Page last updated: 2024-08-21

quinazolines and 1843u89

quinazolines has been researched along with 1843u89 in 33 studies

Research

Studies (33)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's25 (75.76)18.2507
2000's8 (24.24)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Cieśla, J; Maley, F; Montfort, WR; Weichsel, A1
Erlichman, C; Mandelbaum, S; Mitrovski, B; Pressacco, J1
Banks, SD; Barrett, LL; Dickerson, S; Pendergast, W; Smith, GK; Waters, KA1
Dev, IK; Dickerson, SH; Duch, DS; Ferone, R; Pendergast, W; Smith, GK1
Erlichman, C; Mitrovski, B1
Dallas, WS; Dev, IK; Ferone, R; Hanlon, M; McKee, DD; Yates, BB1
Banks, S; Dev, IK; Dickerson, SH; Duch, DS; Ferone, R; Heath, LS; Humphreys, J; Knick, V; Pendergast, W; Singer, S1
Amyx, H; Boytos, CM; Duch, DS; Ferone, R; Smith, GK; Wilson, HR1
Calvert, AH; Jackman, AL1
Chen, CH; Davis, RA; Maley, F1
Ferone, R; Hanlon, MH1
Stout, TJ; Stroud, RM1
Montfort, WR; Weichsel, A1
Bertino, JR; Ercikan, E; Gorlick, R; Longo, GS; Tong, WP1
Jansen, G; Peters, GJ; Pinedo, HM; Telleman, F; van der Wilt, CL; van Triest, B1
Dolnick, BJ; Lu, K; Rustum, YM; Yin, MB1
Takimoto, CH1
Hannun, YA; Jayadev, S; Laethem, RM; Sexton, CJ; Smith, GK; Strum, JC; Sundseth, R1
Banerjee, D; Bertino, JR; Ercikan-Abali, EA; Liu-Chen, X; Maley, F; Tong, Y; Zhao, SC1
Bertino, JR; Li, WW; Tong, WP1
Assaraf, YG; Borst, P; Broxterman, HJ; Hooijberg, JH; Jansen, G; Kool, M; Noordhuis, P; Peters, GJ; Pinedo, HM; Scheper, RJ1
Jansen, G; Peters, GJ; Pinedo, HM; Smid, K; Smitskamp-Wilms, E1
Newell, DR1
Danenberg, PV; Malli, H; Swenson, S1
Jiang, L; Lee, PC; Rathod, PK; White, J1
Kuiper, CM; Peters, GJ; van der Wilt, CL1
Aherne, GW; Brunton, L; Jackman, AL; Monaghan, P; Titley, J; Valenti, M; Welsh, SJ1
Assaraf, YG; Drori, S; Jansen, G; Mauritz, R; Peters, GJ1
Burris, H; Goetz, A; Hohneker, JA; Johnson, TR; Lampkin, T; Rowinsky, EK; Sailstad, J; Schwartz, G; Smetzer, L; Von Hoff, DD1
Callender, MA; Chu, E; Farrell, MP; Schmitz, JC1
Abbott, E; Brown, EN; Colagiovanni, DB; Desjardins, J; Drolet, DW; Emerson, DL1
Fukushima, M; Hoogeland, MF; Peters, GJ; Temmink, OH1
Aispuro-Hernandez, E; Arvizu-Flores, AA; Garcia-Orozco, KD; Maley, F; Rojo-Domínguez, A; Sotelo-Mundo, RR; Valenzuela-Soto, E; Varela-Romero, A; Velazquez-Contreras, EF; Yepiz-Plascencia, G1

Reviews

5 review(s) available for quinazolines and 1843u89

ArticleYear
Folate-based thymidylate synthase inhibitors as anticancer drugs.
    Annals of oncology : official journal of the European Society for Medical Oncology, 1995, Volume: 6, Issue:9

    Topics: Antineoplastic Agents; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Indoles; Isoindoles; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase

1995
Antifolates in clinical development.
    Seminars in oncology, 1997, Volume: 24, Issue:5 Suppl 18

    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
Clinical pharmacokinetics of antitumor antifolates.
    Seminars in oncology, 1999, Volume: 26, Issue:2 Suppl 6

    Topics: Antimetabolites, Antineoplastic; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Isoindoles; Methotrexate; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase

1999
Thymidylate synthase inhibitors.
    Seminars in oncology, 1999, Volume: 26, Issue:6

    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 as anticancer agents: from bench to bedside.
    Cancer chemotherapy and pharmacology, 2003, Volume: 52 Suppl 1

