quinazolines has been researched along with nolatrexed in 52 studies
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 23 (44.23) | 18.2507 |
2000's | 24 (46.15) | 29.6817 |
2010's | 4 (7.69) | 24.3611 |
2020's | 1 (1.92) | 2.80 |
Authors | Studies |
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Bartlett, CA; Boritzki, TJ; Hillard, JA; Howland, EF; Johnston, AL; Kosa, M; Margosiak, SA; Morse, CA; Shetty, BV; Webber, S | 1 |
Dash, AK; Tyle, P | 1 |
DeGoeij, K; Mester, J; Sluyser, M | 1 |
Buquet-Fagot, C; Djelloul, S; Gespach, C; Mester, J; Raymond, E | 1 |
Jansen, G; Peters, GJ; Pinedo, HM; Telleman, F; van der Wilt, CL; van Triest, B | 1 |
Takimoto, CH | 1 |
Clendeninn, NJ; Creaven, PJ; Dixon, M; Johnston, A; Loewen, GM; Meropol, NJ; Pendyala, L; Proefrock, A; Wu, EY | 1 |
Bailey, NP; Boddy, AV; Calvert, AH; Calvete, JA; Clendeninn, N; Green, M; Hines, J; Johnstone, A; Lind, MJ; Newell, DR; Rafi, I; Taylor, GA | 1 |
Banerjee, D; Bertino, JR; Capiaux, GM; Ercikan-Abali, EA; Liu-Chen, X; Tong, Y; Zhao, SC | 1 |
Chen, J; Ge, L; Hu, M; Li, Y; Roland, K; Roy, S; Tyle, P | 1 |
Bavetsias, V; Jackman, AL | 1 |
Banerjee, D; Bertino, JR; Ercikan-Abali, EA; Liu-Chen, X; Maley, F; Tong, Y; Zhao, SC | 1 |
Bailey, N; Balmanno, K; Boddy, AV; Calvert, AH; Calvete, JA; Jackson, RC; Lind, M; Rafi, I; Taylor, GA; Webber, S | 1 |
Brown, SL; Kim, JH; Kim, SH | 1 |
Boddy, AV; Calvert, AH; Calvete, JA; Clendeninn, N; Griffin, MJ; Hughes, AN; Johnston, A; Newell, DR; Rafi, I | 1 |
Boddy, A; Bowman, A; Byrne, B; Clendeninn, NJ; Jodrell, DI; Johnston, A; Rafi, I; Rye, R; Taylor, GA | 1 |
Clendennin, N; Johnston, A; Rudy, J; Stuart, K; Tessitore, J | 1 |
Bertino, JR; Sapse, AM; Sapse, DS; Tong, Y | 1 |
Chak, K; Chan, AT; Chao, Y; Huang, A; Johnson, P; Johnston, A; Lee, SD; Leung, TW; Lui, MC; Mok, TS; Yeo, W | 1 |
Canestrari, JG; McGuire, JJ; Nagel, GS | 1 |
Rastogi, S; Roy, S; Suryanarayanan, R; Tyle, P; Zamansky, I | 1 |
Danenberg, PV; Malli, H; Swenson, S | 1 |
Berger, FG; Fantz, C; Forsthoefel, A; Jennings, W; Kitchens, M; Lebioda, L; Minor, W; Phan, J; Shaw, D; Spencer, HT | 1 |
Boddy, AV; Calvert, AH; Griffin, MJ; Hughes, AN; Johnston, A; Kerr, B; Lee, C; Liang, B; Newell, DR | 1 |
Kuiper, CM; Peters, GJ; van der Wilt, CL | 1 |
Strømhaug, A; Warren, DJ | 1 |
Aherne, GW; Brunton, L; Jackman, AL; Monaghan, P; Titley, J; Valenti, M; Welsh, SJ | 1 |
Assaraf, YG; Drori, S; Jansen, G; Mauritz, R; Peters, GJ | 1 |
