Compounds > thiazoles
Page last updated: 2024-08-21

thiazoles and 5f-203

thiazoles has been researched along with 5f-203 in 23 studies

Research

Studies (23)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (56.52)29.6817
2010's9 (39.13)24.3611
2020's1 (4.35)2.80

Authors

AuthorsStudies
Bradshaw, TD; Browne, HL; Chua, MS; Hutchinson, I; Stevens, MF; Trapani, V; Westwell, AD1
Ciolino, HP; Hose, C; Leong, CO; Loaiza-Pérez, AI; Patel, V; Sausville, EA; Stevens, MF; Trapani, V; Trepel, JB; Yeh, GC1
Connelly, J; Harris, E; Hose, C; Monks, A; Sausville, EA1
Hollingshead, M; Hose, CD; Monks, A; Sausville, EA1
Bradshaw, TD; Westwell, AD1
Bibby, MC; Bradshaw, TD; Leong, CO; Stevens, MF; Suggitt, M; Swaine, DJ1
Brantley, E; Ciolino, HP; Gutkind, JS; Hose, CD; Loaiza-Pérez, AI; Patel, V; Sausville, EA; Stinson, SF; Trapani, V; Yeh, GC1
Agama, K; Antony, S; Brantley, E; Kohlhagen, G; Meng, L; Pommier, Y; Sausville, EA; Stinson, SF1
Connelly, J; Covell, DG; Monks, A; Sausville, EA; Wallqvist, A1
Anna, C; Baek, SJ; Eling, TE; Hollingshead, M; Hose, C; Martinez, JM; Monks, A; Okazaki, R; Sali, T; Walker, NJ1
Bae, I; Eling, TE; Kang, BD; Kang, HJ; Kim, HJ; Kwon, SH; Lee, SH1
Barrett, DA; Bradshaw, TD; Bruce, M; Farmer, PB; Gaskell, M; Henderson, CJ; Leong, CO; Stevens, MF; Wolf, R; Wren, JE; Wright, EK1
Bazzi, R; Bell, DR; Bradshaw, TD; Rowlands, JC; Stevens, MF1
Bradshaw, TD; Choo, HL; Leong, CO; Muruhadas, A; Randhawa, N; Stevens, MF; Tan, BS; Tiong, KH1
Guengerich, FP; Wang, K1
Bradshaw, TD; Callero, MA; De Dios, DO; Luzzani, GA; Perez, AI1
Kesharwani, SS; Nandekar, PP; Sangamwar, AT; Shaikh, N; Tumbi, KM1
Amis, LH; Babb, CE; Brantley, E; Campbell, P; Darwanto, A; Davis, WL; Livingston, WJ; McLean, LS; Rowland, L; Scott, L; Senthil, M; Sowers, LC; Watkins, CN; Zylstra, D1
Bradshaw, TD; Citossi, F; Farmer, PB; Gaskell, M; Hose, C; Kaur, B; Kellam, B; Leong, CO; Marlow, M; Monks, A; Singh, R; Stevens, MF; Stocks, M; Stone, EL1
Bradshaw, TD; Callero, MA; Flumian, C; Kuruppu, AI; Loaiza Perez, AI; Luzzani, GA; Todaro, L; Trapani, V1
Boyle, K; Brantley, EJ; Campbell, PS; Daly, D; Mavingire, N; McLean, L; Rowland, LK; Thorne, G; Unternaehrer, J; Whang, S; Wooten, JV; Zylstra, D1
Bradshaw, TD; Breen, AF; Cassioli, ML; Scurr, D; Thomas, NR; Turyanska, L; Wells, G; Zhang, J1
Bradshaw, TD; Cheng, X; Liu, Y; Luo, Y; Shi, D; Stevens, MFG; Tang, T; Wang, Y; Yang, Y; Zhang, J1

Reviews

1 review(s) available for thiazoles and 5f-203

ArticleYear
The development of the antitumour benzothiazole prodrug, Phortress, as a clinical candidate.
    Current medicinal chemistry, 2004, Volume: 11, Issue:8