    Topics: Antineoplastic Agents; Enzyme Inhibitors; Humans; Indoles; Isoindoles; Neoplasms; Quinazolines; Randomized Controlled Trials as Topic; Thiophenes; Thymidylate Synthase

2003

Trials

1 trial(s) available for quinazolines and 1843u89

ArticleYear
A phase I and pharmacokinetic study of 1843U89, a noncompetitive inhibitor of thymidylate synthase, in patients with advanced solid malignancies.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2001, Volume: 7, Issue:7

    Topics: Adult; Aged; Antineoplastic Agents; Area Under Curve; Dose-Response Relationship, Drug; Enzyme Inhibitors; Exanthema; Female; Folic Acid; Humans; Indoles; Infusions, Intravenous; Isoindoles; Male; Middle Aged; Mouth Mucosa; Neoplasms; Neutropenia; Quinazolines; Stomatitis; Thymidylate Synthase

2001

Other Studies

27 other study(ies) available for quinazolines and 1843u89

ArticleYear
Promotion of purine nucleotide binding to thymidylate synthase by a potent folate analogue inhibitor, 1843U89.
    Proceedings of the National Academy of Sciences of the United States of America, 1995, Apr-11, Volume: 92, Issue:8

    Topics: Circular Dichroism; Crystallography, X-Ray; Escherichia coli; Folic Acid; Hydrogen Bonding; Indoles; Isoindoles; Models, Molecular; Molecular Sequence Data; Purine Nucleotides; Quinazolines; Recombinant Proteins; Thymidylate Synthase

1995
Biochemical effects of folate-based inhibitors of thymidylate synthase in MGH-U1 cells.
    Cancer chemotherapy and pharmacology, 1994, Volume: 35, Issue:2

    Topics: Cell Survival; Deoxyuracil Nucleotides; Deoxyuridine; Folic Acid; Folic Acid Antagonists; Glutamates; Humans; In Vitro Techniques; Indoles; Isoindoles; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured; Urinary Bladder Neoplasms

1994
Destruction of WiDr multicellular tumor spheroids with the novel thymidylate synthase inhibitor 1843U89 at physiological thymidine concentrations.
    Cancer chemotherapy and pharmacology, 1994, Volume: 33, Issue:6

    Topics: Antineoplastic Agents; Carcinoma; Cell Division; Colonic Neoplasms; Humans; Indoles; Isoindoles; Methotrexate; Quinazolines; Thymidine; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured

1994
Benzo[f]quinazoline inhibitors of thymidylate synthase: methyleneamino-linked aroylglutamate derivatives.
    Journal of medicinal chemistry, 1994, Mar-18, Volume: 37, Issue:6

    Topics: Adenocarcinoma; Antineoplastic Agents; Breast Neoplasms; Colonic Neoplasms; Glutamates; Humans; Indoles; Isoindoles; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured

1994
Comparative cytotoxicity of folate-based inhibitors of thymidylate synthase and 5-fluorouracil +/- leucovorin in MGH-U1 cells.
    Cancer chemotherapy and pharmacology, 1994, Volume: 34, Issue:1

    Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cell Survival; Drug Screening Assays, Antitumor; Fluorouracil; Folic Acid; Glutamates; Humans; Indoles; Isoindoles; Leucovorin; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured; Urinary Bladder Neoplasms

1994
Mode of binding of folate analogs to thymidylate synthase. Evidence for two asymmetric but interactive substrate binding sites.
    The Journal of biological chemistry, 1994, Jan-21, Volume: 269, Issue:3

    Topics: Binding Sites; Carbon Radioisotopes; Deoxyuracil Nucleotides; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Isoindoles; Kinetics; Macromolecular Substances; Mathematics; Protein Binding; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase

1994
Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase.
    Cancer research, 1993, Feb-15, Volume: 53, Issue:4

    Topics: Animals; Binding, Competitive; Breast Neoplasms; Cell Division; Colonic Neoplasms; Female; Humans; Indoles; Isoindoles; Leucovorin; Leukemia L1210; Leukemia, T-Cell; Methotrexate; Quinazolines; Structure-Activity Relationship; Subrenal Capsule Assay; Tetrahydrofolates; Thymidylate Synthase

1993
Enhanced antitumor activity for the thymidylate synthase inhibitor 1843U89 through decreased host toxicity with oral folic acid.
    Cancer research, 1995, Dec-15, Volume: 55, Issue:24