Cassidy, J | 1 |
Ackland, SP; Sakoff, JA | 1 |
Ablett, S; Boddy, AV; Brampton, M; Clendeninn, N; Estlin, EJ; Hobson, R; Johnston, A; Kohler, J; Lashford, L; Lewis, IJ; McDowell, H; Morland, B; Newell, DR; Pearson, AD; Pinkerton, CR; Pitsiladis, M; Price, L; Taylor, GA | 1 |
Chao, Y; Chen, FD; Chi, KH; Chou, SL; Liu, RS; Wang, HE; Wang, YS; Yen, SH | 1 |
Backus, HH; Jansen, G; Kuiper, CM; Peters, GJ; Pinedo, HM; van Groeningen, CJ; Wouters, D | 1 |
Niculescu-Duvaz, I | 1 |
Backus, HH; Kuiper, CM; Peters, GJ; Pinedo, HM; van der Wilt, CL; van Groeningen, CJ; Wouters, D | 1 |
Belpomme, D; Clendeninn, N; Domenge, C; Humblet, Y; Johnston, A; Kelly, C; Penning, C; Pivot, X; Ruxer, R; Schneider, M; Stern, J; Tortochaux, J; Wadler, S | 1 |
Aboagye, E; Boddy, AV; Calvert, AH; Gunn, RN; Hughes, AN; Newell, DR; Osman, S; Price, PM; Rafi, I; Taylor, GA; Wells, P | 1 |
Callender, MA; Chu, E; Farrell, MP; Schmitz, JC | 1 |
Ackland, SP; Howitt, IJ; McCluskey, A; Sakoff, JA | 1 |
Li, YL; Wu, SG | 1 |
Fukushima, M; Hoogeland, MF; Peters, GJ; Temmink, OH | 1 |
Aboagye, E; Pillai, RG; Price, P; Yau, K | 1 |
Assaraf, YG; Berman, B; Bram, E; Ifergan, I; Jansen, G; Shafran, A | 1 |
Clendeninn, N; Dancey, J; Hamburg, S; Hochster, H; Jhawer, M; Mani, S; Rosen, L; Tempero, M | 1 |
Croitoru, A; Feld, R; Feun, L; Gallo, J; Gish, RG; Jeziorski, K; Kennealey, GT; Lazar, L; Leighton, J; Porta, C; Ruff, P | 1 |
Chen, SZ; Wang, SM; Zhang, JR | 1 |
Shao, CF; Wan, SH; Wang, GF; Wu, SY; Xu, W; Zhang, JJ; Zhang, JY | 1 |
Jing, CQ; Li, LP; Tian, SB | 1 |
Lin, J; Wang, L; Xie, B; Xu, T; Zhang, W; Zheng, J; Zhou, J | 1 |
Contestabile, R; CutruzzolĂ , F; Daidone, F; Fiascarelli, A; Giardina, G; Koes, DR; Marani, M; McDermott, LA; Montini, G; Paiardini, A; Paone, A; Parroni, A; Rinaldo, S | 1 |
Chen, D; Jansson, A; Larsson, A; Nordlund, P; Sim, D | 1 |
Chen, G; Maiti, S; MaitiDutta, S | 1 |
6 review(s) available for quinazolines and nolatrexed
Article | Year |
---|---|
Antifolates in clinical development.
Topics: Aminopterin; Animals; Antimetabolites, Antineoplastic; Clinical Trials as Topic; Drug Design; Enzyme Inhibitors; Folic Acid Antagonists; Glutamates; Guanine; Humans; Indoles; Isoindoles; Pemetrexed; Pyrimidines; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase | 1997 |
Nonpolyglutamatable antifolates as inhibitors of thymidylate synthase (TS) and potential antitumour agents.
