Compounds > 5-bromoisatin
Page last updated: 2024-11-05

5-bromoisatin

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5-bromoisatin is a halogenated derivative of isatin, a naturally occurring compound found in plants. It is synthesized through the bromination of isatin, often using bromine in an acidic medium. 5-bromoisatin has shown promising biological activity, particularly as a potential anticancer agent. It is studied for its ability to inhibit the growth of various cancer cell lines, including those of breast, colon, and lung cancers. This activity is attributed to its interaction with specific enzymes and signaling pathways involved in cancer cell proliferation. Research continues to explore its potential as a therapeutic agent for various diseases, including cancer, Alzheimer's disease, and epilepsy.'

Cross-References

ID SourceID
PubMed CID6889
CHEMBL ID115897
CHEBI ID149786
SCHEMBL ID136581
MeSH IDM0129761

Synonyms (59)

Synonym
AC-14581
AKOS002375882
EN300-18123
BB 0258954
isatin, 5-bromo-
5-bromoisatin
nsc4980
wln: t56 bmvvj ge
5-bromoindole-2,3-dione
nsc-4980
1h-indole-2, 5-bromo-
5-bromisatin
indole-2, 5-bromo-
87-48-9
einecs 201-747-7
indole-2,3-dione, 5-bromo-
5-bromoindoline-2,3-dione
nsc 4980
5-bromisatin [czech]
brn 0383760
1h-indole-2,3-dione, 5-bromo-
5-bromo-2,3-dihydro-1h-indole-2,3-dione
isatin-based compound, 34
bdbm22814
5-bromo-1h-indole-2,3-dione
STK364356
5-bromoisatin, technical grade, 90%
B1566
5-bromo-2,3-indolinedione
AKOS000200674
CHEMBL115897
CHEBI:149786
A842244
5-bromoindoline-2,3-dione;5-bromoisatin
STL140691
5-bromo-2-hydroxy-3h-indol-3-one
5-21-10-00264 (beilstein handbook reference)
FS-2520
F0900-5717
FT-0620163
5-bromo isatin
5-bromo-1h-indole-2,3dione
5-bromo -1h-indole-2,3-dione
5-bromo-isatin
SCHEMBL136581
AM808100
DTXSID30236037
W-104018
STR04158
5-bromo-1h-indole-2,3-dione #
bromoisatin
CS-W007383
sr-01000402436
SR-01000402436-1
Z57833927
BCP04280
mfcd00005719
SB66105
F11278
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[role 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]

Drug Classes (1)

ClassDescription
indolesAny compound containing an indole skeleton.
[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 (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Coagulation factor XIIHomo sapiens (human)Ki43.27000.00251.86697.2500AID1798240
CholinesteraseHomo sapiens (human)Ki51.37430.00001.51739.7300AID1798240; AID281481
Liver carboxylesterase 1Oryctolagus cuniculus (rabbit)Ki43.27000.01361.70257.2500AID1798240
Protein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)IC50 (µMol)65.00000.04502.67428.0000AID594815
AcetylcholinesteraseHomo sapiens (human)Ki51.37430.00001.27869.7300AID1798240; AID281480
Liver carboxylesterase 1Homo sapiens (human)Ki41.61710.00252.01368.4800AID1798240; AID281478
CruzipainTrypanosoma cruziIC50 (µMol)10.00000.00022.04508.0000AID213673
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (78)

