quinazolines has been researched along with Leukemia L 1210 in 121 studies
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 55 (45.45) | 18.7374 |
1990's | 52 (42.98) | 18.2507 |
2000's | 12 (9.92) | 29.6817 |
2010's | 2 (1.65) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
Authors | Studies |
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Cipak, L; Jantova, S; Repicky, A | 1 |
Chandra, KL; Desper, J; Naganaboina, VK; Perchellet, EM; Perchellet, JP; Rayat, S; Waters, AM | 1 |
Cipak, L | 1 |
Cipák, L; Horváth, V; Jantová, S; Rauko, P; Slamenová, D | 1 |
Cascioferro, S; Daidone, G; Maggio, B; Plescia, F; Raffa, D; Schillaci, D | 2 |
Cabezas-Herrera, J; Durrant, MC; García-Cánovas, F; Navarro-Perán, E; Rodríguez-López, JN; Thorneley, RN | 1 |
Bavetsias, V; Forster, MD; Gibbs, DD; Green, M; Henderson, E; Jackman, AL; Mitchell, F; Raynaud, F; Theti, DS; Valenti, M; Wood, N | 1 |
Elslager, EF; Johnson, JL; Werbel, LM | 1 |
Bertino, J; Cashmore, A; Eibl, B; Kamen, BA | 1 |
Besserer, JA; Boritzki, TJ; Elslager, EF; Fry, DW; Jackson, RC; Leopold, WR; Sloan, BJ | 1 |
Calvert, AH; Harrap, KR; Jackman, AL; Taylor, GA | 2 |
Atassi, G; Brassinne, C; Coune, A; Frühling, J; Hildebrand, J; Laduron, C; Penasse, W; Ruysschaert, JM | 1 |
Baron, M; Cros, S; Giorgi-Renault, S; Mailliet, P; Paoletti, C; Renault, J; Voisin, E | 1 |
Calvert, AH; Harrap, KR; Hart, LI; Jackman, AL | 1 |
Bertino, JR; Fernandes, DJ; Hynes, JB | 1 |
Brown, SJ; Calvert, AH; Harrap, KR; Jackman, AL; Jones, M; Jones, TR | 1 |
Calvert, AH; Dady, PJ; Grzelakowska-Sztabert, B; Harrap, KR; Jones, TR; Paine, RM; Taylor, GA | 1 |
Boyle, FT; Brown, M; Brunton, L; Jackman, AL; Kimbell, R | 1 |
Bavetsias, V; Bisset, GM; Boyle, FT; Brown, M; Brunton, L; Hughes, LR; Jackman, AL; Kimbell, R; Marsham, P | 1 |
Aherne, GW; Boyle, FT; Brown, M; Gibson, W; Hardcastle, A; Jackman, AL; Kelland, LR; Kimbell, R | 1 |
Bleasdale, C; Bowman, K; Calvert, AH; Curtin, NJ; Durkacz, BW; Griffin, RJ; Newell, DR; Pemberton, LC; Porteous, JK; Rhodes, D | 1 |
Boyle, FT; Brown, M; Brunton, L; Harrap, KR; Jackman, AL; Kimbell, R; Wardleworth, JM | 1 |
Barker, AJ; Boyle, FT; Calvert, AH; Hughes, LR; Jackman, AL; Kimbell, R; Marsham, PR; O'Connor, BM; Pegg, SJ; Wardleworth, JM | 1 |
Chong, LK; Tattersall, MH | 1 |
Harrap, KR | 1 |
Braña, MF; Castellano, JM; Keilhauer, G; Machuca, A; Martín, Y; Redondo, C; Schlick, E; Walker, N | 1 |
Chen, XH; Dai, ZR; Liu, JQ; Meng, XY; Yu, AZ; Zhang, XP | 1 |
Fetzer, OS; Freisheim, JH; Hynes, JB; Shane, B | 1 |
Freisheim, JH; Hagan, RL; Hynes, JB; Shane, B | 1 |
Bavetsias, V; Bisset, GM; Calvert, AH; Gibson, W; Harrap, KR; Jackman, AL; Jodrell, DI; Kimbell, R; Smith, MN; Stephens, TC | 1 |
