Page last updated: 2024-11-08

nsc 674495

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

NSC 674495: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID384525
CHEMBL ID11825
SCHEMBL ID1326042
MeSH IDM0337756

Synonyms (41)

Synonym
smr001565831
BB 0245167
NCI60_026383
mls002702269 ,
NSC674495 ,
nsc-674495
benzothiazole, 2-(4-amino-3-methylphenyl)-
benzenamine, 4-(benzothiazol-2-yl)-2-methyl-
BAS 06856403
4-benzothiazol-2-yl-2-methyl-phenylamine
df 203
2-(4-amino-3-methylphenyl)benzothiazole
nsc 674495
df-203
4-(1,3-benzothiazol-2-yl)-2-methylaniline
STK027735
bdbm50141278
4-benzothiazol-2-yl-2-methyl-phenyl amine
4-(3h-1lambda*4*-benzothiazol-2-yl)-2-methyl-phenylamine
4-(benzo[d]thiazol-2-yl)-2-methylbenzenamine
cid_384525
AKOS000108517
CHEMBL11825 ,
BBL008089
SCHEMBL1326042
178804-04-1
benzenamine, 4-(2-benzothiazolyl)-2-methyl-
CCG-35258
4-(benzo[d]thiazol-2-yl)-2-methylaniline
2-(4'-amino-3'-methylphenyl)benzothiazole
HMS3433D11
DTXSID30327656
mfcd00950805
SR-01000319885-1
sr-01000319885
[4-(1,3-benzothiazol-2-yl)-2-methylphenyl]amine
VS-01825
bm8 ,
4-(1,3-benzothiazol-2-yl)-2-methyl-aniline
EN300-231774
PD011737

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"A series of water-soluble L-lysyl- and L-alanyl-amide prodrugs of the lipophilic antitumor 2-(4-aminophenyl)benzothiazoles has been synthesized to address formulation and bioavailability issues related to the desired parenteral administration of the chosen clinical candidate."( Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs.
Hutchinson, I; Jennings, SA; Stevens, MF; Vishnuvajjala, BR; Westwell, AD, 2002
)
0.31

Dosage Studied

ExcerptRelevanceReference
"0 microg/ml, and was applied to monitor the plasma concentration of MAB in a rat dosed with 25 mg/kg as a 1 min intravenous infusion."( Analysis of 2-(3-methyl-4-aminophenyl)-benzothiazole (NSC 674495) in plasma by gas chromatography with mass-selective detection.
Bramhall, C; Buckley, J; Daw, TW; Phillips, LR; Stinson, SF, 1999
)
0.55
" The biphasic dose-response relationship characteristically shown by the benzothiazole series against sensitive cell lines was exhibited by the 4- and 6-fluoro-benzothiazoles (10b,d) but not by the 5- and 7-fluoro-benzothiazoles (10h,i)."( Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
Bradshaw, TD; Browne, HL; Chua, MS; Hutchinson, I; Stevens, MF; Trapani, V; Westwell, AD, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.12510.631035.7641100.0000AID504339
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
glp-1 receptor, partialHomo sapiens (human)Potency7.94330.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency3.16230.100020.879379.4328AID588456
ClpPBacillus subtilisPotency1.25891.995322.673039.8107AID651965
TDP1 proteinHomo sapiens (human)Potency21.83690.000811.382244.6684AID686978; AID686979
Smad3Homo sapiens (human)Potency0.11220.00527.809829.0929AID588855
regulator of G-protein signaling 4Homo sapiens (human)Potency100.00000.531815.435837.6858AID504845
chromobox protein homolog 1Homo sapiens (human)Potency79.43280.006026.168889.1251AID540317
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency2.05960.00419.984825.9290AID504444
importin subunit beta-1 isoform 1Homo sapiens (human)Potency33.52785.804836.130665.1308AID540253; AID540263
snurportin-1Homo sapiens (human)Potency33.52785.804836.130665.1308AID540253; AID540263
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency22.38725.804816.996225.9290AID540253
gemininHomo sapiens (human)Potency19.47630.004611.374133.4983AID624296; AID624297
TAR DNA-binding protein 43Homo sapiens (human)Potency17.78281.778316.208135.4813AID652104
[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)
1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)IC50 (µMol)40.00000.06000.06000.0600AID102975
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear hormone receptor family member daf-12Caenorhabditis elegansEC50 (µMol)67.64904.23604.23604.2360AID743038
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
positive regulation of cytokine production1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
positive regulation of cytokine-mediated signaling pathway1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
phospholipid metabolic process1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
phosphatidic acid biosynthetic process1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
epidermis development1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
response to xenobiotic stimulus1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
CDP-diacylglycerol biosynthetic process1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
triglyceride biosynthetic process1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
1-acylglycerol-3-phosphate O-acyltransferase activity1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
endoplasmic reticulum1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
endoplasmic reticulum membrane1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
plasma membrane1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
specific granule membrane1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
endoplasmic reticulum1-acyl-sn-glycerol-3-phosphate acyltransferase betaHomo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (96)