Processvia Protein(s)Taxonomy
plasma kallikrein-kinin cascadeCoagulation factor XIIHomo sapiens (human)
Factor XII activationCoagulation factor XIIHomo sapiens (human)
blood coagulation, intrinsic pathwayCoagulation factor XIIHomo sapiens (human)
positive regulation of plasminogen activationCoagulation factor XIIHomo sapiens (human)
protein processingCoagulation factor XIIHomo sapiens (human)
protein autoprocessingCoagulation factor XIIHomo sapiens (human)
positive regulation of blood coagulationCoagulation factor XIIHomo sapiens (human)
zymogen activationCoagulation factor XIIHomo sapiens (human)
fibrinolysisCoagulation factor XIIHomo sapiens (human)
innate immune responseCoagulation factor XIIHomo sapiens (human)
response to misfolded proteinCoagulation factor XIIHomo sapiens (human)
positive regulation of fibrinolysisCoagulation factor XIIHomo sapiens (human)
blood coagulationCoagulation factor XIIHomo sapiens (human)
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
gene expressionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
dopamine secretionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
chromatin remodelingProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
proteolysisProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
peptide cross-linkingProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
protein deaminationProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
negative regulation of endoplasmic reticulum calcium ion concentrationProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
regulation of apoptotic processProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of apoptotic processProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
apoptotic cell clearanceProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of GTPase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of cell adhesionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of neurogenesisProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of small GTPase mediated signal transductionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of mitochondrial calcium ion concentrationProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
bone developmentProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
branching involved in salivary gland morphogenesisProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
salivary gland cavitationProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
cellular response to cocaineProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
cellular response to dopamineProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
positive regulation of sprouting angiogenesisProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
cellular response to serotoninProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
regulation of apoptotic cell clearanceProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
cholesterol biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
response to toxic substanceLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol effluxLiver carboxylesterase 1Homo sapiens (human)
negative regulation of cholesterol storageLiver carboxylesterase 1Homo sapiens (human)
epithelial cell differentiationLiver carboxylesterase 1Homo sapiens (human)
cholesterol homeostasisLiver carboxylesterase 1Homo sapiens (human)
reverse cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
medium-chain fatty acid metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cellular response to cholesterolLiver carboxylesterase 1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusLiver carboxylesterase 1Homo sapiens (human)
cholesterol ester hydrolysis involved in cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid secretionLiver carboxylesterase 1Homo sapiens (human)
lipid catabolic processLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
serine-type endopeptidase activityCoagulation factor XIIHomo sapiens (human)
calcium ion bindingCoagulation factor XIIHomo sapiens (human)
protein bindingCoagulation factor XIIHomo sapiens (human)
misfolded protein bindingCoagulation factor XIIHomo sapiens (human)
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
protein-glutamine gamma-glutamyltransferase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
calcium ion bindingProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
protein bindingProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
GTP bindingProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
peptidase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
protein-glutamine glutaminase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
histone serotonyltransferase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
histone dopaminyltransferase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
peptide noradrenalinyltransferase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
peptide histaminyltransferase activityProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
sterol esterase activityLiver carboxylesterase 1Homo sapiens (human)
methylumbelliferyl-acetate deacetylase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylesterase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylic ester hydrolase activityLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
extracellular regionCoagulation factor XIIHomo sapiens (human)
extracellular spaceCoagulation factor XIIHomo sapiens (human)
plasma membraneCoagulation factor XIIHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor XIIHomo sapiens (human)
extracellular exosomeCoagulation factor XIIHomo sapiens (human)