    Topics: Animals; Body Weight; Dogs; Dose-Response Relationship, Drug; Enzyme Inhibitors; Folic Acid; Humans; Indoles; Intestinal Diseases; Isoindoles; Leucovorin; Mice; Neoplasms, Experimental; Osteosarcoma; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured

1995
Thermodynamic stabilization of nucleotide binding to thymidylate synthase by a potent benzoquinazoline folate analogue inhibitor.
    Biochemistry, 1996, Jul-02, Volume: 35, Issue:26

    Topics: Calorimetry, Differential Scanning; Folic Acid Antagonists; Indoles; Isoindoles; Nucleotides; Protein Denaturation; Quinazolines; Substrate Specificity; Thermodynamics; Thymidylate Synthase

1996
In vitro uptake, anabolism, and cellular retention of 1843U89 and other benzoquinazoline inhibitors of thymidylate synthase.
    Cancer research, 1996, Jul-15, Volume: 56, Issue:14

    Topics: Animals; Carcinoma; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Intestinal Neoplasms; Isoindoles; Leucovorin; Liver; Metabolic Clearance Rate; Peptide Synthases; Polyglutamic Acid; Quinazolines; Swine; Thymidylate Synthase; Tumor Cells, Cultured

1996
The complex of the anti-cancer therapeutic, BW1843U89, with thymidylate synthase at 2.0 A resolution: implications for a new mode of inhibition.
    Structure (London, England : 1993), 1996, Jan-15, Volume: 4, Issue:1

    Topics: Antineoplastic Agents; Binding Sites; Binding, Competitive; Crystallography, X-Ray; Deoxyuracil Nucleotides; Drug Design; Enzyme Inhibitors; Escherichia coli; Folic Acid Antagonists; Indoles; Isoindoles; Models, Molecular; Molecular Structure; Protein Binding; Protein Conformation; Quinazolines; Thymidylate Synthase

1996
Ligand-induced distortion of an active site in thymidylate synthase upon binding anticancer drug 1843U89.
    Nature structural biology, 1995, Volume: 2, Issue:12

    Topics: Antineoplastic Agents; Binding Sites; Crystallography; Indoles; Isoindoles; Ligands; Protein Conformation; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase

1995
Disparate affinities of antifolates for folylpolyglutamate synthetase from human leukemia cells.
    Blood, 1997, Aug-01, Volume: 90, Issue:3

    Topics: Acute Disease; Antimetabolites, Antineoplastic; Drug Resistance, Neoplasm; Enzyme Inhibitors; Folic Acid Antagonists; HL-60 Cells; Humans; Indoles; Isoindoles; Kinetics; Leukemia, Myeloid; Methotrexate; Neoplasm Proteins; Organ Specificity; Peptide Synthases; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured

1997
Cross-resistance to antifolates in multidrug resistant cell lines with P-glycoprotein or multidrug resistance protein expression.
    Biochemical pharmacology, 1997, Jun-15, Volume: 53, Issue:12

    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
Recent advances in the study of rTS proteins. rTS expression during growth and in response to thymidylate synthase inhibitors in human tumor cells.
    Advances in enzyme regulation, 1997, Volume: 37

    Topics: Blotting, Western; Cell Division; Electrophoresis, Polyacrylamide Gel; Enzyme Inhibitors; Floxuridine; Folic Acid Antagonists; Gene Expression Regulation, Neoplastic; Humans; Hydro-Lyases; Indoles; Isoindoles; Protein Biosynthesis; Proteins; Quinazolines; Racemases and Epimerases; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured

1997
Increases in neutral, Mg2+-dependent and acidic, Mg2+-independent sphingomyelinase activities precede commitment to apoptosis and are not a consequence of caspase 3-like activity in Molt-4 cells in response to thymidylate synthase inhibition by GW1843.
    Blood, 1998, Jun-01, Volume: 91, Issue:11

    Topics: Apoptosis; Caspase 3; Caspases; Ceramides; Cysteine Endopeptidases; Diglycerides; Enzyme Inhibitors; Enzyme Precursors; Humans; Indoles; Isoindoles; Leukemia, T-Cell; Magnesium; Quinazolines; Sphingomyelin Phosphodiesterase; Thymidylate Synthase; Tumor Cells, Cultured

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.
    The Journal of biological chemistry, 1998, Nov-20, Volume: 273, Issue:47

    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
Antitumor activity of antifolate inhibitors of thymidylate and purine synthesis in human soft tissue sarcoma cell lines with intrinsic resistance to methotrexate.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 1995, Volume: 1, Issue:6

