thiophenes has been researched along with methotrexate in 59 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 1 (1.69) | 18.7374 |
| 1990's | 33 (55.93) | 18.2507 |
| 2000's | 14 (23.73) | 29.6817 |
| 2010's | 9 (15.25) | 24.3611 |
| 2020's | 2 (3.39) | 2.80 |
| Authors | Studies |
|---|---|
| Bader, H; Beardsley, GP; DeYarman, MT; Freisheim, JH; Galivan, J; Kerwar, SS; Moroson, BA; O'Connor, BM; Rosowsky, A; Russello, O | 1 |
| Arredondo, MA; Guimaraes, MA; Rustum, YM; Yin, MB; Zhang, ZG | 1 |
| Brown, M; Calvert, AH; Gibson, W; Hughes, LR; Jackman, AL; Judson, IR; Kimbell, R; Taylor, GA | 1 |
| Braunsberg, H; Coldham, NG; Patel, K | 1 |
| Davies, GE | 1 |
| Aherne, GW; Boyle, FT; Brown, M; Gibson, W; Hardcastle, A; Jackman, AL; Kelland, LR; Kimbell, R | 1 |
| Jansen, G; Peters, GJ; Pinedo, HM; Rijnboutt, S; Schornagel, JH; Westerhof, GR | 1 |
| Bonmassar, E; Lu, K; McGuire, JJ; Rustum, YM; Yin, MB | 1 |
| Lehman, NL; Moran, RG; Smith, SG | 1 |
| Haile, WH; Heitzman, KJ; McCloskey, DE; McGuire, JJ; Piper, JR; Russell, CA | 1 |
| Abraham, A; Galivan, J; McGuire, JJ; Nair, MG; Vishnuvajjala, BR | 1 |
| Malmberg, M; Rustum, YM; Slocum, HK; Yin, MB; Zhang, ZG | 1 |
| Jackman, AL; Kobayashi, H; Miyachi, H; Skelton, L; Takemura, Y | 1 |
| Gibson, W; Jackman, AL; Kimbell, R; Kobayashi, H; Miyachi, H; Takemura, Y | 2 |
| Jansen, G; Jolivet, J; Kathmann, I; Molthoff, C; Pinard, MF; Ratnam, M; Schornagel, JH; Westerhof, R | 1 |
| DeGoeij, K; Mester, J; Sluyser, M | 1 |
| Iversen, L; Kragballe, K; Svendsen, M | 1 |
| Andis, SL; Beardsley, GP; Bewley, JR; Chen, VJ; Gates, SB; Gossett, LS; Habeck, LL; Kohler, W; MacKellar, WC; Mendelsohn, LG; Moroson, BA; Patel, VF; Ratnam, M; Rayl, EA; Schultz, RM; Shackelford, KA; Shih, C; Soose, DJ | 1 |
| Bertino, JR; Fan, J; Hochhauser, D; Li, WW | 1 |
| Bertino, JR; Ercikan, E; Gorlick, R; Longo, GS; Tong, WP | 1 |
| Jansen, G; Peters, GJ; Pinedo, HM; Telleman, F; van der Wilt, CL; van Triest, B | 1 |
| Kamen, B | 1 |
| Kobayashi, H; Ohnuma, T; Takemura, Y | 1 |
| Kinsella, AR; Smith, D | 1 |
| Andis, SL; Bewley, JR; Chen, VJ; Iversen, PW; Mendelsohn, LG; Schultz, RM; Seitz, DE; Shih, C; Tonkinson, JL | 2 |
| Bertino, JR; Li, WW; Tong, WP | 1 |
| Assaraf, YG; Borst, P; Broxterman, HJ; Hooijberg, JH; Jansen, G; Kool, M; Noordhuis, P; Peters, GJ; Pinedo, HM; Scheper, RJ | 1 |
| Aherne, GW; Barnes, MJ; Calvete, JA; Estlin, EJ; Hardcastle, A; Lunec, J; McGuire, JJ; Newell, DR; Pearson, AD; Taylor, GA | 1 |
| Agostinelli, R; Baldelli, AM; Barni, S; Cascinu, S; Catalano, G; Catalano, V; Frontini, L; Gasparini, G; Giuliodori, L; Labianca, R; Martignoni, G; Mattioli, R; Silva, RR | 1 |
| Jansen, G; Peters, GJ; Pinedo, HM; Smid, K; Smitskamp-Wilms, E | 1 |