Topics: Antimetabolites, Antineoplastic; Cell Division; Excitatory Amino Acid Antagonists; Folic Acid Antagonists; Humans; Indoles; Peptide Synthases; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1998 |
Thymidylate synthase inhibitors.
Topics: Animals; Antimetabolites, Antineoplastic; Colorectal Neoplasms; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Indoles; Isoindoles; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase | 1999 |
Thymidylate synthase inhibitors in colorectal cancer.
Topics: Antineoplastic Agents; Clinical Trials as Topic; Colorectal Neoplasms; Enzyme Inhibitors; Folic Acid; Glutamates; Guanine; Humans; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase | 2000 |
Thymitaq (Zarix).
Topics: Animals; Antimetabolites, Antineoplastic; Clinical Trials as Topic; Contraindications; Enzyme Inhibitors; Humans; Neoplasms; Quinazolines; Radiation-Sensitizing Agents; Structure-Activity Relationship; Thymidylate Synthase | 2001 |
Thymidylate synthase inhibitors as anticancer agents: from bench to bedside.
Topics: Antineoplastic Agents; Enzyme Inhibitors; Humans; Indoles; Isoindoles; Neoplasms; Quinazolines; Randomized Controlled Trials as Topic; Thiophenes; Thymidylate Synthase | 2003 |
13 trial(s) available for quinazolines and nolatrexed
Article | Year |
---|---|
Initial clinical trial and pharmacokinetics of Thymitaq (AG337) by 10-day continuous infusion in patients with advanced solid tumors.
Topics: Adult; Aged; Antimetabolites, Antineoplastic; Area Under Curve; Carcinoma, Squamous Cell; Chromatography, High Pressure Liquid; Dose-Response Relationship, Drug; Humans; Infusions, Intravenous; Middle Aged; Neoplasms; Quinazolines | 1998 |
Preclinical and phase I clinical studies with the nonclassical antifolate thymidylate synthase inhibitor nolatrexed dihydrochloride given by prolonged administration in patients with solid tumors.
Topics: Adult; Aged; Animals; Antimetabolites, Antineoplastic; Evaluation Studies as Topic; Female; Folic Acid Antagonists; Humans; Male; Mice; Middle Aged; Neoplasms; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1998 |
Clinical pharmacokinetic and pharmacodynamic studies with the nonclassical antifolate thymidylate synthase inhibitor 3, 4-dihydro-2-amino-6-methyl-4-oxo-5-(4-pyridylthio)-quinazolone dihydrochloride (AG337) given by 24-hour continuous intravenous infusion
Topics: Antimetabolites, Antineoplastic; Drug Administration Schedule; Drug Eruptions; Enzyme Inhibitors; Female; Folic Acid Antagonists; Humans; Infusions, Intravenous; Male; Neoplasms; Quinazolines; Thymidylate Synthase | 1995 |
Phase I studies with the nonclassical antifolate nolatrexed dihydrochloride (AG337, THYMITAQ) administered orally for 5 days.
Topics: Administration, Oral; Adult; Aged; Antimetabolites, Antineoplastic; Biological Availability; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Food-Drug Interactions; Humans; Infusions, Intravenous; Male; Middle Aged; Neoplasms; Quinazolines | 1999 |
A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration.
Topics: Administration, Oral; Adult; Antimetabolites, Antineoplastic; Biological Availability; Deoxyuridine; Dose-Response Relationship, Drug; Drug Administration Schedule; Exanthema; Humans; Liver Function Tests; Nausea; Neoplasms; Neutropenia; Quinazolines; Stomatitis; Thrombocytopenia; Thymidylate Synthase; Vomiting | 1999 |
A Phase II trial of nolatrexed dihydrochloride in patients with advanced hepatocellular carcinoma.
Topics: Adult; Aged; Antimetabolites, Antineoplastic; Carcinoma, Hepatocellular; Female; Humans; Liver Neoplasms; Male; Middle Aged; Neoplasm Staging; Quinazolines; Survival Analysis; Thymidylate Synthase | 1999 |
A multi-centre randomized phase II study of nolatrexed versus doxorubicin in treatment of Chinese patients with advanced hepatocellular carcinoma.