extracellular spaceCoagulation factor XIIHomo sapiens (human)
rough endoplasmic reticulumCoagulation factor XIIHomo sapiens (human)
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
collagen-containing extracellular matrixProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
nucleusProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
mitochondrionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
endoplasmic reticulumProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
cytosolProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
plasma membraneProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
focal adhesionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
extracellular matrixProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
perinuclear region of cytoplasmProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
collagen-containing extracellular matrixProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
extracellular exosomeProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
chromatinProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
nucleosomeProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
mitochondrionProtein-glutamine gamma-glutamyltransferase 2Homo sapiens (human)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
cytoplasmLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulum lumenLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
cytosolLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
AID284490Cytotoxicity against human U937 cells2007Bioorganic & medicinal chemistry, Jan-15, Volume: 15, Issue:2
In vitro cytotoxicity evaluation of some substituted isatin derivatives.
AID1063516Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Design, synthesis and in vitro cytotoxicity evaluation of 5-(2-carboxyethenyl)isatin derivatives as anticancer agents.
AID1739634Inhibition of Mycobacterium tuberculosis His6-tagged MabA expressed in Escherichia coli BL21 (DE3) assessed as reduction in HBCoA formation using AcAcCoA as substrate preincubated for 30 mins followed by substrate and 100 uM NADPH addition and measured af2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening.
AID281478Inhibition of human liver CE1 expressed in sf21 cells2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
AID594815Inhibition of human transglutaminase 2 using Cbz-Gln-Gly as a substrate by GDH-coupled assay2011Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2.
AID72522Inhibitory activity against Falcipain-2; no effect2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
AID1063518Cytotoxicity against human K562 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Design, synthesis and in vitro cytotoxicity evaluation of 5-(2-carboxyethenyl)isatin derivatives as anticancer agents.
AID1055713Antiproliferative activity against human NCI-H460 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID197811Inhibitory activity was tested against Rhodesain, a cysteine protease from Trypanosoma brucei rhodesiense; not determined2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
AID281479Inhibition of rabbit liver carboxylesterase expressed in sf21 cells2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
AID1055717Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID281481Inhibition of human BChE2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
AID1055716Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1406678Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
AID1055715Antiproliferative activity against human AsPC1 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID1739636Antimycobacterial activity activity against GFP-tagged Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth incubated for 5 days by fluorescence assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening.
AID1284106Anticancer activity against human Jurkat cells after 48 hrs by MTT assay2016European journal of medicinal chemistry, Apr-13, Volume: 112Synthesis and anti-cancer activity evaluation of 5-(2-carboxyethenyl)-isatin derivatives.
AID213673Inhibitory activity against the Trypanosoma cruzi cysteine protease cruzain2003Bioorganic & medicinal chemistry letters, Oct-20, Volume: 13, Issue:20
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
AID1061202Inhibition of GST-tagged SARS coronavirus 3C-like protease at 1 mM by FRET assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis, modification and docking studies of 5-sulfonyl isatin derivatives as SARS-CoV 3C-like protease inhibitors.
AID1406679Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
AID1063517Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
Design, synthesis and in vitro cytotoxicity evaluation of 5-(2-carboxyethenyl)isatin derivatives as anticancer agents.
AID281477Inhibition of human intestinal carboxylesterase expressed in sf21 cells2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
AID465619Anticancer activity against human U937 cells by MTS assay2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
QSAR study of isatin analogues as in vitro anti-cancer agents.
AID1055714Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay2013European journal of medicinal chemistry, , Volume: 70Novel isatin-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
AID281480Inhibition of human AChE2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
AID1798240Enzyme Inhibition Assay from Article 10.1021/jm061471k: \\Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.\\2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (27.27)29.6817
2010's7 (63.64)24.3611
2020's1 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.47