| Creutzig, U; Hählen, K; Janka-Schaub, G; Jansen, G; Kaspers, GJ; Mauritz, R; Noordhuis, P; Peters, GJ; Pieters, R; Rots, MG; van Zantwijk, CH; Veerman, AJ; Willey, JC | 1 |
| Newell, DR | 1 |
| Strømhaug, A; Warren, DJ | 1 |
| Genestier, L; Izeradjene, K; Revillard, JP | 1 |
| Akutsu, M; Furukawa, Y; Kano, Y; Suzuki, K; Tsunoda, S; Yazawa, Y | 1 |
| Arvelo, F; Bras-Gonçalves, RA; Coquelle, A; De Pinieux, G; Dutrillaux, B; Formento, JL; Lesuffleur, T; Milano, G; Pandrea, I; Pocard, M; Poirson-Bichat, F; Poupon, MF; Ronco, G; Villa, P | 1 |
| Curtin, NJ; Errington, J; Lu, X; Lunec, J; Newell, DR | 1 |
| Assaraf, YG; Bunni, MA; Drori, S; Jansen, G; Kathmann, I; Mauritz, R; Noordhuis, P; Peters, GJ; Pinedo, HM; Priest, DG; Rosowsky, A; Schornagel, JH | 1 |
| Fleck, C; Hilger, R; Jurkutat, S; Karge, E; Merkel, U; Schimske, A; Schubert, J | 1 |
| Licun, W; Tannock, IF | 1 |
| Banerjee, D; Bertino, JR; Li, WW; Magro, PG; Russo, AJ | 1 |
| Goldman, ID; Wang, Y; Zhao, R | 1 |
| Assaraf, YG; Ifergan, I; Kadry, WN; Pinter, RY | 1 |
| Chattopadhyay, S; Goldman, ID; Krupenko, N; Krupenko, SA; Zhao, R | 1 |
| DeGroot, J; Hanemaaijer, R; Huizinga, TW; Kraan, MC; Tchetverikov, I; van El, B | 1 |
| De Mattia, E; Toffoli, G | 1 |
| Botchkina, G; Formentini, A; Ju, J; Kornmann, M; Song, B; Titmus, MA; Wang, Y | 1 |
| Aydin, M; Davarci, M; Gökçe, A; Koç, A; Meydan, S; Oktar, S; Oztürk, OH | 1 |
| Guzi, TJ; Parry, D; Pierce, RH; Shanahan, F; Taricani, L | 1 |
| Guo, Y; Li, C; Liu, JY; Tian, C; Wang, XW; Zhang, ZL | 1 |
| Assaraf, YG; Dijkmans, BA; Gerards, AH; Jansen, G; Lems, WF; Oerlemans, R; Scheper, RJ; van der Heijden, JW | 1 |
| Contestabile, R; Cutruzzolà, F; Daidone, F; Fiascarelli, A; Giardina, G; Koes, DR; Marani, M; McDermott, LA; Montini, G; Paiardini, A; Paone, A; Parroni, A; Rinaldo, S | 1 |
| Chernobrovkin, A; Marin-Vicente, C; Visa, N; Zubarev, RA | 1 |
| Sharma, L | 1 |
| Kanamitsu, K; Kusuhara, H; Schuetz, JD; Sugiyama, Y; Takeuchi, K | 1 |
| Chen, Y; Cui, Z; Ding, M; Fang, H; Li, H; Lin, Y; Ma, C; Niu, Q; Sun, H; Sun, S; Wang, S; Xiao, N; Xu, Y; Zhou, BS | 1 |
| Charushin, VN; Kovalev, IS; Majee, A; Santra, S; Varaksin, MV; Zyryanov, GV | 1 |
6 review(s) available for thiophenes and methotrexate
| Article | Year |
|---|---|
Folate and antifolate pharmacology.
Topics: Antimetabolites, Antineoplastic; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Trimetrexate | 1997 |
Tumor resistance to antimetabolites.
Topics: Antimetabolites, Antineoplastic; Cell Cycle Proteins; Deoxycytidine; DNA Damage; DNA, Neoplasm; Drug Resistance, Neoplasm; Fluorouracil; Gemcitabine; Gene Amplification; Humans; Methotrexate; Mutation; Neoplasms; Quinazolines; Thiophenes | 1998 |
Clinical pharmacokinetics of antitumor antifolates.