Topics: Adult; Aged; Antimetabolites, Antineoplastic; Antineoplastic Agents; Carcinoma, Hepatocellular; Doxorubicin; Female; Humans; Infusions, Intravenous; Liver Neoplasms; Male; Middle Aged; Quinazolines; Survival Analysis | 1999 |
Clinical pharmacokinetic and in vitro combination studies of nolatrexed dihydrochloride (AG337, Thymitaq) and paclitaxel.
Topics: Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Area Under Curve; Drug Monitoring; Female; Head and Neck Neoplasms; Humans; Male; Middle Aged; Paclitaxel; Quinazolines; Tumor Cells, Cultured | 2000 |
A phase I study of nolatrexed dihydrochloride in children with advanced cancer. A United Kingdom Children's Cancer Study Group Investigation.
Topics: Acute Disease; Adolescent; Antimetabolites, Antineoplastic; Child; Child, Preschool; Enzyme Inhibitors; Female; Humans; Infant; Leukemia, Myeloid; Male; Neoplasms; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines | 2001 |
Result of two randomized trials comparing nolatrexed (Thymitaq) versus methotrexate in patients with recurrent head and neck cancer.
Topics: Adult; Aged; Aged, 80 and over; Antimetabolites, Antineoplastic; Carcinoma, Squamous Cell; Diarrhea; Enzyme Inhibitors; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Middle Aged; Neoplasm Recurrence, Local; Neutropenia; Quinazolines; Thymidylate Synthase; Treatment Outcome | 2001 |
Phase II trial of nolatrexed dihydrochloride [Thymitaq, AG 337] in patients with advanced hepatocellular carcinoma.
Topics: Adult; Aged; Aged, 80 and over; Antimetabolites, Antineoplastic; Carcinoma, Hepatocellular; Drug Administration Schedule; Exanthema; Female; Humans; Infusions, Intravenous; Liver Neoplasms; Male; Metabolic Clearance Rate; Middle Aged; Nausea; Quinazolines; Stomatitis; Survival Analysis; Time Factors; Treatment Outcome | 2007 |
Phase III randomized controlled trial comparing the survival of patients with unresectable hepatocellular carcinoma treated with nolatrexed or doxorubicin.
Topics: Adult; Aged; Carcinoma, Hepatocellular; Dose-Response Relationship, Drug; Doxorubicin; Drug Administration Schedule; Female; Humans; Infusions, Intravenous; Liver Neoplasms; Male; Maximum Tolerated Dose; Middle Aged; Neoplasm Staging; Palliative Care; Quality of Life; Quinazolines; Risk Assessment; Survival Analysis; Terminally Ill | 2007 |
Metastatic nasopharyngeal carcinoma outcomes in patients on cisplatin with nolatrexed or 5-fluorouracil.
Topics: Adult; Aged; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Carcinoma; Cisplatin; Disease-Free Survival; Female; Fluorouracil; Humans; Male; Middle Aged; Nasopharyngeal Carcinoma; Nasopharyngeal Neoplasms; Neoplasm Recurrence, Local; Quinazolines; Survival Rate; Treatment Outcome | 2014 |
33 other study(ies) available for quinazolines and nolatrexed
Article | Year |
---|---|
AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies.
Topics: Administration, Oral; Animals; Antimetabolites, Antineoplastic; Cell Cycle; Enzyme Inhibitors; Folic Acid Antagonists; Growth Inhibitors; Humans; Leukemia L1210; Leukemia L5178; Mice; Quinazolines; Rats; Solubility; Thymidylate Synthase | 1996 |
Solid-state characterization of AG337 (Thymitaq), a novel antitumor drug.
