 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1474938Induction of apoptosis in human HCT116 cells after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1433256Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1392948Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 10 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1551745Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 48 hrs by MTT assay2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1455345Induction of ROS accumulation in human HCT116 cells at 10 uM after 3 hrs by DCFH-DA staining-based fluorescence microscopic analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455316Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered daily for 21 consecutive days relative to control2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433247Induction of apoptosis in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant at 1 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1455339Cmax in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433234Induction of cell death in p53 null human U937 cells at 1 to 4 uM after 24 hrs by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1173275Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
AID1433236Induction of cell death in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant assessed as combination index at 1 to 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1392950Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 7 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1433296Induction of DNA damage in p53 null human U937 cells assessed as increase in gammaH2AX expression level by measuring ratio of gammaH2AX to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1392925Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells by Western blot analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1474920Antiproliferative activity against human Saos2 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1392931Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 5 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1455367Inhibition of IL-1beta-mediated adhesion of human rhodamine 123-labeled HCT116 cells to HUVEC at 50 nM after 1 hr by fluoresence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433232Induction of apoptosis in p53 null human U937 cells assessed as caspase 3 cleavage at 2 uM after 24 hrs in presence of SAHA by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433244Induction of apoptosis in p53 null human U937 cells at 1 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433305Effect on SAHA-induced apoptosis in p53 null human U937 cells assessed as increase in Bim EL expression level by measuring ratio of Bim EL to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433301Induction of DNA damage in p53 null human U937 cells assessed as decrease in CHK1 expression level by measuring ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1677566Inhibition of TrxR in human BEL-7402/5-FU cells by colorimetric assay
AID1455377Inhibition of TGF-beta1-induced increase in expression levels of vimentin protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455328Antiproliferative activity against human K562 cells after 72 hrs in presence of ligustrazine by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1276122Cytotoxicity against human SF188 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1551762Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation at 150 uM preincubated for 3 mins followed by collagen addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1276118Cytotoxicity against human T98G cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1455346Induction of ROS accumulation in human CCD-841 cells at 10 uM after 3 hrs by DCFH-DA staining-based fluorescence microscopic analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1426174Electrophilicity of the compound assessed as second-oder rate constant for reaction with cysteamine under pseudo-first-oder condition at 40 uM by spectrophotometric method2017European journal of medicinal chemistry, Jan-27, Volume: 126Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy.
AID1433269Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433270Inhibition of HDAC in p53 null human U937 cells assessed as hyper acetylation of histone H4 at 1 uM after 4 hrs by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459275Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 20 uM after 24 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1551764Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of PAF-induced platelet aggregation at 150 uM preincubated for 3 mins followed by PAF addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1551755Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida albicans ATCC 102312019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1433287Cytotoxicity against p53 null human U937 cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1158950Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1174985Cytotoxicity against human MA9.3 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design of a hydrogen peroxide-activatable agent that specifically targets cancer cells.
AID1433266Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459305Effect on tubulin polymerization in human MCF7 cells at 12017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1433297Effect on SAHA-induced DNA damage in p53 null human U937 cells assessed as increase in gammaH2AX expression level by measuring ratio of gammaH2AX to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1677583Inhibition of AKT phosphorylation in human BEL-7402/5-FU cells at 2 uM incubated for 72 hrs by Western blot analysis
AID1433304Induction of apoptosis in p53 null human U937 cells assessed as decrease in XIAP expression level by measuring ratio of XIAP to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1168750Cytotoxicity against human PANC1 cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay2014European journal of medicinal chemistry, Nov-24, Volume: 87A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness.
AID1433255Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1474931Induction of apoptosis in human Saos2 cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID336829Cytotoxicity against human A549 cells after 6 days by MTT assay
AID1551742Antifungal activity against Candida glabrata ATCC 90030 after 24 hrs by CLSI broth microdilution method2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1433299Upregulation of Rad51 protein expression in p53 null human U937 cells assessed as ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1276119Cytotoxicity against human HT1080 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1677572Induction of autophagy in human BEL-7402/5-FU cells expressing mRFP-eGFP-LC3 assessed as autophagosomes at 2 uM after 24 hrs by confocal laser scanning microscopic method
AID1677561Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1392935Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 5 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1455379Inhibition of TGF-beta1-induced increase in expression levels of snail protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433261Antiproliferative activity against human OCI-AML3 cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433262Antiproliferative activity against human CMS cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1916768Cytotoxicity against human HCT-116 incubated for 24 hrs by CCK-8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy.