Assay IDTitleYearJournalArticle
AID201019Growth inhibition of the SR leukemia cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID202174Growth inhibition of the SK-MEL-5 Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID42300Growth inhibition of the BT-549 Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID8860Growth inhibition of the A549/ATCC non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID93637Growth inhibition against ovarian cancer cell line IGROV12001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID201812Growth inhibition of the SK-MEL-2 Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID201977Growth inhibition of the SK-MEL-28 Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID259223Antiproliferative activity against human breast cancer cell line MCF72006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines.
AID200955Growth inhibition of the SF-268 CNS cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID143486Growth inhibition of the NCI/ADR-RES Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID57893Growth inhibition of the DU-145 Prostate cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID92292In vitro concentration to reduce colony formation of human tumor xenografts to 30% of the control1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID105217Growth inhibition of the MDA-ME-231/ATCC Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID8230Growth inhibition of the 786-O Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID200487Growth inhibition of the SNB19 CNS cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID143050Growth inhibition of the NCI-H460 non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID497352Cell cycle arrest in human BCC cells assessed as accumulation at sub G1 phase at 4 uM incubated for 4 hrs followed by 1 J/cm'2 UV irradiation measured after 24 hrs by annexin V/propidium iodide-based flow cytometry2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis, and biological evaluation of 2-(4-aminophenyl)benzothiazole derivatives as photosensitizing agents.
AID94856Growth inhibition of the KM12 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID156197Growth inhibition of the PC-3 Prostate cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID92289Clonal growth inhibition by the compound at at a concentration of 10(ug/mL) in human tumor xenografts in vitro. active, T/C < 30%; activity value is 2/221999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID145775Growth inhibition of the OVCAR-8 Ovarian cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID85238Growth inhibition of the Hs 578.T Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID79808Growth inhibition against colon cancer cell line HCC2998; not tested2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID67447Growth inhibition of the EKVX non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID78643Growth inhibition of the HCT-15 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID80855Growth inhibition of the HCT116 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID215131Growth inhibition of the UO-31 Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID46468Growth inhibition of the COLO-205 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID19199Log P (Octanol:buffer pH 7.4)2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Antitumour benzothiazoles. Part 15: The synthesis and physico-chemical properties of 2-(4-aminophenyl)benzothiazole sulfamate salt derivatives.
AID102445Growth inhibition against breast cancer line MCF-72001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID93628Growth inhibition of the UACC-62 Ovarian cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID259225Antiproliferative activity against human colon cancer cell line KM122006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines.
AID102556Growth inhibition of the MALME-3M Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID104082In vitro cytotoxicity against MCF-7 human mammary carcinoma cells1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID201119Growth inhibition of the SF-295 CNS cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID43864Growth inhibition of the CCRF-CEM leukemia cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID101526Growth inhibition of the M14 Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID202982Growth inhibition of the SK-OV-3 Ovarian cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID201298Growth inhibition of the SF-539 CNS cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID105218Growth inhibition of the MDA-ME-435 Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID145189Growth inhibition of the NCI-H322M non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID167421Growth inhibition of the RXF-393 Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID145085Growth inhibition against non-small cell lung cancer cell line NCI-H2662001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID209039Growth inhibition against cancer cell line TH-102001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID145615Growth inhibition against ovarian cancer cell line OVCAR-42001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID105242Growth inhibition of the MDA-N Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID102101In vitro antitumor activity against MCF-7 carcinoma cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID96332Growth inhibition of the K-562 leukemia cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID259226Antiproliferative activity against human colon cancer cell line HCC29982006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines.