Topics: Antimetabolites, Antineoplastic; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Isoindoles; Methotrexate; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase | 1999 |
C677T and A1298C MTHFR polymorphisms, a challenge for antifolate and fluoropyrimidine-based therapy personalisation.
Topics: Animals; Antimetabolites, Antineoplastic; Drug Resistance, Neoplasm; Fluorouracil; Folic Acid Antagonists; Humans; Methotrexate; Methylenetetrahydrofolate Reductase (NADPH2); Neoplasms; Pharmacogenetics; Polymorphism, Genetic; Quinazolines; Thiophenes; Treatment Outcome | 2009 |
Osteoarthritis year in review 2015: clinical.
Topics: Adalimumab; Antirheumatic Agents; Arthroplasty, Replacement; Bone Density Conservation Agents; Chondroitin Sulfates; Cognitive Behavioral Therapy; Diphosphonates; Exercise Therapy; Glucosamine; Humans; Methotrexate; Osteoarthritis; Physical Therapy Modalities; Resistance Training; Thiophenes; Transcutaneous Electric Nerve Stimulation; Treatment Outcome; Ultrasonic Therapy | 2016 |
Folic Acid Antimetabolites (Antifolates): A Brief Review on Synthetic Strategies and Application Opportunities.
Topics: Antimetabolites; Folic Acid; Folic Acid Antagonists; Methotrexate; Pemetrexed; Quinazolines; Thiophenes | 2022 |
2 trial(s) available for thiophenes and methotrexate
| Article | Year |
|---|---|
A phase II study of Tomudex alternated with methotrexate, 5-fluorouracil, leucovorin in first-line chemotherapy of metastatic colorectal cancer.
Topics: Adenocarcinoma; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Colorectal Neoplasms; Disease-Free Survival; Female; Fluorouracil; Humans; Leucovorin; Lymphatic Metastasis; Male; Methotrexate; Middle Aged; Prognosis; Quinazolines; Survival Rate; Thiophenes; Treatment Outcome | 1999 |
Leflunomide and methotrexate reduce levels of activated matrix metalloproteinases in complexes with alpha2 macroglobulin in serum of rheumatoid arthritis patients.
Topics: Aged; alpha-Macroglobulins; Antirheumatic Agents; Arthritis, Rheumatoid; Biomarkers; C-Reactive Protein; Down-Regulation; Enzyme Inhibitors; Female; Humans; Isoxazoles; Leflunomide; Male; Matrix Metalloproteinases; Methotrexate; Middle Aged; Multiprotein Complexes; Phenylalanine; Statistics, Nonparametric; Thiophenes | 2008 |
51 other study(ies) available for thiophenes and methotrexate
| Article | Year |
|---|---|
Biochemical and biological studies on 2-desamino-2-methylaminopterin, an antifolate the polyglutamates of which are more potent than the monoglutamate against three key enzymes of folate metabolism.
Topics: Acyltransferases; Aminopterin; Animals; Antineoplastic Agents; Carcinoma, Hepatocellular; Cell Division; Drug Administration Schedule; Folic Acid; Folic Acid Antagonists; Hydroxymethyl and Formyl Transferases; Leukemia L1210; Male; Methotrexate; Mice; Phosphoribosylaminoimidazolecarboxamide Formyltransferase; Phosphoribosylglycinamide Formyltransferase; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1992 |
Time dependence of DNA lesions and growth inhibition by ICI D1694, a new quinazoline antifolate thymidylate synthase inhibitor.
Topics: Cell Division; Cell Line; DNA; DNA Damage; DNA, Single-Stranded; Fluorouracil; Formyltetrahydrofolates; Methotrexate; Quinazolines; Rhodamines; Thiophenes; Thymidine; Thymidylate Synthase; Time Factors | 1992 |
ICI D1694, a quinazoline antifolate thymidylate synthase inhibitor that is a potent inhibitor of L1210 tumor cell growth in vitro and in vivo: a new agent for clinical study.
Topics: Animals; Carrier Proteins; Cell Division; Drug Screening Assays, Antitumor; Folate Receptors, GPI-Anchored; Folic Acid; Glutamates; Leukemia L1210; Male; Methotrexate; Mice; Mice, Inbred DBA; Quinazolines; Receptors, Cell Surface; Thiophenes; Thymidylate Synthase | 1991 |
Hormone and cytotoxic drug responsiveness of cultured human breast cancer cells resistant to specific hormones.