AID1741868Inhibition of TrxR in human MDA-MB-231 cells measured after 72 hrs by colorimetric method2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1459280Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 5 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1459273Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 1 to 20 uM in presence of N-acetyl cysteine after 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1474941Cell cycle arrest in human HCT116 cells decrease in population at G0/G1 phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1741866Antiproliferative activity against human KB-VIN cells after 72 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1206044Antiproliferative activity against HFF1 cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1455324Antiproliferative activity against human K562 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1392934Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 1 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1741862Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1459299Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 1 to 20 uM in presence of trolox after 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1455349Antiproliferative activity against human HCT116 cells at 8 uM after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1459296Binding affinity to colchicine-binding site of beta tubulin in human HT-29 cells assessed as inhibition of formation of protein-N,N'-Ethylene-bis(iodoacetamide) adduct at 40 uM after 2 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1377679Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1741865Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1455380Inhibition of TGF-beta1-induced increase in expression levels of twist protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433263Antiproliferative activity against human CMK cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1455338Half life in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433257Antiproliferative activity against human CMY cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1229947Cytotoxicity against rat PC12 cells assessed as reduction in cell viability at 20 uM incubated for 24 hrs by MTT assay2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Synthesis of piperlongumine analogues and discovery of nuclear factor erythroid 2-related factor 2 (Nrf2) activators as potential neuroprotective agents.
AID1393006Growth inhibition of human PC3 cells after 24 to 48 hrs by WST-1 assay2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1433272Effect on SAHA-induced HDAC inhibition in p53 null human U937 cells assessed as hyper acetylation of histone H4 at 1 uM after 4 hrs by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459291Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1474933Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1158948Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1276115Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1455341Volume of distribution at steady state in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1392922Growth inhibition of human PC3 cells after 48 hrs by WST-1 assay2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1459304Induction of tubulin depolymerization in human Jurkat cells at 5 to 20 uM after 4 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1741871Induction of reactive oxygen species generation in human MDA-MB-231 cells measured after 24 hrs by DCFH-DA probe based flow cytometry2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1396584Senolytic activity against non-senescent human WI38 cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
AID1474930Induction of apoptosis in human Saos2 cells at 1 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1551760Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Staphylococcus aureus ATCC 65382019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1433285Cytotoxicity against human MCF10A cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1474935Cell cycle arrest in human Saos2 cells assessed as accumulation at S phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1474934Cell cycle arrest in human Saos2 cells assessed as accumulation at G2/M phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1396586Selectivity index, ratio of EC50 for non-senescent human WI38 cells to EC50 for ionizing radiation induced human WI38 senescent cells2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
AID1564521Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1551758Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida glabrata ATCC 900302019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1433267Antiproliferative activity against human HL60 cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459285Induction of apoptosis in human MCF7 cells assessed as downregulation of Mcl-1 expression at 10 uM after 72 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1455320Solubility of compound in phosphate buffer at pH 7.4 after 8 hrs by HPLC analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1677574Induction of autophagy in human BEL-7402/5-FU cells expressing mRFP-eGFP-LC3 assessed as auto lysosomes at 2 uM after 24 hrs by confocal laser scanning microscopic method
AID1392930Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 1 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1741886Induction of autophagy in human MDA-MB-231 cells transfected with mRFP-eGFP-LC3 assessed as increase in LC3-II expression at 1.8 uM measured after 72 hrs by Western blot analysis2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1459272Cytotoxicity in human MCF10A cells at 10 uM after 24 to 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1433271Inhibition of HDAC6 in p53 null human U937 cells assessed as hyper acetylation of alpha tubulin at 1 uM after 4 hrs by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433259Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1741874Induction of apoptosis in human MDA-MB-231 cells at 1.8 uM measured after 72 hrs by APC-Annexin V/7-AAD staining based flow cytometry relative to control2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1455336Antiproliferative activity against human CCD-841 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1158949Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1433295Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs in presence of SAHA by SYBR gold staining based alkaline comet assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459294Binding affinity to colchicine-binding site of beta tubulin in human MCF7 cells assessed as inhibition of formation of protein-N,N'-Ethylene-bis(iodoacetamide) adduct at 40 uM after 2 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1206040Antiproliferative activity against human A375 cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1168751Cytotoxicity against human HaCaT cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay2014European journal of medicinal chemistry, Nov-24, Volume: 87A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness.