AID92284Clonal growth inhibition by the compound at at a concentration of 1(ug/mL) in human tumor xenografts in vitro. active, T/C < 30%.Sensitive cell lines are lung adrenocarcinoma 289 and mammary MCF-7; activity value is 2/221999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID102975Inhibitory concentration against human lysophosphatidic acid acyltransferase-beta (LPAAT-beta) expressed in Sf9 insect cell membranes2004Bioorganic & medicinal chemistry letters, Mar-22, Volume: 14, Issue:6
Synthesis and SAR of 2-arylbenzoxazoles, benzothiazoles and benzimidazoles as inhibitors of lysophosphatidic acid acyltransferase-beta.
AID83780Growth inhibition of the HT-29 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID209387Growth inhibition of the TK-10 Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID28914log P value in octanol:buffer at pH 7.42002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs.
AID214762Growth inhibition of the UACC-62 Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID28913log P value in cyclohexane:buffer at pH 7.42002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs.
AID144774In vitro antitumor activity against carcinoma cell lines by 6-day assay1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID200467Growth inhibition of the SN12C Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID28982Delta logP2002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Antitumor benzothiazoles. 16. Synthesis and pharmaceutical properties of antitumor 2-(4-aminophenyl)benzothiazole amino acid prodrugs.
AID214243Growth inhibition of the U251 CNS cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID143348Growth inhibition of the NCI-H522 non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID10031Growth inhibition of the ACHN Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID144773In vitro antitumor activity against carcinoma cell lines by 2-day assay1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID79792Growth inhibition of the HCC2998 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID144652Mean GI50 values are recorded over the NCI 60-cell panel.2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID101769Growth inhibition of the MCF-7 Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID8270Growth inhibition of the A498 Renal cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID144944Growth inhibition of the NCI-H226 non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID259224Antiproliferative activity against human breast cancer cell line MDA4682006Journal of medicinal chemistry, Jan-12, Volume: 49, Issue:1
Antitumor benzothiazoles. 26.(1) 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines.
AID200673Growth inhibition of the SNB-75 CNS cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID81516Growth inhibition of the HOP-62 non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID92283Clonal growth inhibition by the compound at at a concentration of 0.1(ug/mL) in human tumor xenografts in vitro. active, T/C < 30%; activity value is 2/221999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID100701Growth inhibition of the LOX IMVI Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID143181Growth inhibition against non-small cell lung cancer cell line NCI-H4602001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID145602Growth inhibition of the OVCAR-4 Ovarian cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID19198Log P (Cyclohexane:buffer pH 7.4)2001Bioorganic & medicinal chemistry letters, Apr-23, Volume: 11, Issue:8
Antitumour benzothiazoles. Part 15: The synthesis and physico-chemical properties of 2-(4-aminophenyl)benzothiazole sulfamate salt derivatives.
AID145750Growth inhibition against ovarian cancer cell line OVCAR-52001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID201851Growth inhibition of the SW-620 colon cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID104117In vitro antitumor activity against MDA-468 carcinoma cell line.1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Antitumor benzothiazoles. 7. Synthesis of 2-(4-acylaminophenyl)benzothiazoles and investigations into the role of acetylation in the antitumor activities of the parent amines.
AID81665Growth inhibition of the HL-60(TB) leukemia cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID210123Growth inhibition of the T-47D Breast cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID214594Growth inhibition of the UACC-257 Melanoma cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID105485Growth inhibition of the MOLT-4 leukemia cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
AID209978Growth inhibition against breast cancer line T-47-D2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
AID145060Growth inhibition of the NCI-H23 non-small cell lung cancer cell line for 2-day in vitro assay.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Antitumor benzothiazoles. 8. Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4-aminophenyl)benzothiazoles.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (21)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (14.29)18.2507
2000's14 (66.67)29.6817
2010's3 (14.29)24.3611
2020's1 (4.76)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 (%)
Trials0 (0.00%)5.53%
Reviews2 (9.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (90.48%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]