Topics: Breast Neoplasms; Cell Division; Dexamethasone; Drug Resistance; Estradiol; Humans; Medroxyprogesterone; Medroxyprogesterone Acetate; Methotrexate; Pyrrolidines; Tamoxifen; Thiophenes; Tumor Cells, Cultured; Vincristine | 1990 |
Immunosuppressive activity of 3-acetyl-5-(4-fluorobenzylidene)-4-hydroxy-2-oxo-2:5-dihydrothiophen (I.C.I. 47,776).
Topics: Anaphylaxis; Animals; Antibody Formation; Cyclophosphamide; Depression, Chemical; Guinea Pigs; Immunosuppressive Agents; Mercaptopurine; Methotrexate; Mice; Rats; Species Specificity; Thioguanine; Thiophenes | 1968 |
Mechanisms of acquired resistance to the quinazoline thymidylate synthase inhibitor ZD1694 (Tomudex) in one mouse and three human cell lines.
Topics: Animals; Antineoplastic Agents; Carrier Proteins; Deoxyuracil Nucleotides; Drug Resistance; Female; Folate Receptors, GPI-Anchored; Folic Acid; Folic Acid Antagonists; Humans; Kinetics; Leukemia L1210; Lymphocytes; Methotrexate; Mice; Neoplasm Proteins; Ovarian Neoplasms; Peptide Synthases; Polyglutamic Acid; Proteins; Quinazolines; Receptors, Cell Surface; Thiophenes; Thymidylate Synthase; Thymine Nucleotides; Tumor Cells, Cultured | 1995 |
Functional activity of the reduced folate carrier in KB, MA104, and IGROV-I cells expressing folate-binding protein.
Topics: Aminopterin; Animals; Carrier Proteins; Cell Division; Female; Folate Receptors, GPI-Anchored; Folic Acid; Folic Acid Antagonists; Glutamates; Haplorhini; Humans; Kidney; Leucovorin; Methotrexate; Nasopharyngeal Neoplasms; Ovarian Neoplasms; Quinazolines; Receptors, Cell Surface; Tetrahydrofolates; Thiophenes; Tumor Cells, Cultured | 1995 |
Mechanisms of resistance to N-[5-[N-(3,4-dihydro-2-methyl-4- oxoquinazolin-6-ylmethyl)-N-methylamino]-2-thenoyl]-L-glutamic acid (ZD1694), a folate-based thymidylate synthase inhibitor, in the HCT-8 human ileocecal adenocarcinoma cell line.
Topics: Cell Division; Cell-Free System; Dose-Response Relationship, Drug; Drug Resistance; Folic Acid Antagonists; Glutamates; Guanine; Humans; Methotrexate; Pemetrexed; Peptide Synthases; Pteroylpolyglutamic Acids; Quinazolines; Thiophenes; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured | 1995 |
Cytotoxicity of antifolate inhibitors of thymidylate and purine synthesis to WiDr colonic carcinoma cells.
Topics: Acyltransferases; Antineoplastic Agents; Cell Division; Cell Survival; Colonic Neoplasms; Folic Acid Antagonists; Humans; Hydroxymethyl and Formyl Transferases; Hypoxanthine; Hypoxanthines; Methotrexate; Phosphoribosylglycinamide Formyltransferase; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidine; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
Cross-resistance studies of folylpolyglutamate synthetase-deficient, methotrexate-resistant CCRF-CEM human leukemia sublines.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Agents; Cell Division; Drug Resistance; Folic Acid Antagonists; Humans; Leucovorin; Methotrexate; Peptide Synthases; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Pyrimidines; Quinazolines; Tetrahydrofolates; Thiophenes; Tumor Cells, Cultured | 1993 |
New thiophene substituted 10-deazaaminopterins: synthesis and biological evaluation.
Topics: Aminopterin; Animals; Antineoplastic Agents; Cell Division; Cell Line; Cell Survival; Drug Evaluation, Preclinical; Female; Folic Acid Antagonists; Glutamates; Humans; Male; Methotrexate; Mice; Pterins; Rats; Structure-Activity Relationship; Thiophenes; Tumor Cells, Cultured | 1993 |
Isolation and characterization of a human ileocecal carcinoma cell line (HCT-8) subclone resistant to fluorodeoxyuridine.
Topics: Antimetabolites, Antineoplastic; Cell Division; Colonic Neoplasms; Drug Resistance; Floxuridine; Fluorouracil; Humans; Methotrexate; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidine Kinase; Thymidine Phosphorylase; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
Effect of hammerhead ribozyme against human thymidylate synthase on the cytotoxicity of thymidylate synthase inhibitors.
