Compounds > indibulin
Page last updated: 2024-09-20

indibulin

Description

indibulin: Tubulin Modulator/Antineoplastic Agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2929
CHEMBL ID49642
SCHEMBL ID3165856
MeSH IDM0511873

Synonyms (57)

Synonym
2-(1-(4-chlorobenzyl)-1h-indol-3-yl)-2-oxo-n-(pyridin-4-yl)acetamide
D-24851 ,
indibulin [inn]
NCGC00160428-01
204205-90-3
zio-301
CHEMBL49642
indibulin
2-[1-(4-chlorobenzyl)-1h-indol-3-yl]-2-oxo-n-(pyridin-4-yl)acetamide
2-[1-[(4-chlorophenyl)methyl]indol-3-yl]-2-oxo-n-pyridin-4-ylacetamide
AKOS005619980
STK783524
2-(1-(4-chlorophenylmethyl)-1h-indol-3-yl)-2-oxo-n-(pyridin-4-yl)acetamide
80k4h2rb8p ,
1h-indole-3-acetamide, 1-((4-chlorophenyl)methyl)-alpha-oxo-n-4-pyridinyl-
unii-80k4h2rb8p
indibulin [usan:inn]
d 24851
indibulin (usan/inn)
D10013
NCGC00160428-02
indibulin [usan]
2-{1-[(4-chlorophenyl)methyl]-1h-indol-3-yl}-2-oxo-n-(pyridin-4-yl)acetamide
SCHEMBL3165856
MLS006011745
smr004703467
2-[1-(4-chlorobenzyl)-1h-indol-3-yl]-2-oxo-n-pyridin-4-ylacetamide
1h-indole-3-acetamide, 1-[(4-chlorophenyl)methyl]-.alpha.-oxo-n-(4-pyridinyl)-
SOLIIYNRSAWTSQ-UHFFFAOYSA-N
DTXSID70174368
SR-01000883991-1
sr-01000883991
J-013299
2-[1-(4-chlorobenzyl)-1h-indol-3-yl]-2-oxo-n-(4-pyridinyl)acetamide
FT-0745397
DB06169
BS-16422
c22h16cln3o2
AMY21420
SB16543
mfcd05861105
zio 301;d 24851;zio301;d24851;zio-301;d-24851
BCP33949
1h-indole-3-acetamide, 1-[(4-chlorophenyl)methyl]-alpha-oxo-n-4-pyridinyl-
HY-13649
CS-0007536
zio 301;d 24851
Q27269154
D82641
EX-A4542
S0444
d 24851zio 301
zio 301
A934135
nsc-758489
nsc758489
bdbm50510963

Research Excerpts

Overview

ExcerptReference
"Indibulin is a synthetic small molecule which antitumor activity is based upon destabilization of microtubules. "( Beijnen, JH; Daehling, A; Kuppens, IE; Schellens, JH; Schot, M; Schuessler, VM; Voest, EE; Witteveen, PO, 2007)

Actions

ExcerptReference
"Indibulin did not inhibit the binding of vinblastine or taxol to tubulin."( Kumari, A; Panda, D; Prassanawar, SS, 2023)

Treatment

ExcerptReference
"Indibulin treatment also perturbed the localization of end-binding proteins at the growing microtubule ends in MCF-7 cells."( Kapoor, S; Panda, D; Srivastava, S, 2018)

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency0.00930.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency0.82890.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.10680.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency0.13210.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency0.30110.01238.964839.8107AID1645842
polyproteinZika virusPotency0.00930.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency0.69690.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.30110.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.30110.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.30110.01238.964839.8107AID1645842
[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)
Tubulin beta-2B chainBos taurus (cattle)IC50 (µMol)0.25000.25001.88388.7000AID1545776
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)0.25000.25001.87798.7000AID1545776
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)0.25000.25001.86568.7000AID1545776
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (48)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
microtubule-based processTubulin beta-2B chainBos taurus (cattle)
nervous system developmentTubulin beta-2B chainBos taurus (cattle)
positive regulation of axon guidanceTubulin beta-2B chainBos taurus (cattle)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
GTPase activityTubulin beta-2B chainBos taurus (cattle)
metal ion bindingTubulin beta-2B chainBos taurus (cattle)
protein heterodimerization activityTubulin beta-2B chainBos taurus (cattle)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
microtubule cytoskeletonTubulin beta-2B chainBos taurus (cattle)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (117)