Boyle, FT; Brown, M; Hughes, LR; Jackman, AL; Kimbell, R; Matusiak, ZS; Slater, AM; Smith, MN; Stephens, TC | 1 |
Bavetsias, V; Bisset, GM; Boyle, FT; Jackman, AL; Pawelczak, K; Thornton, TJ | 1 |
Aherne, W; Boyle, FT; Hardcastle, A; Jackman, AL; Kimbell, R | 1 |
Boyle, FT; Jackman, AL; Jansen, G; Schornagel, JH; Westerhof, GR | 1 |
Banks, S; Dev, IK; Dickerson, SH; Duch, DS; Ferone, R; Heath, LS; Humphreys, J; Knick, V; Pendergast, W; Singer, S | 1 |
Bavetsias, V; Bisset, GM; Boyle, FT; Gibson, W; Jackman, AL; Kimbell, R | 1 |
Boyle, FT; Hennequin, LF; Jackman, AL; Kimbell, R; Marsham, PR; Wardleworth, JM | 1 |
Bartlett, CA; Boritzki, TJ; Hillard, JA; Howland, EF; Johnston, AL; Kosa, M; Margosiak, SA; Morse, CA; Shetty, BV; Webber, S | 1 |
Appelt, K; Bacquet, RJ; Bartlett, CA; Booth, CL; Herrmann, SM; Howland, EF; Janson, CA; Jones, TR; Kathardekar, V; Lewis, KK; Marzoni, GP; Matthews, DA; Moomaw, EW; Morse, CA; Palmer, CL; Smith, WW; Varney, MD; Villafranca, JE; Ward, RW; Webber, S; Webber, SE; Welsh, KM; White, J | 1 |
Aherne, GW; Boyle, FT; Brunton, L; Jackman, AL; Jansen, G; Kimbell, R; Smith, MN; Stephens, TC; Wardleworth, JM | 1 |
Bowman, KJ; Curtin, NJ; Golding, BT; Griffin, RJ; White, A | 1 |
Bowman, K; Calvert, AH; Curtin, NJ; Golding, BT; Griffin, RJ; Newell, DR; Pemberton, LC; Srinivasan, S | 1 |
Brunton, LA; Jackman, AL; Kimbell, R; Ormerod, MG; Skelton, LA; Titley, J | 1 |
Bowman, KJ; Calvert, AH; Curtin, NJ; Golding, BT; Griffin, RJ; Huang, B; Loughlin, PJ; Newell, DR; Turner, RN | 1 |
Boyle, FT; Brown, M; Hennequin, LF; Jackman, AL; Kimbell, R; Marsham, PR; Wardleworth, JM | 1 |
Jiang, L; Lee, PC; Rathod, PK; White, J | 1 |
Bavetsias, V; Boyle, FT; Jackman, AL; Kimbell, R; Marriott, JH; Matusiak, ZS; Melin, C | 1 |
Aherne, GW; Brunton, L; Clarke, SJ; Farrugia, DC; Jackman, AL | 1 |
Besson, T; Guillaumet, G; Lamazzi, C; Léonce, S; Pfeiffer, B; Rees, CW; Renard, P | 1 |
Ackland, SP; Sakoff, JA | 1 |
Bowman, KJ; Calvert, AH; Curtin, NJ; Newell, DR | 1 |
Bertino, JR; Chen, BK; Horváth, C | 1 |
Bertino, JR; Hynes, JB; Moroson, BA; Scanlon, KJ | 1 |
Allen, BA; Hillcoat, BL; Ledig, KW; McCormack, JJ | 1 |
Bertino, JR; Cashmore, AR; Elslager, EF; Moroson, BA; Sawicki, WL | 1 |
De Martino, G; Massa, S | 1 |
Buck, JM; D'Souza, L; Freisheim, JH; Hynes, JB | 1 |
Colvin, PL; Eason, DE; Garrett, CM; Hynes, JB | 1 |
Hynes, JB; Oatis, JE | 1 |
Garrett, CM; Hynes, JB | 1 |
Donsback, RC; Sirotnak, FM | 1 |
Bader, H; Beardsley, GP; DeYarman, MT; Freisheim, JH; Galivan, J; Kerwar, SS; Moroson, BA; O'Connor, BM; Rosowsky, A; Russello, O | 1 |