Topics: B-Lymphocytes; Base Sequence; Drug Resistance; Drug Synergism; Enzyme Induction; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Molecular Sequence Data; Nucleic Acid Conformation; Quinazolines; Repetitive Sequences, Nucleic Acid; RNA, Catalytic; RNA, Messenger; Thiophenes; Thymidylate Synthase; Transfection; Trimetrexate | 1995 |
The influence of drug-exposure conditions on the development of resistance to methotrexate or ZD1694 in cultured human leukaemia cells.
Topics: Antimetabolites, Antineoplastic; Drug Resistance; gamma-Glutamyl Hydrolase; Gene Expression Regulation, Enzymologic; Humans; Leukemia; Methotrexate; Peptide Synthases; Pteroylpolyglutamic Acids; Quinazolines; RNA, Messenger; Tetrahydrofolate Dehydrogenase; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1996 |
Functional aspects of membrane folate receptors in human breast cancer cells with transport-related resistance to methotrexate.
Topics: Aminopterin; Antimetabolites, Antineoplastic; Binding Sites; Breast Neoplasms; Carrier Proteins; Cell Membrane; DNA, Complementary; Female; Folate Receptors, GPI-Anchored; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Polymerase Chain Reaction; Quinazolines; Receptors, Cell Surface; RNA, Messenger; Spectrometry, Fluorescence; Structure-Activity Relationship; Tetrahydrofolates; Thiophenes; Tumor Cells, Cultured | 1996 |
Biological activity and intracellular metabolism of ZD1694 in human leukemia cell lines with different resistance mechanisms to antifolate drugs.
Topics: Antimetabolites, Antineoplastic; Drug Resistance; Folic Acid Antagonists; Humans; Leukemia; Methotrexate; Polyglutamic Acid; Quinazolines; Tetrahydrofolate Dehydrogenase; Thiophenes; Tumor Cells, Cultured | 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 |
Cyclosporin A down-regulates the LTA4 hydrolase level in human keratinocyte cultures.
Topics: 8,11,14-Eicosatrienoic Acid; Anti-Inflammatory Agents; Antineoplastic Agents; Calcitriol; Cells, Cultured; Cyclosporine; Dexamethasone; Down-Regulation; Epoxide Hydrolases; Humans; Interferon-gamma; Keratinocytes; Leukotriene B4; Methotrexate; Psoriasis; Thiophenes; Tretinoin | 1996 |
LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes.
Topics: 5,10-Methylenetetrahydrofolate Reductase (FADH2); Acyltransferases; Aminohydrolases; Antimetabolites, Antineoplastic; Folic Acid Antagonists; Formate-Tetrahydrofolate Ligase; Glutamates; Guanine; Humans; Hydroxymethyl and Formyl Transferases; Methotrexate; Methylenetetrahydrofolate Dehydrogenase (NADP); Methylenetetrahydrofolate Reductase (NADPH2); Molecular Structure; Multienzyme Complexes; Oxidoreductases; Pemetrexed; Phosphoribosylaminoimidazolecarboxamide Formyltransferase; Phosphoribosylglycinamide Formyltransferase; Polyglutamic Acid; Quinazolines; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1997 |
Overexpression of p21waf1 leads to increased inhibition of E2F-1 phosphorylation and sensitivity to anticancer drugs in retinoblastoma-negative human sarcoma cells.
Topics: Anti-Bacterial Agents; Antibiotics, Antineoplastic; Antimetabolites, Antineoplastic; Apoptosis; Carrier Proteins; Cell Cycle; Cell Cycle Proteins; Cyclin-Dependent Kinase Inhibitor p21; Cyclin-Dependent Kinases; Cyclins; DNA-Binding Proteins; Doxorubicin; E2F Transcription Factors; E2F1 Transcription Factor; Gene Expression Regulation, Neoplastic; Genes, p53; Humans; Methotrexate; Osteosarcoma; Phosphorylation; Quinazolines; Retinoblastoma Protein; Retinoblastoma-Binding Protein 1; Tetracycline; Tetrahydrofolate Dehydrogenase; Thiophenes; Thymidylate Synthase; Transcription Factor DP1; Transcription Factors; Tumor Cells, Cultured | 1997 |
Disparate affinities of antifolates for folylpolyglutamate synthetase from human leukemia cells.
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.
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 |
Variable expression of RFC1 in human leukemia cell lines resistant to antifolates.