    Topics: Aniline Compounds; Animals; Antineoplastic Agents; Benzothiazoles; Cytochrome P-450 CYP1A1; Dose-Response Relationship, Drug; Drug Design; Prodrugs; Thiazoles; Time Factors

2004

Other Studies

22 other study(ies) available for thiazoles and 5f-203

ArticleYear
Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles.
    Journal of medicinal chemistry, 2001, Apr-26, Volume: 44, Issue:9

    Topics: Antineoplastic Agents; Blotting, Western; Cytochrome P-450 CYP1A1; Drug Screening Assays, Antitumor; Enzyme Induction; Humans; Stereoisomerism; Structure-Activity Relationship; Thiazoles; Tumor Cells, Cultured

2001
DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated in aryl hydrocarbon receptor deficient MCF-7 cells.
    British journal of cancer, 2003, Feb-24, Volume: 88, Issue:4

    Topics: Aryl Hydrocarbon Hydroxylases; Cell Cycle; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP1A1; Cytochrome P-450 CYP1B1; DNA Adducts; DNA Damage; Enzyme Induction; Humans; Receptors, Aryl Hydrocarbon; Signal Transduction; Thiazoles; Tumor Cells, Cultured

2003
Genotoxic profiling of MCF-7 breast cancer cell line elucidates gene expression modifications underlying toxicity of the anticancer drug 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole.
    Molecular pharmacology, 2003, Volume: 63, Issue:3

    Topics: Antineoplastic Agents; Breast Neoplasms; Female; Gene Expression; Gene Expression Profiling; Humans; Oligonucleotide Array Sequence Analysis; Reverse Transcriptase Polymerase Chain Reaction; Thiazoles; Tumor Cells, Cultured

2003
Induction of CYP1A1 in tumor cells by the antitumor agent 2-[4-amino-3-methylphenyl]-5-fluoro-benzothiazole: a potential surrogate marker for patient sensitivity.
    Molecular cancer therapeutics, 2003, Volume: 2, Issue:12

    Topics: Antineoplastic Agents; Base Sequence; Cytochrome P-450 CYP1A1; DNA Primers; Enzyme Induction; Humans; Polymerase Chain Reaction; RNA, Messenger; Thiazoles

2003
In vitro, in vivo, and in silico analyses of the antitumor activity of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazoles.
    Molecular cancer therapeutics, 2004, Volume: 3, Issue:12

    Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Cell Cycle; Comet Assay; Computational Biology; Cytochrome P-450 CYP1A1; DNA Adducts; DNA Damage; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Female; Humans; In Vitro Techniques; Membranes, Artificial; Mice; Mice, Nude; Thiazoles; Time Factors; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2004
The antitumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces NF-kappaB activity in drug-sensitive MCF-7 cells.
    Anti-cancer drugs, 2005, Volume: 16, Issue:2

    Topics: Antineoplastic Agents; Cell Line, Tumor; Drug Resistance, Neoplasm; Electrophoretic Mobility Shift Assay; Female; Genes, Reporter; Humans; Interleukin-6; Luciferases; NF-kappa B; Receptors, Aryl Hydrocarbon; Response Elements; Reverse Transcriptase Polymerase Chain Reaction; Thiazoles; Transcription, Genetic

2005
Anti-tumor drug candidate 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole induces single-strand breaks and DNA-protein cross-links in sensitive MCF-7 breast cancer cells.
    Cancer chemotherapy and pharmacology, 2006, Volume: 58, Issue:1

    Topics: Antineoplastic Agents; Breast Neoplasms; Cell Cycle; Cell Line, Tumor; DNA Damage; DNA Topoisomerases, Type I; DNA Topoisomerases, Type II; Humans; Thiazoles

2006
Differential gene expression as a potential classifier of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole-sensitive and -insensitive cell lines.
    Molecular pharmacology, 2006, Volume: 69, Issue:3

    Topics: Cell Line, Tumor; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Gene Expression; Gene Expression Profiling; Humans; Thiazoles

2006
Drug-induced expression of nonsteroidal anti-inflammatory drug-activated gene/macrophage inhibitory cytokine-1/prostate-derived factor, a putative tumor suppressor, inhibits tumor growth.
    The Journal of pharmacology and experimental therapeutics, 2006, Volume: 318, Issue:2