AID1459274Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 20 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1433258Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1551748Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation at 300 uM preincubated for 3 mins followed by collagen addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1551759Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida parapsilosis ATCC 220192019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1430070Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1433294Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs by SYBR gold staining based alkaline comet assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433292Induction of apoptosis in p53 null human U937 cells at 2 uM preincubated with NAC for 3 hrs followed by compound addition measured after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1377681Antiproliferative activity against human A549 cells at 10 uM after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1377683Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1173278Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
AID1430075Permeability of the compound at pH 7.42017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1433249Induction of apoptosis in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant at 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1396588Induction of ROS production in ionizing radiation induced human WI38 senescent cells up to 64 uM after 1.5 hrs by DHR123 dye based flow cytometry2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
AID1455376Inhibition of TGF-beta1-induced decrease in expression levels of E-cadherin protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1173274Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 1 uM2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
AID1433303Induction of apoptosis in p53 null human U937 cells assessed as increase in Bim EL expression level by measuring ratio of Bim EL to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433291Induction of apoptosis in p53 null human U937 cells at 2 uM preincubated with NAC for 3 hrs followed by compound addition measured after 24 hrs by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459278Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 10 uM after 24 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1433248Induction of apoptosis in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant at 2 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459307Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1276116Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1677559Cytotoxicity against human BEL-7402/5-FU cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1433273Effect on SAHA-induced HDAC6 inhibition in p53 null human U937 cells assessed as hyper acetylation of alpha tubulin at 1 uM after 4 hrs by Western blot analysis2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1158953Cytotoxicity against human WI38 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1551749Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation at 300 uM preincubated for 3 mins followed by arachidonic acid addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1206052Induction of ROS production in human A549 cells after 3 hrs by DHE staining-based fluorescence assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1377684Cytotoxicity against human CCD-841 cells assessed as reduction in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1741861Inhibition of purified rat liver TrxR measured after 75 mins in presence of NADPH by DTNB based assay2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1433245Induction of apoptosis in p53 null human U937 cells at 2 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1728183Cytotoxicity against rat PC12 cells at 50 uM by MTT assay2021European journal of medicinal chemistry, Jan-15, Volume: 210Identification and optimization of piperlongumine analogues as potential antioxidant and anti-inflammatory agents via activation of Nrf2.
AID1459292Induction of microtubule depolymerization in human MCF7 cells at 10 uM after 16 hrs by immunofluorescence analysis2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1474940Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1433252Antiproliferative activity against human CMK cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1377677Aqueous solubility of the compound in pure water by HPLC analysis2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1459268Antiproliferative activity in human Jurkat cells assessed as cell viability after 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1433284Cytotoxicity against human MCF10A cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1455388Inhibition of TGF-beta1-regulated increase in nuclear beta-catenin in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1206046Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1741882Induction of autophagy in human MDA-MB-231 cells transfected with mRFP-eGFP-LC3 assessed as accumulation of autolysosome by measuring increase in red fluorescence at 1.8 uM measured after 24 hrs by confocal laser scanning microscopy2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1433251Antiproliferative activity against human CMS cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1229945Cytotoxicity against human L02 cells assessed as reduction in cell viability at 20 uM to 100 uM incubated for 24 hrs by MTT assay2015Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
Synthesis of piperlongumine analogues and discovery of nuclear factor erythroid 2-related factor 2 (Nrf2) activators as potential neuroprotective agents.
AID1455333Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1474939Induction of apoptosis in human Saos2 cells after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1459821Inhibition of NF-kappaB in human A549 cells after 24 hrs by luciferase reporter gene assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Synthesis of coumaperine derivatives: Their NF-κB inhibitory effect, inhibition of cell migration and their cytotoxic activity.