Topics: Antimetabolites, Antineoplastic; Calorimetry, Differential Scanning; Crystallization; Quinazolines; Thermogravimetry; X-Ray Diffraction | 1996 |
Modulation of [5-125I]iododeoxyuridine incorporation into tumour and normal tissue DNA by methotrexate and thymidylate synthase inhibitors.
Topics: Animals; Antimetabolites, Antineoplastic; Dihydrouracil Dehydrogenase (NAD+); DNA, Neoplasm; Female; Fluorouracil; Idoxuridine; Intestine, Small; Iodine Radioisotopes; Liver; Mammary Neoplasms, Experimental; Methotrexate; Mice; Oxidoreductases; Oxidoreductases Acting on CH-CH Group Donors; Quinazolines; Thiophenes; Thymidylate Synthase; Uracil | 1996 |
Synergy between the non-classical thymidylate synthase inhibitor AG337 (Thymitaq) and cisplatin in human colon and ovarian cancer cells.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Cisplatin; Colonic Neoplasms; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Drug Synergism; Female; Fluorouracil; Humans; Ovarian Neoplasms; Quinazolines; Tumor Cells, Cultured | 1996 |
Cross-resistance to antifolates in multidrug resistant cell lines with P-glycoprotein or multidrug resistance protein expression.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Blotting, Western; Cell Division; Drug Resistance, Multiple; Fluorodeoxyuridylate; Fluorouracil; Folic Acid Antagonists; Gene Expression Regulation; Humans; Indoles; Isoindoles; Methotrexate; Peptide Synthases; Polymerase Chain Reaction; Quinazolines; RNA, Messenger; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1997 |
Isolation and characterization of thymitaq (AG337) and 5-fluoro-2-deoxyuridylate-resistant mutants of human thymidylate synthase from ethyl methanesulfonate-exposed human sarcoma HT1080 cells.
Topics: Cloning, Molecular; Drug Resistance; Enzyme Inhibitors; Escherichia coli; Ethyl Methanesulfonate; Fluorodeoxyuridylate; Folic Acid; Folic Acid Antagonists; Gene Expression Regulation, Enzymologic; Humans; Kinetics; Mutagenesis; Mutagenesis, Site-Directed; Polymorphism, Single-Stranded Conformational; Quinazolines; Recombinant Proteins; Sarcoma; Thymidylate Synthase; Tumor Cells, Cultured | 1998 |
Determination of absorption characteristics of AG337, a novel thymidylate synthase inhibitor, using a perfused rat intestinal model.
Topics: Animals; Biological Transport; Cell Membrane Permeability; Drug Stability; Duodenum; Enzyme Inhibitors; Hydrogen-Ion Concentration; Ileum; Intestinal Absorption; Jejunum; Male; Nucleosides; Perfusion; Purines; Quinazolines; Rats; Rats, Sprague-Dawley; Sodium; Temperature; Thymidylate Synthase | 1998 |
Probing the folate-binding site of human thymidylate synthase by site-directed mutagenesis. Generation of mutants that confer resistance to raltitrexed, Thymitaq, and BW1843U89.
Topics: Animals; Antimetabolites, Antineoplastic; Binding Sites; Bone Marrow Cells; Drug Resistance; Folic Acid; Folic Acid Antagonists; Granulocytes; Humans; Indoles; Isoindoles; Isoleucine; Kinetics; Macrophages; Mice; Models, Molecular; Mutagenesis, Site-Directed; Quinazolines; Recombinant Proteins; Stem Cells; Thiophenes; Thymidylate Synthase | 1998 |
The potentiation of radiation response in human colon carcinoma cells in vitro and murine lymphoma in vivo by AG337 (Thymitaq), a novel thymidylate synthase inhibitor.