Topics: Antimetabolites, Antineoplastic; Biological Transport; Carrier Proteins; Drug Resistance, Neoplasm; Folic Acid; Folic Acid Antagonists; Humans; Leucovorin; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Membrane Proteins; Membrane Transport Proteins; Methotrexate; Phenotype; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines; Tetrahydrofolate Dehydrogenase; Thiophenes; Tumor Cells, Cultured | 1998 |
Preclinical cellular pharmacology of LY231514 (MTA): a comparison with methotrexate, LY309887 and raltitrexed for their effects on intracellular folate and nucleoside triphosphate pools in CCRF-CEM cells.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Agents; Chromatography, High Pressure Liquid; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Folic Acid; Glutamates; Guanine; Humans; Hydroxymethyl and Formyl Transferases; Methotrexate; Nucleotides; Pemetrexed; Phosphoribosylglycinamide Formyltransferase; Quinazolines; Reproducibility of Results; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1998 |
Antitumor activity of antifolate inhibitors of thymidylate and purine synthesis in human soft tissue sarcoma cell lines with intrinsic resistance to methotrexate.
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.
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 |
Impact of polyglutamation on sensitivity to raltitrexed and methotrexate in relation to drug-induced inhibition of de novo thymidylate and purine biosynthesis in CCRF-CEM cell lines.
Topics: Biological Transport; Cell Division; Drug Screening Assays, Antitumor; Folic Acid Antagonists; Growth Inhibitors; Humans; Inhibitory Concentration 50; Leukemia; Methotrexate; Peptide Synthases; Purines; Quinazolines; RNA, Messenger; Thiophenes; Thymidine Monophosphate; Thymidylate Synthase; 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.
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 |
Circumvention of methotrexate resistance in childhood leukemia subtypes by rationally designed antifolates.
Topics: Antimetabolites, Antineoplastic; Child; Child, Preschool; Drug Resistance, Neoplasm; Folic Acid Antagonists; Humans; Leukemia; Methotrexate; Quinazolines; Thiophenes; Treatment Outcome; Trimetrexate | 1999 |
Cellular pharmacology of MTA: a correlation of MTA-induced cellular toxicity and in vitro enzyme inhibition with its effect on intracellular folate and nucleoside triphosphate pools in CCRF-CEM cells.
Topics: Acid Anhydride Hydrolases; Antimetabolites, Antineoplastic; Deoxyribonucleotides; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Methotrexate; Nucleoside-Diphosphate Kinase; Nucleoside-Triphosphatase; Pemetrexed; Quinazolines; Ribonucleotides; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Thymine Nucleotides; 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 |
Inhibition of thymidine synthesis by folate analogues induces a Fas-Fas ligand-independent deletion of superantigen-reactive peripheral T cells.
Topics: Animals; CD8-Positive T-Lymphocytes; Clonal Deletion; Enterotoxins; Fas Ligand Protein; fas Receptor; Folic Acid Antagonists; Growth Inhibitors; Injections, Intraperitoneal; Injections, Intravenous; Ligands; Lymphocyte Activation; Lymphocyte Depletion; Membrane Glycoproteins; Methotrexate; Mice; Mice, Inbred BALB C; Mice, Inbred C57BL; Mice, Inbred MRL lpr; Nucleic Acid Synthesis Inhibitors; Quinazolines; Staphylococcus aureus; Superantigens; T-Lymphocyte Subsets; Thiophenes; Thymidine; Thymidylate Synthase | 2001 |
Schedule-dependent synergism and antagonism between raltitrexed ("Tomudex") and methotrexate in human colon cancer cell lines in vitro.
Topics: Antineoplastic Combined Chemotherapy Protocols; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug Screening Assays, Antitumor; Drug Synergism; Humans; Methotrexate; Quinazolines; Thiophenes; Tumor Cells, Cultured | 2001 |
Synergistic efficacy of 3n-butyrate and 5-fluorouracil in human colorectal cancer xenografts via modulation of DNA synthesis.
Topics: Animals; Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Biomarkers; Butyrates; Cell Differentiation; Cell Division; Colorectal Neoplasms; Dihydrouracil Dehydrogenase (NADP); DNA; Drug Synergism; Female; Fluorouracil; Glucose; Humans; Liver Neoplasms; Male; Methotrexate; Mice; Mice, Nude; Neoplasm Transplantation; Organoplatinum Compounds; Oxaliplatin; Oxidoreductases; Protein-Tyrosine Kinases; Quinazolines; RNA, Messenger; Thiophenes; Thymidylate Synthase; Transplantation, Heterologous | 2001 |
The impact of p53 status on cellular sensitivity to antifolate drugs.