Barker, AJ; Bishop, JA; Burrows, KD; Hughes, LR; Jackman, AL; O'Connor, BM; Roberts, N; Warner, P | 1 |
Jackman, AL; Kimbell, R; Ward, WH | 1 |
Bishop, JA; Calvert, AH; Jackman, AL; Marsham, PR; O'Connor, BM; Thornton, TJ | 1 |
Galivan, J; Malik, ND; Piper, JR; Rhee, MS; Sirotnak, FM | 1 |
Gibson, W; Jackman, AL; Jodrell, DI; Stephens, TC | 1 |
Chen, XH; Dai, ZR; Liu, JQ; Xu, XG; Yu, AZ; Zhang, XP | 1 |
Goldman, ID; Mikulecky, DC; Rape, TJ; Seither, RL; Trent, DF | 2 |
Goldman, ID; Seither, RL; Trent, DF | 2 |
Brown, M; Calvert, AH; Gibson, W; Hughes, LR; Jackman, AL; Judson, IR; Kimbell, R; Taylor, GA | 1 |
Chen, XH; Meng, XY; Yu, AZ; Zhang, XP | 1 |
Atassi, G; Baron, M; Bissery, MC; Cros, S; Gebel-Servolles, P; Giorgi-Renault, S; Lavelle, F; Paoletti, C; Renault, J | 1 |
Calvert, AH; Flinn, A; Jackman, AL; Jones, TR; O'Connor, BM; Thornton, TJ; Warner, P | 1 |
Bishop, JA; Calvert, AH; Hayter, AJ; Hughes, LR; Jackman, AL; Marsham, PR; O'Connor, BM; Oldfield, J; Wardleworth, JM | 1 |
Bishop, JA; Calvert, AH; Daw, MR; Hayter, AJ; Hughes, LR; Jackman, AL; Marsham, PR; O'Connor, BM; Snowden, JL | 1 |
Dexter, DL; Dusak, BA; Hamel, E; Hesson, DP; Jiang, JB; Kang, GJ | 1 |
Matherly, LH; Muench, SP | 1 |
Keyomarsi, K; Moran, RG | 1 |
Fry, DW | 1 |
Bishop, JA; Burrows, KD; Calvert, AH; Hughes, LR; Jackman, AL; Jones, TR; Marsham, PR; O'Connor, BM; Oldfield, J; Smith, RC | 1 |
Bishop, JA; Calvert, AH; Hughes, LR; Jackman, AL; Jones, TR; Marsham, PR; O'Connor, BM; Thornton, TJ | 1 |
Bishop, JA; Bisset, GM; Calvert, AH; Hughes, LR; Jackman, AL; Marsham, PR; O'Connor, BM; Oldfield, J; Thornton, TJ | 1 |
Berman, EM; Fry, DW; McNamara, DJ; Werbel, LM | 1 |
Barlowe, CK; Goldman, ID; Matherly, LH | 1 |
Calvert, AH; Jackman, AL; Jones, TR; Newell, DR; Sikora, E; Simmonds, AJ | 1 |
Calvert, AH; Jackman, AL; Newell, DR; Sikora, E | 1 |
Gaumont, Y; Kisliuk, RL; Murthy, BR; Nair, MG; Piper, JR; Sirotnak, FM; Thorndike, J | 1 |
Bertino, JR; Chou, TC; Romanini, A; Sherwood, RF; Sobrero, AF | 1 |
Balmanno, K; Calvert, AH; Hughes, LR; Jackman, AL; Taylor, GA | 1 |
Chen, GD; Dai, ZR; Li, BS; Li, GY; Xin, ZM; Zhang, XP; Zhou, WC | 1 |
Li, BS; Li, GD; Xin, ZM; Zhang, XP; Zhou, WC | 1 |
Calvert, AH; Flinn, A; Jackman, AL; Jones, TR; Newell, DR; Thornton, TJ | 1 |
Cole, A; Freisheim, JH; Hagan, RL; Hynes, JB; Kohler, W; Patil, SA | 1 |
Goldman, ID; Matherly, LH; Schuetz, JD; Westin, EH | 1 |
Bishop, JA; Calvert, AH; Chambers, P; Hayter, AJ; Hughes, LR; Jackman, AL; Marsham, PR; O'Connor, BM | 1 |
Betteridge, RF; Calvert, AH; Jackman, AL; Jones, TR; Neidle, S | 1 |
Griswold, DP; Hook, KE; Leopold, WR; Nelson, JM; Roberts, BJ | 1 |
Alison, DL; Calvert, AH; Harrap, KR; Jackman, AL | 1 |