    Topics: Animals; Antibiotics, Antineoplastic; Antineoplastic Agents; Apoptosis; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Cycloheximide; Cytokines; Dactinomycin; Extracellular Signal-Regulated MAP Kinases; Gene Expression; Growth Differentiation Factor 15; Humans; Mice; Neoplasm Transplantation; Phosphorylation; RNA, Neoplasm; RNA, Small Interfering; Suppressor Factors, Immunologic; Thiazoles; Transplantation, Heterologous; Up-Regulation

2006
BRCA1 modulates sensitivity to 5F-203 by regulating xenobiotic stress-inducible protein levels and EROD activity.
    Cancer chemotherapy and pharmacology, 2008, Volume: 62, Issue:4

    Topics: Antineoplastic Agents; Breast Neoplasms; Cell Line, Tumor; Cell Survival; Cyclin-Dependent Kinase Inhibitor p21; Cytochrome P-450 CYP1A1; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Enzyme Induction; Female; Gene Expression Regulation, Neoplastic; Gene Silencing; Humans; Prodrugs; RNA, Small Interfering; Thiazoles; Tumor Suppressor Protein p53; Ubiquitin-Protein Ligases

2008
Preclinical toxicokinetic evaluation of phortress [2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole lysylamide dihydrochloride] in two rodent species.
    Pharmacology, 2009, Volume: 83, Issue:2

    Topics: Alkaline Phosphatase; Animals; beta-Galactosidase; Body Weight; Cytochrome P-450 CYP1A1; DNA Adducts; Drug Evaluation, Preclinical; Female; Genes, Reporter; Kidney; Liver; Lung; Male; Maximum Tolerated Dose; Mice; Mice, Inbred ICR; Organ Size; Prodrugs; Rats; Rats, Sprague-Dawley; Thiazoles

2009
2-(4-Amino-3-methylphenyl)-5-fluorobenzothiazole is a ligand and shows species-specific partial agonism of the aryl hydrocarbon receptor.
    Toxicology and applied pharmacology, 2009, May-15, Volume: 237, Issue:1

    Topics: Actins; Analysis of Variance; Animals; Antineoplastic Agents; Benzothiazoles; Cell Line, Tumor; Cytochrome P-450 CYP1A1; Enzyme Induction; Humans; Male; Rats; Rats, Wistar; Receptors, Aryl Hydrocarbon; RNA, Messenger; Species Specificity; Statistics, Nonparametric; Thiazoles

2009
CYP2S1 and CYP2W1 mediate 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (GW-610, NSC 721648) sensitivity in breast and colorectal cancer cells.
    Molecular cancer therapeutics, 2011, Volume: 10, Issue:10

    Topics: Antineoplastic Agents; Benzothiazoles; Breast Neoplasms; Cell Growth Processes; Cell Line, Tumor; Colorectal Neoplasms; Cytochrome P-450 CYP1A1; Cytochrome P-450 Enzyme System; Cytochrome P450 Family 2; Enzyme Induction; Female; Humans; Male; Thiazoles

2011
Bioactivation of fluorinated 2-aryl-benzothiazole antitumor molecules by human cytochrome P450s 1A1 and 2W1 and deactivation by cytochrome P450 2S1.
    Chemical research in toxicology, 2012, Aug-20, Volume: 25, Issue:8

    Topics: Antineoplastic Agents; Benzothiazoles; Biocatalysis; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP1A1; Cytochrome P-450 Enzyme System; Cytochrome P450 Family 2; DNA Adducts; Humans; Kinetics; Microsomes, Liver; Oxidation-Reduction; Spectrometry, Mass, Electrospray Ionization; Thiazoles

2012
Biomarkers of sensitivity to potent and selective antitumor 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F203) in ovarian cancer.
    Journal of cellular biochemistry, 2013, Volume: 114, Issue:10