Topics: Apoptosis; Blotting, Western; Cell Cycle; Cell Division; Cyclin-Dependent Kinase Inhibitor p21; Cyclins; DNA Mutational Analysis; DNA, Neoplasm; Dose-Response Relationship, Drug; Folic Acid Antagonists; Gene Expression Regulation, Neoplastic; Genotype; Glutamates; Guanine; Humans; Methotrexate; Mutation; Pemetrexed; Quinazolines; Sensitivity and Specificity; Tetrahydrofolates; Thiophenes; Tumor Cells, Cultured; Tumor Suppressor Protein p53 | 2001 |
Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis.
Topics: Biological Transport; Drug Resistance, Multiple; Drug Screening Assays, Antitumor; Folic Acid; Folic Acid Antagonists; gamma-Glutamyl Hydrolase; Glutamates; Guanine; Homeostasis; Humans; Leukemia; Methotrexate; Ornithine; Pemetrexed; Peptide Synthases; Polyglutamic Acid; Pterins; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 2002 |
Ex vivo stimulation of renal transport of the cytostatic drugs methotrexate, cisplatin, topotecan (Hycamtin) and raltitrexed (Tomudex) by dexamethasone, T3 and EGF in intact human and rat kidney tissue and in human renal cell carcinoma.
Topics: Animals; Antimetabolites, Antineoplastic; Antineoplastic Agents; Biological Transport; Carcinoma, Renal Cell; Cisplatin; Dexamethasone; Epidermal Growth Factor; Female; Glucocorticoids; Humans; Kidney; Kidney Neoplasms; Methotrexate; Quinazolines; Rats; Rats, Wistar; Thiophenes; Topotecan; Triiodothyronine | 2002 |
Selective estrogen receptor modulators as inhibitors of repopulation of human breast cancer cell lines after chemotherapy.
Topics: Antineoplastic Agents, Hormonal; Breast Neoplasms; Cell Division; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Female; Fluorouracil; Humans; Methotrexate; Neoplasms, Hormone-Dependent; Piperidines; Receptors, Estrogen; Selective Estrogen Receptor Modulators; Tamoxifen; Thiophenes; Tumor Cells, Cultured; Tumor Stem Cell Assay | 2003 |
p14ARF expression increases dihydrofolate reductase degradation and paradoxically results in resistance to folate antagonists in cells with nonfunctional p53.
Topics: Cell Division; Cell Line, Tumor; Drug Resistance, Neoplasm; Enzyme Stability; Fibrosarcoma; Folic Acid Antagonists; Humans; Methotrexate; Neoplastic Stem Cells; Quinazolines; Tetrahydrofolate Dehydrogenase; Thiophenes; Thymidine; Thymidylate Synthase; Trimetrexate; Tumor Suppressor Protein p14ARF; Tumor Suppressor Protein p53 | 2004 |
Characterization of a folate transporter in HeLa cells with a low pH optimum and high affinity for pemetrexed distinct from the reduced folate carrier.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Agents; Biological Transport; Blotting, Northern; Carrier Proteins; Cell Line; Cell Line, Tumor; Folate Receptors, GPI-Anchored; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; HeLa Cells; Humans; Hydrogen-Ion Concentration; Ions; Kinetics; Membrane Transport Proteins; Methotrexate; Pemetrexed; Protein Isoforms; Quinazolines; Receptors, Cell Surface; Reduced Folate Carrier Protein; RNA; Thiophenes; Time Factors; Transfection; Trimetrexate | 2004 |
Computer modelling of antifolate inhibition of folate metabolism using hybrid functional petri nets.
Topics: Antimetabolites, Antineoplastic; Computer Simulation; Dose-Response Relationship, Drug; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Models, Chemical; Purines; Quinazolines; Signal Transduction; Tetrahydrofolates; Thiophenes; Thymidine Monophosphate | 2006 |
The inverse relationship between reduced folate carrier function and pemetrexed activity in a human colon cancer cell line.