Gaumont, Y; Hsiao, MC; Kalman, TI; Kisliuk, RL; Nair, IG; Nair, MG; Nanavati, NT | 1 |
Atassi, G; Dumont, P; Kabbe, HJ; Yoder, O | 1 |
Crossley, PH; Imam, AM; Jackman, AL; Little, PF | 1 |
Betteridge, RF; Calvert, AH; Davies, LC; Harrap, KR; Jackman, AL; Jones, TR; Smithers, MJ; Taylor, MA | 1 |
Gale, GR; Hynes, JB; Smith, AB | 1 |
Cheng, YC; Dutschman, GE; Fisher, MH; Nair, MG; Nanavathi, NT; Starnes, MC | 1 |
Freisheim, JH; Hynes, JB; Kumar, A; Susten, SS | 1 |
Betteridge, RF; Calvert, AH; Eakin, MA; Harland, SJ; Hayter, AJ; Jackman, AL; Jones, TR; Newell, DR; Smithers, MJ; Stocker, A | 1 |
McCormack, JJ; Richter, WE | 1 |
Donsbach, RC; Sirotnak, FM | 2 |
Atwell, GJ; Cain, BF | 1 |
Modest, EJ; Rosowsky, A | 1 |
Hutchison, DJ | 2 |
Buskirk, HH; Li, LH; Moxley, TE; Neil, GL | 1 |
Bertino, JR; Capizzi, RL; Cashmore, AR; Johns, DG; Nahas, A | 1 |
Abboud, G; Bertino, JR; Fölsch, E; Gralla, E | 1 |
4 review(s) available for quinazolines and Leukemia L 1210
Article | Year |
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The antitumour activity of ZD9331, a non-polyglutamatable quinazoline thymidylate synthase inhibitor.
Topics: Animals; Antineoplastic Agents; Biological Transport; Clinical Trials, Phase II as Topic; Drug Resistance; Humans; Leukemia L1210; Methotrexate; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1994 |
Initiatives with platinum- and quinazoline-based antitumor molecules--Fourteenth Bruce F. Cain Memorial Award Lecture.
Topics: Animals; Antineoplastic Agents; Cisplatin; Drug Resistance; Female; Humans; Leukemia L1210; Mice; Neoplasm Transplantation; Organoplatinum Compounds; Ovarian Neoplasms; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase | 1995 |
Synthesis and biological activity of tricyclic antifolate compounds with fixed geometry.
Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Carcinoma; Cell Line; Chickens; Enterococcus faecalis; Folic Acid Antagonists; Humans; Leukemia L1210; Liver; Malaria; Mammary Neoplasms, Experimental; Mice; Mouth Neoplasms; Pyrimethamine; Quinazolines; Structure-Activity Relationship | 1971 |
New approaches to chemotherapy.
Topics: Administration, Oral; Aminopterin; Animals; Enterococcus faecalis; Folic Acid Antagonists; Injections, Intraperitoneal; Lethal Dose 50; Leukemia L1210; Methotrexate; Mice; Mice, Inbred Strains; Quinazolines | 1971 |
117 other study(ies) available for quinazolines and Leukemia L 1210
Article | Year |
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3-(5-Nitro-2-thienyl)-9-chloro-5-morpholin-4-yl[1,2,4]triazolo[4,3-c]quinazoline induces ROS-mitochondrial mediated death signaling and activation of p38 MAPK in murine L1210 leukemia cells.