Assay IDTitleYearJournalArticle
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1731653Antiproliferative activity against human Jurkat cells assessed as cell survival at 10 uM (Rvb = 104.3 +/ 10.2 %)2021Bioorganic & medicinal chemistry letters, 04-01, Volume: 37Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization.
AID449971Cytotoxicity against mouse L1210 cells after 48 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and structure-activity relationships of N-aryl(indol-3-yl)glyoxamides as antitumor agents.
AID1700010Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID677620Antitrypanosomal activity against bloodstream form of Trypanosoma brucei 427 after 48 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Identification of selective tubulin inhibitors as potential anti-trypanosomal agents.
AID1267184Aqueous solubility of the compound by UV-HPLC2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID1700012Cytotoxicity against human SK-OV-3 cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1432113Growth inhibition of human PC3 cells after 48 hrs by MTT assay
AID1432155Induction of apoptosis in human DU145 cells assessed as upregulation of Bax protein expression at 400 nM after 48 hrs by Western blot method
AID1267188Solubility in 2% DMSO containing 50 mM potassium phosphate buffer solution pH 7.4 at 1 uM by dynamic light scattering method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID116620Percent increase in life span of P388-inoculated leukemic mice at a dose of 200 mg/kg2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1267202Cytotoxicity against multidrug resistant human MES-SA/Dx5 cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID1700009Cytotoxicity against human A549 cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1700006Induction of microtubule destabilization in sea urchin embryo assessed as embryo spinning measured after 0.5 to 20 hrs2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1267217Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID1700005Antimitotic activity against sea urchin embryo assessed as cleavage arrest measured 2.5 to 6 hrs post-fertilization by light microscopy analysis2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1700004Antimitotic activity against sea urchin embryo assessed as cleavage alteration measured 2.5 to 6 hrs post-fertilization by light microscopy analysis2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1507098Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell survival after 48 hrs by MTT assay2017European journal of medicinal chemistry, Aug-18, Volume: 136
AID677621Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Identification of selective tubulin inhibitors as potential anti-trypanosomal agents.
AID1700014Cytotoxicity against human DU-145 cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID116621Percent increase in life span of P388-inoculated leukemic mice at a dose of 25 mg/kg2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID106338In vitro anticancer activity against human uterus MES-SA/DX5 subline (doxorubicin-resistant)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1432138Induction of apoptosis in human DU145 cells assessed as early apoptotic cells at 400 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.81%)
AID1700016Cytotoxicity against human HFF cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID431417Antiproliferative activity against human HT-29 cells2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
AID1700031Aggregation property of the compound in water2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1507097Cytotoxicity against human MCF7 cells assessed as reduction in cell survival after 48 hrs by MTT assay2017European journal of medicinal chemistry, Aug-18, Volume: 136
AID1267218Cytotoxicity against human MES-SA cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID116619Percent increase in life span of P388-inoculated leukemic mice at a dose of 100 mg/kg2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1731655Antiproliferative activity against human SMS-SB cells assessed as cell survival at 10 uM (Rvb = 100 +/ 6 %)2021Bioorganic & medicinal chemistry letters, 04-01, Volume: 37Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization.
AID1700011Cytotoxicity against human A-375 cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1267190Cytotoxicity against human FADU cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID449970Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and structure-activity relationships of N-aryl(indol-3-yl)glyoxamides as antitumor agents.
AID1700013Cytotoxicity against human PC-3 cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID1267216Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID1672883Antiproliferative activity against D4-9-31 resistance human A2780 cells incubated for 72 hrs by ATPlite reagent based assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Resistance mechanisms and cross-resistance for a pyridine-pyrimidine amide inhibitor of microtubule polymerization.
AID86572In vitro anticancer activity against human hepatocellular HepG2 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1432112Growth inhibition of human DU145 cells after 48 hrs by MTT assay
AID1432152Inhibition of porcine brain tubulin polymerization measured for 1 hr by fluorescence assay
AID1432150Inhibition of porcine brain tubulin polymerization at 0.5 uM measured for 1 hr by fluorescence assay relative to control
AID1267215Cytotoxicity against human SCC4 cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID431418Antiproliferative activity against human MDA-MB-231 cells2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