Topics: Animals; Antimetabolites, Antineoplastic; Cell Survival; Drug Therapy, Combination; Enzyme Inhibitors; HT29 Cells; Humans; Leukemia L5178; Male; Mice; Mice, Inbred DBA; Quinazolines; Thymidylate Synthase | 1998 |
Ab initio studies of some amino acid residue complexes with 4-mercaptopyridine as a model for thymitaq (AG337), an inhibitor of thymidylate synthase.
Topics: Acetamides; Amino Acids; Benzene; Binding Sites; Electrons; Hydrogen; Ions; Methane; Models, Chemical; Pentanes; Pyridines; Quinazolines; Thermodynamics; Thymidylate Synthase | 1999 |
Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines.
Topics: Cell Cycle; Cell Division; Culture Media; Drug Resistance; Enzyme Inhibitors; Fetal Blood; Head and Neck Neoplasms; Humans; Hypoxanthine; Inhibitory Concentration 50; Leucovorin; Leukemia; Methotrexate; Quinazolines; Thymidine; Thymidine Phosphorylase; Thymidylate Synthase; Tumor Cells, Cultured | 1999 |
Solid-state phase transitions of AG337, an antitumor agent.
Topics: Antimetabolites, Antineoplastic; Calorimetry, Differential Scanning; Drug Storage; Humidity; Quinazolines; Spectroscopy, Fourier Transform Infrared; Temperature; Thermogravimetry; X-Ray Diffraction | 1999 |
Drug-resistant variants of Escherichia coli thymidylate synthase: effects of substitutions at Pro-254.
Topics: Amino Acid Substitution; Crystallography, X-Ray; Deoxyuracil Nucleotides; Drug Resistance; Drug Resistance, Microbial; Enzyme Inhibitors; Escherichia coli; Fluorodeoxyuridylate; Folic Acid Antagonists; Humans; Kinetics; Mutation; Proline; Protein Conformation; Quinazolines; Tetrahydrofolates; Thymidylate Synthase; Transfection | 2000 |
Combination studies of antifolates with 5-fluorouracil in colon cancer cell lines.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Cell Division; Colonic Neoplasms; DNA Damage; Fluorouracil; Folic Acid Antagonists; Glutamates; Guanine; Humans; Indoles; Isoindoles; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1999 |
A comparison of the effects of nine folate analogs on early and late murine hematopoietic progenitor cells in vitro.
Topics: Aminopterin; Animals; Cell Division; Cells, Cultured; Enzyme Inhibitors; Female; Folic Acid; Folic Acid Antagonists; Hematopoietic Stem Cells; Methotrexate; Mice; Mice, Inbred BALB C; Quinazolines; Tetrahydrofolates; Thiophenes; Trimetrexate | 2000 |
Comparison of thymidylate synthase (TS) protein up-regulation after exposure to TS inhibitors in normal and tumor cell lines and tissues.
Topics: Analysis of Variance; Animals; Antimetabolites, Antineoplastic; Antineoplastic Agents; Blotting, Western; Dose-Response Relationship, Drug; Enzyme-Linked Immunosorbent Assay; Female; Fibroblasts; Flow Cytometry; Fluorouracil; Glutamates; Guanine; Humans; Indoles; Inhibitory Concentration 50; Isoindoles; Mice; Mice, Inbred DBA; Microscopy, Confocal; Neoplasm Transplantation; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured; Up-Regulation | 2000 |
Clustering of mutations in the first transmembrane domain of the human reduced folate carrier in GW1843U89-resistant leukemia cells with impaired antifolate transport and augmented folate uptake.
Topics: Antimetabolites, Antineoplastic; Biological Transport; Blotting, Northern; Blotting, Southern; Blotting, Western; Carrier Proteins; Cell Division; Cell Membrane; Chlorides; DNA Mutational Analysis; DNA, Complementary; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Enzyme Inhibitors; Exons; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Inhibitory Concentration 50; Isoindoles; Kinetics; Leucovorin; Leukemia; Membrane Proteins; Membrane Transport Proteins; Methotrexate; Mutagenesis, Site-Directed; Mutation; Polymorphism, Single-Stranded Conformational; Protein Structure, Secondary; Protein Structure, Tertiary; Quinazolines; Recombinant Proteins; Reduced Folate Carrier Protein; Thymidylate Synthase; Time Factors; Transfection; Trimetrexate; Tumor Cells, Cultured | 2000 |
Thymidylate synthase inhibition induces S-phase arrest, biphasic mitochondrial alterations and caspase-dependent apoptosis in leukaemia cells.