    Topics: Antineoplastic Agents; Apoptosis; Blotting, Western; Caspase 3; Cell Line, Tumor; Cells, Cultured; Cyclin D1; Cytochrome P-450 CYP1A1; DNA Damage; Female; Flow Cytometry; Humans; Microscopy, Confocal; Ovarian Neoplasms; Phosphorylation; Reactive Oxygen Species; Thiazoles

2013
Molecular dynamics simulation studies for DNA sequence recognition by reactive metabolites of anticancer compounds.
    Journal of molecular recognition : JMR, 2014, Volume: 27, Issue:3

    Topics: Antineoplastic Agents; Binding Sites; Biotransformation; Cell Line, Tumor; Crystallography, X-Ray; Cytochrome P-450 CYP1A1; DNA; DNA Adducts; Flavonoids; Humans; Intercalating Agents; Kinetics; Molecular Docking Simulation; Molecular Dynamics Simulation; Nucleic Acid Conformation; Static Electricity; Thermodynamics; Thiazoles

2014
Aryl Hydrocarbon Receptor Ligand 5F 203 Induces Oxidative Stress That Triggers DNA Damage in Human Breast Cancer Cells.
    Chemical research in toxicology, 2015, May-18, Volume: 28, Issue:5

    Topics: Antineoplastic Agents; Apoptosis; Breast; Breast Neoplasms; Cell Line, Tumor; DNA Damage; Female; Gene Expression Regulation, Neoplastic; Humans; JNK Mitogen-Activated Protein Kinases; MCF-7 Cells; Oxidative Stress; p38 Mitogen-Activated Protein Kinases; Reactive Oxygen Species; Receptors, Aryl Hydrocarbon; Thiazoles

2015
Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery.
    Bioorganic & medicinal chemistry, 2015, Nov-01, Volume: 23, Issue:21

    Topics: Antineoplastic Agents; Benzothiazoles; Cell Line, Tumor; Cell Survival; Chromatography, High Pressure Liquid; Cytochrome P-450 CYP1A1; DNA Adducts; Drug Resistance, Neoplasm; Gene Expression Regulation; Histones; Humans; Hydrogels; Microscopy, Confocal; Prodrugs; Resveratrol; Stilbenes; Thiazoles

2015
In Vitro Antitumor Effects of AHR Ligands Aminoflavone (AFP 464) and Benzothiazole (5F 203) in Human Renal Carcinoma Cells.
    Journal of cellular biochemistry, 2017, Volume: 118, Issue:12

    Topics: Antineoplastic Agents; Carcinoma, Renal Cell; Cell Line, Tumor; Flavonoids; Humans; Kidney Neoplasms; Neoplasm Proteins; Receptors, Aryl Hydrocarbon; Signal Transduction; Thiazoles

2017
Putative tumor suppressor cytoglobin promotes aryl hydrocarbon receptor ligand-mediated triple negative breast cancer cell death.
    Journal of cellular biochemistry, 2019, Volume: 120, Issue:4

    Topics: Animals; Apoptosis; Basic Helix-Loop-Helix Transcription Factors; Caspase 3; Cathepsin B; Cell Line, Tumor; Cytoglobin; Female; Humans; Ligands; Mice; Mice, Nude; Receptors, Aryl Hydrocarbon; Thiazoles; Transfection; Triple Negative Breast Neoplasms; Tumor Burden; Tumor Suppressor Proteins; Xenograft Model Antitumor Assays

2019
Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery.
    International journal of nanomedicine, 2019, Volume: 14

    Topics: Antineoplastic Agents; Apoferritins; Cell Line, Tumor; Cytochrome P-450 Enzyme System; Drug Delivery Systems; Female; Humans; Receptors, Aryl Hydrocarbon; Thiazoles

2019
The antitumour activity of 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole in human gastric cancer models is mediated by AhR signalling.
    Journal of cellular and molecular medicine, 2020, Volume: 24, Issue:2

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Proliferation; Cytochrome P-450 Enzyme System; DNA Damage; Gene Expression Regulation, Neoplastic; Humans; Intracellular Space; Mice, Inbred BALB C; Mice, Nude; Receptors, Aryl Hydrocarbon; Signal Transduction; Stomach Neoplasms; Thiazoles

2020