AID1545776Inhibition of bovine brain tubulin polymerization incubated for 1 hr2019European journal of medicinal chemistry, Dec-01, Volume: 183Indole: A privileged scaffold for the design of anti-cancer agents.
AID449972Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and structure-activity relationships of N-aryl(indol-3-yl)glyoxamides as antitumor agents.
AID1731652Antiproliferative activity against human U-937 cells assessed as cell survival at 10 uM (Rvb = 100 +/ 8.7 %)2021Bioorganic & medicinal chemistry letters, 04-01, Volume: 37Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization.
AID106328In vitro anticancer activity against human uterus MES-SA cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1267189Solubility in 2% DMSO containing 50 mM potassium phosphate buffer solution pH 7.4 at 10 uM by dynamic light scattering method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID88806In vitro anticancer activity against human gastric NUGC3 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1267182Inhibition of porcine brain tubulin polymerization assessed as reduction in GTP-induced microtubule assembly after 60 mins by OD340 method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID1432139Induction of apoptosis in human DU145 cells assessed as late apoptotic cells at 400 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 2.55%)
AID1646361Antiproliferative activity against human HeLa cells assessed as reduction in cell viability2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors.
AID324961Cytotoxicity against human HL60/TX1000 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines.
AID1432140Induction of apoptosis in human DU145 cells assessed as necrotic cells at 400 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.75%)
AID1267180Inhibition of porcine brain tubulin polymerization after 60 mins by DAPI staining based fluorescence method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
AID1731654Antiproliferative activity against human BT-474 cells assessed as cell survival at 10 uM (Rvb = 100 +/ 6.3 %)2021Bioorganic & medicinal chemistry letters, 04-01, Volume: 37Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization.
AID1432137Induction of apoptosis in human DU145 cells assessed as live cells at 400 nM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 95.89%)
AID103746In vitro anticancer activity against human breast MCF-7 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID26229Calculated partition coefficient (clogP) (AlogP)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID152705In vitro anticancer activity against murine leukemic P388 cells2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1432115Growth inhibition of human HCT15 cells after 48 hrs by MTT assay
AID449973Cell cycle arrest in human KB/HeLa cells assessed as accumulation in G2/M phase by cytometric analysis2009Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18
Synthesis and structure-activity relationships of N-aryl(indol-3-yl)glyoxamides as antitumor agents.
AID1672882Antiproliferative activity against human A2780 cells incubated for 72 hrs by ATPlite reagent based assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Resistance mechanisms and cross-resistance for a pyridine-pyrimidine amide inhibitor of microtubule polymerization.
AID1700015Cytotoxicity against human T47D cells assessed as cell growth inhibition2020Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
Synthesis and biological evaluation of indolylglyoxylamide bisphosphonates, antimitotic microtubule-targeting derivatives of indibulin with improved aqueous solubility.
AID103929In vitro anticancer activity against human breast MCF-7/ADR subline (adriamycin-resistant)2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID431416Inhibition of bovine brain tubulin polymerization2009Journal of medicinal chemistry, Oct-08, Volume: 52, Issue:19
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
AID1432114Growth inhibition of human A549 cells after 48 hrs by MTT assay
AID116622Percent increase in life span of P388-inoculated leukemic mice at a dose of 50 mg/kg2003Journal of medicinal chemistry, Apr-24, Volume: 46, Issue:9
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (36)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (36.11)29.6817
2010's12 (33.33)24.3611
2020's11 (30.56)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 (5.41%)5.53%
Reviews1 (2.70%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (91.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceDescriptionRelationhip StrengthStudiesTrialsClassesRoles
paclitaxel[no description available]medium50taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
fluorouracil[no description available]medium10nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
vinblastine[no description available]medium20
vinorelbine[no description available]medium10acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid		antineoplastic agent;
photosensitizing agent
bpr0l075[no description available]medium10
nocodazole[no description available]medium10aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes		antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator
colchicine[no description available]medium70alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
e 7010[no description available]medium10sulfonamide
jcc 76[no description available]medium10
nsc751382[no description available]medium10
vincristine[no description available]medium30acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
podophyllotoxin[no description available]medium20furonaphthodioxole;
lignan;
organic heterotetracyclic compound		antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
docetaxel anhydrous[no description available]medium10secondary alpha-hydroxy ketone;