Topics: Animals; Apoptosis; Caspase 3; Cytochromes c; Enzyme Activation; JNK Mitogen-Activated Protein Kinases; Leukemia L1210; Membrane Potential, Mitochondrial; Mice; Mitochondria; Molecular Structure; p38 Mitogen-Activated Protein Kinases; Poly(ADP-ribose) Polymerases; Quinazolines; Reactive Oxygen Species; Signal Transduction; Triazoles | 2009 |
Bioactivity of synthetic 2-halo-3-aryl-4(3H)-quinazoliniminium halides in L1210 leukemia and SK-BR-3 mammary tumor cells in vitro.
Topics: Animals; Breast Neoplasms; Cell Growth Processes; Cell Line, Tumor; DNA, Neoplasm; Female; Humans; Ki-67 Antigen; Leukemia L1210; Mice; Quinazolines | 2011 |
Novel nonclassical antifolate, 2-[N-(2´-Hydroxyethyl)amino]methyl-3H-quinazolin-4-one, with a potent antineoplastic activity toward leukemia cells.
Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Survival; Cisplatin; Dacarbazine; Female; Folic Acid Antagonists; Humans; Leukemia; Leukemia L1210; Male; Mice; Mice, Inbred DBA; Mitogen-Activated Protein Kinases; Quinazolines; Temozolomide; U937 Cells | 2012 |
Induction of cytotoxicity and ssDNA breaks by 9-bromo-5-morpholino-tetrazolo[1,5-c]quinazoline in tumor cells cultured in vitro.
Topics: Animals; Antineoplastic Agents; Apoptosis; Caco-2 Cells; Cell Cycle; Cell Survival; Comet Assay; DNA, Single-Stranded; Humans; Leukemia L1210; Mice; Quinazolines; Tetrazoles; Tumor Cells, Cultured | 2003 |
Synthesis and antileukemic activity of new 3-(1-phenyl-3-methylpyrazol-5-yl)-2-styrylquinazolin-4(3H)-ones.
Topics: Animals; Antineoplastic Agents; Cell Division; Dogs; HL-60 Cells; Humans; Indicators and Reagents; K562 Cells; Leukemia; Leukemia L1210; Magnetic Resonance Spectroscopy; Quinazolines; Structure-Activity Relationship | 2004 |
Synthesis and antileukemic activity of new 3-(5-methylisoxazol-3-yl) and 3-(pyrimidin-2-yl)-2-styrylquinazolin-4(3H)-ones.
Topics: Animals; Antineoplastic Agents; Colchicine; Czech Republic; Drug Evaluation, Preclinical; HL-60 Cells; Humans; K562 Cells; Leukemia L1210; Molecular Structure; Oxazoles; Quinazolines | 2004 |
The antifolate activity of tea catechins.
Topics: Animals; Catechin; Cattle; Chickens; Enzyme Inhibitors; Folic Acid Antagonists; Humans; Kinetics; Leukemia L1210; Liver; Mice; Models, Molecular; Quinazolines; Tea; Tetrahydrofolate Dehydrogenase | 2005 |
BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors.
Topics: Animals; Apoptosis; Biological Transport; Carrier Proteins; Cell Proliferation; Choriocarcinoma; Enzyme Inhibitors; Female; Folate Receptors, GPI-Anchored; Folic Acid; Humans; Idoxuridine; Iodine Radioisotopes; Leukemia L1210; Lung Neoplasms; Membrane Transport Proteins; Mice; Mice, Nude; Ovarian Neoplasms; Quinazolines; Receptors, Cell Surface; Reduced Folate Carrier Protein; Thymidylate Synthase; Tissue Distribution; Transplantation, Heterologous; Tumor Cells, Cultured | 2005 |
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
Topics: Animals; Antimalarials; Antineoplastic Agents; Bacteria; Drug Resistance; Folic Acid Antagonists; Haplorhini; Leukemia L1210; Leukemia P388; Mice; Plasmodium falciparum; Quinazolines; Trimetrexate | 1983 |
Uptake and efficacy of trimetrexate (TMQ, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline), a non-classical antifolate in methotrexate-resistant leukemia cells in vitro.