Topics: Amino Acid Substitution; Antineoplastic Agents; Arginine; Carrier Proteins; Cell Line, Tumor; Colonic Neoplasms; Drug Resistance, Neoplasm; Folate Receptors, GPI-Anchored; Folic Acid Antagonists; Glutamates; Glycine; Guanine; Humans; Leucovorin; Methotrexate; Mutation; Pemetrexed; Phosphoribosylglycinamide Formyltransferase; Purines; Pyrimidines; Quinazolines; Receptors, Cell Surface; Thiophenes; Thymidylate Synthase | 2006 |
Molecular mechanism of chemoresistance by miR-215 in osteosarcoma and colon cancer cells.
Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Agents; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Colonic Neoplasms; Drug Resistance, Neoplasm; Female; Gene Expression Regulation; Gene Knockdown Techniques; Humans; Male; Methotrexate; MicroRNAs; Middle Aged; Nuclear Proteins; Osteosarcoma; Quinazolines; Reverse Transcriptase Polymerase Chain Reaction; RNA, Small Interfering; Tetrahydrofolate Dehydrogenase; Thiophenes; Thymidylate Synthase; Transfection; Ubiquitin-Protein Ligases | 2010 |
Beneficial effect of erdosteine on methotrexate-induced testicular toxicity in mice.
Topics: Analysis of Variance; Animals; Drug Interactions; Lipid Peroxidation; Male; Malondialdehyde; Methotrexate; Mice; Oxidative Stress; Peroxidase; Statistics, Nonparametric; Testicular Diseases; Testis; Thioglycolates; Thiophenes | 2010 |
Phenotypic enhancement of thymidylate synthetase pathway inhibitors following ablation of Neil1 DNA glycosylase/lyase.
Topics: Biomarkers; Cell Line; Checkpoint Kinase 1; DNA Glycosylases; DNA Repair; Enzyme Inhibitors; Folic Acid Antagonists; Histones; Humans; Methotrexate; Nucleic Acid Synthesis Inhibitors; Phenotype; Protein Kinases; Quinazolines; Thiophenes; Thymidylate Synthase | 2010 |
[Purification and activity evaluation of methionine synthase].
Topics: 5-Methyltetrahydrofolate-Homocysteine S-Methyltransferase; Animals; Electrophoresis, Polyacrylamide Gel; Folic Acid Antagonists; Liver; Male; Methotrexate; Quinazolines; Rats; Rats, Wistar; Tetrahydrofolates; Thiophenes | 2012 |
Methotrexate analogues display enhanced inhibition of TNF-α production in whole blood from RA patients.
Topics: Antirheumatic Agents; Arthritis, Rheumatoid; Female; Folic Acid Antagonists; Humans; Male; Methotrexate; Middle Aged; Ornithine; Pterins; Quinazolines; T-Lymphocytes; Thiophenes; Trimetrexate; Tumor Necrosis Factor-alpha | 2014 |
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 |
Functional Identification of Target by Expression Proteomics (FITExP) reveals protein targets and highlights mechanisms of action of small molecule drugs.
Topics: Antineoplastic Agents; Apoptosis; Camptothecin; Cell Line, Tumor; Computational Biology; Doxorubicin; Drug Discovery; Fluorouracil; HCT116 Cells; Humans; Methotrexate; Paclitaxel; Proteome; Proteomics; Quinazolines; Small Molecule Libraries; Thiophenes | 2015 |
Investigation of the Importance of Multidrug Resistance-Associated Protein 4 (Mrp4/Abcc4) in the Active Efflux of Anionic Drugs Across the Blood-Brain Barrier.
Topics: 2,4-Dichlorophenoxyacetic Acid; Acridines; Adenosine Triphosphate; Animals; Biological Transport; Blood-Brain Barrier; Brain; Central Nervous System; Cyclic GMP; Humans; Kinetics; Male; Methotrexate; Mice, Inbred C57BL; Multidrug Resistance-Associated Proteins; Ochratoxins; Pravastatin; Quinazolines; Quinolines; Tetrahydroisoquinolines; Thiophenes; Uric Acid | 2017 |
A γ-glutamyl hydrolase lacking the signal peptide confers susceptibility to folates/antifolates in acute lymphoblastic leukemia cells.
Topics: Cell Line, Tumor; Cell Survival; CRISPR-Cas Systems; Drug Resistance, Neoplasm; Folic Acid; Folic Acid Antagonists; gamma-Glutamyl Hydrolase; Gene Editing; Glycosylation; HeLa Cells; Humans; Lymphocytes; Lysosomes; Methotrexate; Polyglutamic Acid; Protein Sorting Signals; Quinazolines; Thiophenes | 2022 |