Topics: Animals; Antimetabolites, Antineoplastic; Caspases; Cell Membrane Permeability; Drug Screening Assays, Antitumor; Enzyme Activation; Enzyme Inhibitors; HL-60 Cells; Humans; Leukemia L1210; Mitochondria; Neoplasm Proteins; Quinazolines; S Phase; Thymidylate Synthase; Time Factors | 2000 |
Preclinical evaluation of locoregional delivery of radiolabeled iododeoxyuridine and thymidylate synthase inhibitor in a hepatoma model.
Topics: Animals; DNA, Neoplasm; Dose-Response Relationship, Drug; Drug Evaluation; Drug Synergism; Drug Therapy, Combination; Female; Humans; Idoxuridine; Iodine Radioisotopes; Liver Neoplasms, Experimental; Male; Mice; Mice, Inbred BALB C; Mice, Inbred C3H; Neoplasm Transplantation; Quinazolines; Rats; Rats, Sprague-Dawley; Thymidylate Synthase; Tumor Cells, Cultured | 2001 |
Differences in the induction of DNA damage, cell cycle arrest, and cell death by 5-fluorouracil and antifolates.
Topics: Antimetabolites, Antineoplastic; Apoptosis; Cell Cycle; Colonic Neoplasms; DNA Damage; DNA, Neoplasm; Dose-Response Relationship, Drug; Enzyme Inhibitors; Flow Cytometry; Fluorometry; Fluorouracil; Folic Acid Antagonists; Humans; Hydroxymethyl and Formyl Transferases; Phosphoribosylglycinamide Formyltransferase; Quinazolines; RNA, Neoplasm; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Tumor Cells, Cultured | 2000 |
Thymidylate synthase inhibition induces p53 dependent and independent cell death.
Topics: Antimetabolites, Antineoplastic; Apoptosis; Caspase 3; Caspases; Colonic Neoplasms; DNA Damage; Enzyme Inhibitors; Fas Ligand Protein; Fluorouracil; Folic Acid Antagonists; Glutamates; Guanine; Humans; Membrane Glycoproteins; Pemetrexed; Proto-Oncogene Proteins c-bcl-2; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured; Tumor Suppressor Protein p53 | 2000 |
2-[11C]thymidine positron emission tomography as an indicator of thymidylate synthase inhibition in patients treated with AG337.
Topics: Adult; Aged; Antimetabolites, Antineoplastic; Area Under Curve; Carbon Radioisotopes; Case-Control Studies; Enzyme Inhibitors; Female; Gastrointestinal Neoplasms; Humans; Liver; Male; Middle Aged; Quinazolines; Regression Analysis; Thymidine; Thymidylate Synthase; Tomography, Emission-Computed | 2003 |
Serine/threonine protein phosphatase inhibition enhances the effect of thymidylate synthase inhibition.
Topics: Antimetabolites, Antineoplastic; Cantharidin; Carcinoma; Cell Cycle; Cell Division; Cell Line, Tumor; Colorectal Neoplasms; DNA, Neoplasm; Drug Synergism; Enzyme Inhibitors; HT29 Cells; Humans; Phosphoprotein Phosphatases; Quinazolines; Thymidylate Synthase | 2004 |
[Effects of nolatrexed on thymidylate synthase protein expression].
Topics: Cell Line; Colorectal Neoplasms; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Hepatocytes; Humans; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 2004 |
Low folate conditions may enhance the interaction of trifluorothymidine with antifolates in colon cancer cells.