tetracyclic diterpenoid		antimalarial;
antineoplastic agent;
photosensitizing agent
vincaleukoblastine[no description available]medium20acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite
epothilone b[no description available]medium10epothilone;
epoxide		antineoplastic agent;
apoptosis inducer;
microtubule-stabilising agent
vorinostat[no description available]medium10dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
belinostat[no description available]medium10hydroxamic acid;
olefinic compound;
sulfonamide		antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
panobinostat[no description available]medium10cinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound		angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor
n-(2-amino-5-fluorobenzyl)-4-(n-(pyridine-3-acrylyl)aminomethyl)benzamide[no description available]medium10
alendronate[no description available]medium101,1-bis(phosphonic acid);
primary amino compound		bone density conservation agent;
EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor
pamidronate[no description available]medium10phosphonoacetic acid
risedronic acid[no description available]medium10pyridines
tubercidin[no description available]medium10antibiotic antifungal agent;
N-glycosylpyrrolopyrimidine;
ribonucleoside		antimetabolite;
antineoplastic agent;
bacterial metabolite
zoledronic acid[no description available]medium101,1-bis(phosphonic acid);
imidazoles		bone density conservation agent
thiazoles[no description available]medium101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
pyrroles[no description available]medium10pyrrole;
secondary amine
glycine[no description available]medium10alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
kahalalide f[no description available]medium10
rofecoxib[no description available]medium10butenolide;
sulfone		analgesic;
cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug
ConditionIndicatedRelationship StrengthStudiesTrials
African Sleeping Sickness0low10
African Trypanosomiasis0low10
Benign Neoplasms0medium42
Benign Neoplasms, Brain0low10
Brain Cancer0low10
Brain Metastases0low10
Brain Neoplasm, Primary0low10
Brain Neoplasms0low10
Brain Neoplasms, Benign0low10
Brain Neoplasms, Malignant0low10
Brain Neoplasms, Malignant, Primary0low10
Brain Neoplasms, Primary Malignant0low10
Brain Tumor, Primary0low10
Brain Tumor, Recurrent0low10
Brain Tumors0low10
Breast Cancer0low20
Breast Carcinoma0low20
Breast Tumors0low20
Cancer0medium42
Cancer of Brain0low10
Cancer of Breast0low20
Cancer of Cervix0low10
Cancer of Head0low10
Cancer of Head and Neck0low10
Cancer of Lung0low30
Cancer of Neck0low10
Cancer of Ovary0low10
Cancer of the Brain0low10
Cancer of the Breast0low20
Cancer of the Cervix0low10
Cancer of the Head0low10
Cancer of the Head and Neck0low10
Cancer of the Lung0low30
Cancer of the Neck0low10
Cancer of the Ovary0low10
Cancer of the Uterine Cervix0low10
Carcinoma0low10
Carcinoma, Anaplastic0low10
Carcinoma, Non-Small Cell Lung0low30
Carcinoma, Non-Small-Cell Lung0low30
Carcinoma, Spindle-Cell0low10
Carcinoma, Undifferentiated0low10
Carcinomatosis0low10
Cervical Cancer0low10
Cervical Neoplasms0low10
Cervix Cancer0low10
Cervix Neoplasms0low10
Congenital Zika Syndrome0low10
Congenital Zika Virus Infection0low10
Disease Models, Animal0low10
Epithelial Neoplasms, Malignant0low10
Epithelial Tumors, Malignant0low10
Epithelioma0low10
Fever, Zika0low10
Glial Cell Tumors0low10
Glioma0low10
Head and Neck Cancer0low10
Head and Neck Neoplasm0low10
Head and Neck Neoplasms0low10
Head Cancer0low10
Head Neoplasm0low10
Head Neoplasms0low10
Head, Neck Neoplasms0low10
Human Mammary Carcinoma0low20
Intracranial Neoplasms0low10
Leucocythaemia0low10
Leucocythemia0low10
Leukemia0low10
Leukemia L 12100low10
Leukemia L12100low10
Leukemia P3880low10
Lung Cancer0low30
Lung Neoplasms0low30
Malignancy0medium42
Malignant Epithelial Neoplasms0low10
Malignant Glioma0low10
Malignant Neoplasm of Breast0low20
Malignant Neoplasms0medium42
Malignant Neoplasms, Brain0low10
Malignant Primary Brain Neoplasms0low10
Malignant Primary Brain Tumors0low10
Malignant Tumor of Breast0low20
Mammary Cancer0low20
Mammary Carcinoma, Human0low20
Mammary Neoplasm, Human0low20
Mammary Neoplasms, Human0low20
Mixed Glioma0low10
Nagana0low10
Neck Cancer0low10
Neck Neoplasm0low10
Neck Neoplasms0low10
Neoplasia0medium42
Neoplasm0medium42
Neoplasms, Benign0medium42
Neoplasms, Brain0low10
Neoplasms, Brain, Benign0low10
Neoplasms, Brain, Malignant0low10
Neoplasms, Brain, Primary0low10
Neoplasms, Breast0low20
Neoplasms, Cervical0low10
Neoplasms, Cervix0low10
Neoplasms, Head0low10
Neoplasms, Head and Neck0low10
Neoplasms, Intracranial0low10
Neoplasms, Lung0low30
Neoplasms, Malignant Epithelial0low10
Neoplasms, Neck0low10
Neoplasms, Ovarian0low10
Neoplasms, Pulmonary0low30
Neoplasms, Upper Aerodigestive Tract0low10
Nervous System Diseases0low10
Nervous System Disorders0low10
Neuroblastoma0low10
Neurologic Disorders0low10
Neurological Disorders0low10
Non-Small Cell Lung Cancer0low30
Non-Small Cell Lung Carcinoma0low30
Non-Small-Cell Lung Carcinoma0low30
Nonsmall Cell Lung Cancer0low30
Ovarian Cancer0low10
Ovarian Neoplasms0low10
Ovary Cancer0low10
Ovary Neoplasms0low10
P388D(1) Leukemia0low10
Primary Brain Neoplasms0low10
Primary Malignant Brain Neoplasms0low10
Primary Malignant Brain Tumors0low10
Pulmonary Cancer0low30
Pulmonary Neoplasms0low30
Reticulum Cell-Like Sarcoma, Yoshida0low10
Sarcoma, Yoshida0low10
Trypanosomiasis, African0low10
Tumors0medium42
Tumors, Breast0low20
UADT Neoplasm0low10
UADT Neoplasms0low10
Upper Aerodigestive Tract Neoplasm0low10
Upper Aerodigestive Tract Neoplasms0low10
Uterine Cervical Cancer0low10
Uterine Cervical Neoplasms0low10
Zika Fever0low10
Zika Virus Disease0low10
Zika Virus Infection0low10
ZikV Infection0low10