AID1377687Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as reduction in tumor weight at 5 mg/kg, ip administered daily for 21 days2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1433264Antiproliferative activity against p53 null human U937 cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1741878Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-3 cleavage at 1.8 uM measured after 72 hrs by Western blot analysis2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1459283Cell cycle arrest in human MCF7 cells assessed as sub G0/G1 phase accumulation at 10 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1392927Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells after 24 hrs by Western blot analysis2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1455384Inhibition of TGF-beta1-induced GSK-3beta phosphorylation in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1564516Inhibition of TrxR in human SH-SY5Y cells using DTNB as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by Ellman's method2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1677558Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1377680Antiproliferative activity against human HCT116 cells at 10 uM after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1455327Antiproliferative activity against human A549 cells after 72 hrs in presence of ligustrazine by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1459281Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 10 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1433302Effect on SAHA-induced DNA damage in p53 null human U937 cells assessed as decrease in CHK1 expression level by measuring ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1433265Antiproliferative activity against human MV4-11 cells after 72 hrs in presence of SAHA by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1206043Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1459284Cell cycle arrest in human MCF7 cells assessed as sub G0/G1 phase accumulation at 20 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1430068Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1433235Induction of cell death in p53 null human U937 cells assessed as combination index at 2 to 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1206042Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1396587Induction of OXR1 degradation in ionizing radiation induced human WI38 senescent cells at 5 uM after 24 hrs by Western blot analysis2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
AID1276117Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1430069Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1455340Clearance in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433246Induction of apoptosis in p53 null human U937 cells at 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1459290Disruption of microtubule network in human MCF7 cells at 20 uM after 16 hrs by immunofluorescence analysis2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1158947Cytotoxicity against human A549 cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1589252Inhibition of MAPK/NFkappaB in ICR mouse RAW264.7 cells assessed as reduction in LPS-induced IL6 production at 10 uM pretreated for 0.5 hrs followed by LPS challenge and measured after 24 hrs by ELISA relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI).
AID1564523Cytotoxicity against human HaCaT assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1459279Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 15 uM after 24 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1430067Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1459306Effect on tubulin polymerization in human Jurkat cells at 12017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID336831Cytotoxicity against human KB cells after 3 days by MTT assay
AID1474923Induction of reactive oxygen species generation in human Saos2 cells at 10 uM after 1 hr by DCFH-DA dye-based fluorescence microscopic analysis relative to control2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1551741Antifungal activity against Candida krusei ATCC 6258 after 24 hrs by CLSI broth microdilution method2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1459282Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 15 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1174984Selectivity ratio of IC50 for human primary CD34+ blood stem cells to IC50 for human MA9.3 cells2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Design of a hydrogen peroxide-activatable agent that specifically targets cancer cells.
AID1474916Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1455325Antiproliferative activity against human U87MG cells after 72 hrs in presence of ligustrazine by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1551751Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation at 300 uM preincubated for 3 mins followed by thrombin addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1741870Down regulation of TrxR1 expression in human MDA-MB-231 cells at 1.8 uM measured after 72 hrs by Western blot analysis2020European journal of medicinal chemistry, Oct-15, Volume: 204Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy.
AID1433300Effect on SAHA-induced DNA damage in p53 null human U937 cells assessed as decrease in Rad51 expression level by measuring ratio of Rad51 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1474917Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1564520Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
AID1551743Antifungal activity against Candida parapsilosis ATCC 22019 after 24 hrs by CLSI broth microdilution method2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1551739Antifungal activity against Candida albicans ATCC 10231 after 24 hrs by CLSI broth microdilution method2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1916767Cytotoxicity against human colon epithelial cells incubated for 24 hrs by CCK-8 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy.
AID1455387Inhibition of TGF-beta1-regulated decrease in cytoplasmic beta-catenin in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455350Antiproliferative activity against human HCT116 cells at 8 uM pretreated with GSH for 1 hr measured after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1433253Antiproliferative activity against human CMY cells after 72 hrs by MTT assay2016Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells.
AID1474922Induction of reactive oxygen species generation in human HCT116 cells at 10 uM after 1 hr by DCFH-DA dye-based fluorescence microscopic analysis2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1276120Cytotoxicity against human HT-29 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1474921Cytotoxicity against human W138 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1455322Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1459303Induction of tubulin depolymerization in human MCF7 cells at 5 to 20 uM after 4 hrs by Western blot method2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1459276Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 10 uM after 48 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1426172Inhibition of GST in human A549 cells at 5 uM after 1.5 hrs by DNs-CV probe based fluorescence microscopic method2017European journal of medicinal chemistry, Jan-27, Volume: 126Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy.
AID1459277Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 5 uM after 24 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1551757Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida krusei ATCC 62582019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1426166Inhibition of equine liver GST assessed as decrease in conjugation of CDNB to GSH preincubated with GSH for 30 mins followed by CDNB addition measured for 3 mins2017European journal of medicinal chemistry, Jan-27, Volume: 126Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy.
AID1276121Cytotoxicity against human GBM10 cells assessed as cell viability after 72 hrs by resazurin reduction assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties.