Topics: Antimetabolites; Colonic Neoplasms; DNA Damage; Drug Interactions; Folic Acid; Folic Acid Antagonists; Homeostasis; Humans; Indoles; Isoindoles; Quinazolines; Thiophenes; Trifluridine; Tumor Cells, Cultured | 2006 |
Elevation of radiolabelled thymidine uptake in RIF-1 fibrosarcoma and HT29 colon adenocarcinoma cells after treatment with thymidylate synthase inhibitors.
Topics: Adenocarcinoma; Biological Transport, Active; Cell Line, Tumor; Cell Survival; Cisplatin; Colonic Neoplasms; Enzyme Inhibitors; Fibrosarcoma; Fluorouracil; HT29 Cells; Humans; Quinazolines; Radionuclide Imaging; Radiopharmaceuticals; Thymidine; Thymidylate Synthase; Time Factors; Tritium | 2006 |
Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates.
Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Transport; Cell Line; Cell Proliferation; Cell Survival; Cisplatin; Dose-Response Relationship, Drug; Doxorubicin; Drug Resistance, Neoplasm; Fluorouracil; Folic Acid Antagonists; Heterocyclic Compounds, 3-Ring; Humans; Indoles; Lipids; Molecular Structure; Mutation; Neoplasm Proteins; Paclitaxel; Pyrimethamine; Pyrimidines; Quinazolines; Rhodamines; Transfection; Trimetrexate | 2006 |
[Preparation of long-circulating nolatrexed dihydrochloride liposomes and its antitumor activity].
Topics: Animals; Antineoplastic Agents; Delayed-Action Preparations; Drug Carriers; Drug Compounding; Liposomes; Liver Neoplasms, Experimental; Mice; Quinazolines | 2008 |
[Measurement of plasma concentration and bioavailability of nolatrexed dihydrochloride in mice].
Topics: Animals; Antimetabolites, Antineoplastic; Biological Availability; Chromatography, High Pressure Liquid; Male; Mass Spectrometry; Mice; Mice, Inbred C57BL; Quinazolines | 2008 |
[Effects of RNA interference and nolatrexed on thymidylate synthase expression and cell proliferation of human colorectal carcinoma LOVO cells].
Topics: Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Colorectal Neoplasms; Humans; Quinazolines; RNA Interference; Thymidylate Synthase | 2012 |
Screening and in vitro testing of antifolate inhibitors of human cytosolic serine hydroxymethyltransferase.
Topics: Folic Acid Antagonists; Glycine Hydroxymethyltransferase; Humans; Methotrexate; Molecular Docking Simulation; Quinazolines; Tetrahydrofolates; Thiophenes | 2015 |
Structural analyses of human thymidylate synthase reveal a site that may control conformational switching between active and inactive states.
Topics: Allosteric Site; Amino Acid Substitution; Binding Sites; Catalytic Domain; Crystallography, X-Ray; Deoxyuracil Nucleotides; Dimerization; Enzyme Activation; Enzyme Stability; Folic Acid Antagonists; Humans; Ligands; Models, Molecular; Mutagenesis, Site-Directed; Mutation; Peptide Fragments; Protein Conformation; Protein Folding; Quinazolines; Recombinant Proteins; Thiophenes; Thymidylate Synthase | 2017 |
Regulations of expressions of rat/human sulfotransferases by anticancer drug, nolatrexed, and micronutrients.
Topics: Animals; Antimetabolites, Antineoplastic; Arylsulfotransferase; Blotting, Western; Cell Cycle; Dose-Response Relationship, Drug; Female; Folic Acid; Hep G2 Cells; Humans; Leucovorin; Male; Methotrexate; Micronutrients; Quinazolines; Rats; Rats, Sprague-Dawley; RNA, Messenger; Sex Factors; Sulfotransferases | 2022 |