    Topics: Antimetabolites, Antineoplastic; Antineoplastic Agents; Biological Transport; Biotransformation; Cell Division; Cell Survival; Drug Resistance, Neoplasm; Folic Acid Antagonists; Humans; Indoles; Isoindoles; Kinetics; Methotrexate; Purines; Quinazolines; Sarcoma; Tetrahydrofolates; Thiophenes; Thymidine Monophosphate; Tumor Cells, Cultured

1995
Antifolate resistance mediated by the multidrug resistance proteins MRP1 and MRP2.
    Cancer research, 1999, Jun-01, Volume: 59, Issue:11

    Topics: Adenosine Triphosphate; Antimetabolites, Antineoplastic; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP-Binding Cassette Transporters; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Folic Acid Antagonists; Glutamates; Humans; Indoles; Isoindoles; Methotrexate; Ovarian Neoplasms; Quinazolines; Thiophenes; Transfection; Tumor Cells, Cultured

1999
Determinants of activity of the antifolate thymidylate synthase inhibitors Tomudex (ZD1694) and GW1843U89 against mono- and multilayered colon cancer cell lines under folate-restricted conditions.
    Cancer research, 1999, Nov-01, Volume: 59, Issue:21

    Topics: Blotting, Western; Cell Cycle; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Folic Acid Antagonists; Humans; Immunohistochemistry; Indoles; Inhibitory Concentration 50; Isoindoles; Methotrexate; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured

1999
Potent and selective activity of a combination of thymidine and 1843U89, a folate-based thymidylate synthase inhibitor, against Plasmodium falciparum.
    Antimicrobial agents and chemotherapy, 2000, Volume: 44, Issue:4

    Topics: Animals; Cell Division; Enzyme Inhibitors; Erythrocytes; Folic Acid Antagonists; Indoles; Isoindoles; Kinetics; Leukemia L1210; Mice; Plasmodium falciparum; Quinazolines; Thymidine; Thymidylate Synthase

2000
Combination studies of antifolates with 5-fluorouracil in colon cancer cell lines.
    Oncology research, 1999, Volume: 11, Issue:8

    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
Comparison of thymidylate synthase (TS) protein up-regulation after exposure to TS inhibitors in normal and tumor cell lines and tissues.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2000, Volume: 6, Issue:6

    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.
    The Journal of biological chemistry, 2000, Oct-06, Volume: 275, Issue:40

    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
Pharmacokinetics, safety, and efficacy of a liposome encapsulated thymidylate synthase inhibitor, OSI-7904L [(S)-2-[5-[(1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl]amino-1-oxo-2-isoindolynl]-glutaric acid] in mice.
    The Journal of pharmacology and experimental therapeutics, 2004, Volume: 309, Issue:3

    Topics: Animals; Antineoplastic Agents; Biological Availability; Carbon Radioisotopes; Disease Models, Animal; Drug Carriers; Drug Delivery Systems; Enzyme Inhibitors; Humans; Indoles; Isoindoles; Liposomes; Metabolic Clearance Rate; Mice; Mice, Inbred BALB C; Neoplasm Transplantation; Neoplasms, Experimental; Quinazolines; Thymidylate Synthase; Tissue Distribution; Treatment Outcome; Tumor Cells, Cultured; Xenograft Model Antitumor Assays

2004
Low folate conditions may enhance the interaction of trifluorothymidine with antifolates in colon cancer cells.
    Cancer chemotherapy and pharmacology, 2006, Volume: 57, Issue:2

    Topics: Antimetabolites; Colonic Neoplasms; DNA Damage; Drug Interactions; Folic Acid; Folic Acid Antagonists; Homeostasis; Humans; Indoles; Isoindoles; Quinazolines; Thiophenes; Trifluridine; Tumor Cells, Cultured

2006
Functional identity of the active sites of crustacean and viral thymidylate synthases.
    Comparative biochemistry and physiology. Toxicology & pharmacology : CBP, 2009, Volume: 150, Issue:3

    Topics: Amino Acid Sequence; Animals; Base Sequence; Catalytic Domain; Cloning, Molecular; Deoxyuracil Nucleotides; Folic Acid; Folic Acid Antagonists; Isoindoles; Kinetics; Models, Molecular; Molecular Sequence Data; Penaeidae; Phylogeny; Quinazolines; Sequence Alignment; Thymidylate Synthase; White spot syndrome virus 1

2009