Research Highlights

Safety/Toxicity (3)

ArticleYear
β-III Tubulin Levels Determine the Neurotoxicity Induced by Colchicine-Site Binding Agent Indibulin.
ACS chemical neuroscience, 01-04, Volume: 14, Issue: 1		2023
Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines.
Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue: 6		2008
D-24851, a novel synthetic microtubule inhibitor, exerts curative antitumoral activity in vivo, shows efficacy toward multidrug-resistant tumor cells, and lacks neurotoxicity.
Cancer research, Jan-01, Volume: 61, Issue: 1		2001
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (2)

ArticleYear
Dose-finding and pharmacokinetic study of orally administered indibulin (D-24851) to patients with advanced solid tumors.
Investigational new drugs, Volume: 28, Issue: 2		2010
Phase I dose-finding and pharmacokinetic trial of orally administered indibulin (D-24851) to patients with solid tumors.
Investigational new drugs, Volume: 25, Issue: 3		2007
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (2)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5		2019
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.
Journal of medicinal chemistry, Dec-10, Volume: 58, Issue: 23		2015
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (1)

ArticleYear
Dose-finding and pharmacokinetic study of orally administered indibulin (D-24851) to patients with advanced solid tumors.
Investigational new drugs, Volume: 28, Issue: 2		2010
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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