AID1459265Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 10 uM after 24 hrs by propidium iodide staining based flow cytometry2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1430074Intrinsic solubility of the compound2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1551750Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of PAF-induced platelet aggregation at 300 uM preincubated for 3 mins followed by PAF addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1551744Antibacterial activity against Staphylococcus aureus ATCC 6538 after 24 hrs by CLSI broth microdilution method2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1158952Cytotoxicity against human Hep3B cells after 72 hrs by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents.
AID1377682Antiproliferative activity against human K562 cells at 10 uM after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents.
AID1455334Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455319Aqueous solubility of compound by HPLC analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455369Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as loss of body weight at 4 mg/kg, ip administered thrice a week for 6 consecutive weeks2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1393007Growth inhibition of human LNCAP cells after 24 to 48 hrs by WST-1 assay2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID336832Cytotoxicity against mouse P388 cells after 3 days by MTT assay
AID1206057Reduction in total GSH level in human A549 cells at 10 uM after 4 hrs by luminescence assay2015Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains.
AID1455337AUC (0 to infinity) in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1589250Inhibition of MAPK/NFkappaB in ICR mouse RAW264.7 cells assessed as reduction in LPS-induced TNFalpha production at 10 uM pretreated for 0.5 hrs followed by LPS challenge and measured after 24 hrs by ELISA relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI).
AID1392951Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 10 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit)2018Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells.
AID1551763Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation at 150 uM preincubated for 3 mins followed by arachidonic acid addition measured after 10 mins relative to control2019European journal of medicinal chemistry, Jul-01, Volume: 173Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
AID1455396Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as mortality at 4 mg/kg, ip administered thrice a week for 6 consecutive weeks2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1474918Antiproliferative activity against human SKHEP1 cells after 72 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells.
AID1455383Inhibition of TGF-beta1-induced AKT phosphorylation in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1396585Senolytic activity against ionizing radiation induced human WI38 senescent cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
AID1459267Antiproliferative activity in human MCF7 cells assessed as cell viability after 48 hrs by alamarBlue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents.
AID1173276Cytotoxicity against mouse RAW264.7 cells assessed as cell proliferation at 1 uM2014Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
AID1455326Antiproliferative activity against human HCT116 cells after 72 hrs in presence of ligustrazine by MTT assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1455365Antiinvasive activity in human HCT116 cells assessed as inhibition of TGF-beta1-induced cell invasion at 50 nM after 48 hrs by crystal violet staining-based assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID336830Cytotoxicity against human HT-29 cells after 6 days by MTT assay
AID1677582Activation of p38 phosphorylation in human BEL-7402/5-FU cells at 2 uM incubated for 72 hrs by Western blot analysis
AID1455378Inhibition of TGF-beta1-induced increase in expression levels of MMP-9 protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo.
AID1430076Antitumor activity in human A549 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered every other day for 21 days2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol.
AID1589254Cytotoxicity against ICR mouse RAW264.7 cells assessed as effect on cell proliferation at 10 uM after 24 hrs by MTT assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI).
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (292)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's23 (7.88)29.6817
2010's187 (64.04)24.3611
2020's82 (28.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (0.67%)5.53%
Reviews12 (4.03%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other284 (95.30%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (9)

ArticleYear
Trihydroxy piperlongumine protects aluminium induced neurotoxicity in zebrafish: Behavioral and biochemical approach.
Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, Volume: 268
2023
Altered hallmarks of DNA double-strand breaks, oxidative DNA damage and cytogenotoxicity by piperlongumine in hippocampus and hepatocytes of rats intoxicated with cyclophosphamide.
Life sciences, Mar-01, Volume: 316
2023
Hyaluronic acid nanoemulsions improve piplartine cytotoxicity in 2D and 3D breast cancer models and reduce tumor development after intraductal administration.
International journal of biological macromolecules, Oct-31, Volume: 219
2022
Using Sensors and Generators of H2O2 to Elucidate the Toxicity Mechanism of Piperlongumine and Phenethyl Isothiocyanate.
Antioxidants & redox signaling, 06-01, Volume: 24, Issue: 16
2016
Piperlongumine for Enhancing Oral Bioavailability and Cytotoxicity of Docetaxel in Triple-Negative Breast Cancer.
Journal of pharmaceutical sciences, Volume: 104, Issue: 12
2015
No evident dose-response relationship between cellular ROS level and its cytotoxicity--a paradoxical issue in ROS-based cancer therapy.