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

MetricThis Compound (vs All)
Research Demand Index31.47 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index30.68 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.47)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
benzoic acid
Benzoic Acid: A fungistatic compound that is widely used as a food preservative. It is conjugated to GLYCINE in the liver and excreted as hippuric acid.. benzoic acid : A compound comprising a benzene ring core carrying a carboxylic acid substituent.. aromatic carboxylic acid : Any carboxylic acid in which the carboxy group is directly bonded to an aromatic ring.		2.2510benzoic acidsalgal metabolite;
antimicrobial food preservative;
drug allergen;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
human xenobiotic metabolite;
plant metabolite
salicylic acid
Scalp: The outer covering of the calvaria. It is composed of several layers: SKIN; subcutaneous connective tissue; the occipitofrontal muscle which includes the tendinous galea aponeurotica; loose connective tissue; and the pericranium (the PERIOSTEUM of the SKULL).		2.2510monohydroxybenzoic acidalgal metabolite;
antifungal agent;
antiinfective agent;
EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor;
keratolytic drug;
plant hormone;
plant metabolite
indole
[no description available]		2.0310indole;
polycyclic heteroarene		Escherichia coli metabolite
aspirin
Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.		2.2510benzoic acids;
phenyl acetates;
salicylates		anticoagulant;
antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
EC 1.1.1.188 (prostaglandin-F synthase) inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
plant activator;
platelet aggregation inhibitor;
prostaglandin antagonist;
teratogenic agent
isoniazid
Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC).		2.2510carbohydrazideantitubercular agent;
drug allergen
mefenamic acid
Mefenamic Acid: A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.. mefenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,3-dimethylphenyl group. Although classed as a non-steroidal anti-inflammatory drug, its anti-inflammatory properties are considered to be minor. It is used to relieve mild to moderate pain, including headaches, dental pain, osteoarthritis and rheumatoid arthritis.		2.2510aminobenzoic acid;
secondary amino compound		analgesic;
antipyretic;
antirheumatic drug;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-steroidal anti-inflammatory drug;
xenobiotic
vorinostat
Vorinostat: A hydroxamic acid and anilide derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used in the treatment of CUTANEOUS T-CELL LYMPHOMA and SEZARY SYNDROME.. vorinostat : A dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. A histone deacetylase inhibitor, it is marketed under the name Zolinza for the treatment of cutaneous T cell lymphoma (CTCL).		2.0810dicarboxylic acid diamide;
hydroxamic acid		antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
triclosan
[no description available]		2.2510aromatic ether;
dichlorobenzene;
monochlorobenzenes;
phenols		antibacterial agent;
antimalarial;
drug allergen;
EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
fungicide;
persistent organic pollutant;
xenobiotic
phthalimide
phthalimide: RN given refers to parent cpd. phthalimide : A dicarboximide that is 2,3-dihydro-1H-isoindole substituted by oxo groups at positions 1 and 3.		2.0310phthalimides
isatin
tribulin: endogenous MONOAMINE OXIDASE inhibitory activity extractable into ethyl acetate found in brain and many mammalian tissues and fluids; ISATIN is a major component; produced in excess following alcohol withdrawal;		3.5680indoledioneEC 1.4.3.4 (monoamine oxidase) inhibitor;
plant metabolite
indene
indene: structure in first source. 1H-indene : An ortho-fused bicyclic arene comprising of benzene and cyclopentene rings.		2.0310indene;
ortho-fused bicyclic arene
indirubin
[no description available]		2.0610
indan
indan: structure in first source. indane : An ortho-fused bicyclic hydrocarbon consisting of a benzene ring fused to a cyclopentane ring; a high-boiling (176 (o)C) colourless liquid.		2.0310indanes;
ortho-fused bicyclic hydrocarbon
indoline
indoline: structure given in first source		2.0310indoles
1-acetylisatin
1-acetylisatin: structure in first source		2.0310indoledione
1,3-indandione
1,3-indandione : A member of the class of indanones that is indane in which the hydrogens at positions 2 and 4 have been replaced by oxo groups.		2.0310aromatic ketone;
beta-diketone;
indanones
5-methylisatin
5-methylisatin: structure in first source		3.1650
n-methylisatin
N-methylisatin: structure given in first source		2.9540
camptothecin
NSC 100880: carboxylate (opened lactone) form of camptothecin; RN refers to (S)-isomer; structure given in first source		2.5220delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol		antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite
5-Methoxyisatin
[no description available]		3.3260indolesanticoronaviral agent
staurosporine
[no description available]		2.0310indolocarbazole alkaloid;
organic heterooctacyclic compound		apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector
n-phenylphthalimide
N-phenylphthalimide: structure given in first source		2.0310
5-Chloro-1H-indole-2,3-dione
[no description available]		3.4570indolesanticoronaviral agent
5-iodoisatin
5-iodoisatin: structure in first source		3.360indolesanticoronaviral agent
6-bromoisatin
6-bromoisatin: anticancer compound from Dicathais orbita; structure in first source		2.4520
isoindigotin
isoindigotin: used in treatment of chronic granulocytic leukemia; structure given in first source		2.0610
5-Fluoroisatin
[no description available]		3.5680indolesanticoronaviral agent
isatin beta-thiosemicarbazone
isatin beta-thiosemicarbazone: isatizon believed to be Russian synonym		2.0110
1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione
[no description available]		2.0310indoles
ethionamide
Ethionamide: A second-line antitubercular agent that inhibits mycolic acid synthesis.. ethionamide : A thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. A prodrug that undergoes metabolic activation by conversion to the corresponding S-oxide.		2.2510pyridines;
thiocarboxamide		antilipemic drug;
antitubercular agent;
fatty acid synthesis inhibitor;
leprostatic drug;
prodrug
5-Nitroisatin
[no description available]		3.360indolesanticoronaviral agent
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		2.2510cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		02.1310
Leukemia, Lymphocytic, T Cell
[description not available]		02.1310
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.1310
Leukemia, T-Cell
A malignant disease of the T-LYMPHOCYTES in the bone marrow, thymus, and/or blood.		02.1310