Scientific reports, May-22, Volume: 4
2014
Cytotoxicity of piperamides towards Aedes aegypti (Diptera: Culicidae).
Journal of medical entomology, Volume: 51, Issue: 2
2014
Diferuloylmethane augments the cytotoxic effects of piplartine isolated from Piper chaba.
Toxicology in vitro : an international journal published in association with BIBRA, Volume: 23, Issue: 6
2009
Evaluation of the genotoxicity of piplartine, an alkamide of Piper tuberculatum, in yeast and mammalian V79 cells.
Mutation research, Apr-30, Volume: 652, Issue: 2
2008
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (3)

ArticleYear
Nanoemulsion formulations for anti-cancer agent piplartine--Characterization, toxicological, pharmacokinetics and efficacy studies.
International journal of pharmaceutics, Feb-10, Volume: 498, Issue: 1-2
2016
LC analysis and pharmacokinetic study of synthetic piperlonguminine in rat plasma after oral administration.
Biomedical chromatography : BMC, Volume: 27, Issue: 7
2013
Simultaneous UFLC-ESI-MS/MS determination of piperine and piperlonguminine in rat plasma after oral administration of alkaloids from Piper longum L.: application to pharmacokinetic studies in rats.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, Oct-01, Volume: 879, Issue: 27
2011
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (10)

ArticleYear
A strategy to improve the solubility and bioavailability of the insoluble drug piperlongumine through albumin nanoparticles.
Pakistan journal of pharmaceutical sciences, Volume: 36, Issue: 2
2023
Enhanced therapeutic efficacy of Piperlongumine for cancer treatment using nano-liposomes mediated delivery.
International journal of pharmaceutics, Aug-25, Volume: 643
2023
Piperlonguminine attenuates renal fibrosis by inhibiting TRPC6.
Journal of ethnopharmacology, Sep-15, Volume: 313
2023
Piperlongumine, a potent anticancer phytotherapeutic: Perspectives on contemporary status and future possibilities as an anticancer agent.
Pharmacological research, Volume: 156
2020
Details of the cooperative binding of piperlongumine with rat serum albumin obtained by spectroscopic and computational analyses.
Scientific reports, 10-30, Volume: 9, Issue: 1
2019
Selective Anticancer Therapy Using Pro-Oxidant Drug-Loaded Chitosan-Fucoidan Nanoparticles.
International journal of molecular sciences, Jun-30, Volume: 20, Issue: 13
2019
Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI).
European journal of medicinal chemistry, Apr-01, Volume: 167
2019
Nanoemulsion formulations for anti-cancer agent piplartine--Characterization, toxicological, pharmacokinetics and efficacy studies.
International journal of pharmaceutics, Feb-10, Volume: 498, Issue: 1-2
2016
Piperlongumine for Enhancing Oral Bioavailability and Cytotoxicity of Docetaxel in Triple-Negative Breast Cancer.
Journal of pharmaceutical sciences, Volume: 104, Issue: 12
2015
Overview of the therapeutic potential of piplartine (piperlongumine).
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, Feb-14, Volume: 48, Issue: 3
2013
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (4)

ArticleYear
Annexin A1 Mimetic Peptide and Piperlongumine: Anti-Inflammatory Profiles in Endotoxin-Induced Uveitis.
Cells, 11-15, Volume: 10, Issue: 11
2021
Minimal dosing of leukocyte targeting TRAIL decreases triple-negative breast cancer metastasis following tumor resection.
Science advances, Volume: 5, Issue: 7
2019
No evident dose-response relationship between cellular ROS level and its cytotoxicity--a paradoxical issue in ROS-based cancer therapy.
Scientific reports, May-22, Volume: 4
2014
Piperlongumine selectively kills glioblastoma multiforme cells via reactive oxygen species accumulation dependent JNK and p38 activation.
Biochemical and biophysical research communications, Jul-19, Volume: 437, Issue: 1
2013
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Interactions (2)

ArticleYear
Piperlongumine combined with vitamin C as a new adjuvant therapy against gastric cancer regulates the ROS-STAT3 pathway.
The Journal of international medical research, Volume: 50, Issue: 4
2022
In vitro and in vivo antitumor effect of 5-FU combined with piplartine and piperine.
Journal of applied toxicology : JAT, Volume: 28, Issue: 2
2008
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]