Topics: Animals; Drug Resistance; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Trimetrexate | 1984 |
Biochemical pharmacology of the lipophilic antifolate, trimetrexate.
Topics: Animals; Cell Line; Culture Techniques; Deoxyuridine; Drug Resistance; Folic Acid; Folic Acid Antagonists; Humans; Kinetics; Leucovorin; Leukemia L1210; Lymphocytes; Methotrexate; Mice; Mice, Inbred Strains; Quinazolines; Ribonucleotides; Thymidine; Trimetrexate | 1984 |
Modulation of anti-metabolite effects. Effects of thymidine on the efficacy of the quinazoline-based thymidylate synthetase inhibitor, CB3717.
Topics: Animals; Antimetabolites, Antineoplastic; Cells, Cultured; Deoxyuridine; Folic Acid; Leukemia L1210; Male; Methyltransferases; Mice; Mice, Inbred DBA; Quinazolines; Thymidine; Thymidylate Synthase | 1984 |
Antitumor activity of a water-insoluble compound entrapped in liposomes on L1210 leukemia in mice.
Topics: Animals; Chromatography, Gel; Dose-Response Relationship, Drug; Female; In Vitro Techniques; Injections, Intraperitoneal; Injections, Intravenous; Leukemia L1210; Liposomes; Male; Mice; Mice, Inbred Strains; Neoplasm Transplantation; Quinazolines | 1983 |
Heterocyclic Quinones. 4. A new highly cytotoxic drug: 6,7-bis(1-aziridinyl)-5,8-quinazolinedione.
Topics: Animals; Antineoplastic Agents; Leukemia L1210; Leukemia P388; Mice; Mutagenicity Tests; Quinazolines; Sarcoma 180 | 1983 |
Inhibition of thymidylate synthetase by the new quinazoline antifolate, CB 3717; enzyme purification and kinetics.
Topics: Animals; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Methyltransferases; Mice; Quinazolines; Thymidylate Synthase | 1984 |
Plasma nucleoside and base levels following treatment with the new thymidylate synthetase inhibitor CB 3717.
Topics: Animals; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Methyltransferases; Mice; Mice, Inbred Strains; Nucleosides; Purines; Pyrimidines; Quinazolines; Thymidylate Synthase | 1984 |
Biochemical and antitumor effects of 5,8-dideazaisopteroylglutamate, a unique quinazoline inhibitor of thymidylate synthase.
Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Cell Line; Colonic Neoplasms; Female; Folic Acid Antagonists; Humans; Leukemia L1210; Methotrexate; Methyltransferases; Mice; Mice, Inbred C57BL; Quinazolines; Thymidylate Synthase | 1983 |
A potent antitumour quinazoline inhibitor of thymidylate synthetase: synthesis, biological properties and therapeutic results in mice.
Topics: Animals; Antineoplastic Agents; Cell Survival; Cells, Cultured; Dose-Response Relationship, Drug; Female; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Methyltransferases; Mice; Mice, Inbred C57BL; Quinazolines; Thymidylate Synthase | 1981 |
Quinazoline antifolates with dual biochemical loci of action. Biochemical and biological studies directed towards overcoming methotrexate resistance.
Topics: Animals; Cell Survival; Female; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Thymidylate Synthase | 1980 |
Quinazoline thymidylate synthase inhibitors: methods for assessing the contribution of polyglutamation to their in vitro activity.
Topics: Animals; Biological Transport; Cell Division; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Leucovorin; Leukemia L1210; Methotrexate; Peptide Synthases; Polyglutamic Acid; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Substrate Specificity; Thymidylate Synthase | 1995 |
Quinazoline-based thymidylate synthase inhibitors: relationship between structural modifications and polyglutamation.
Topics: Animals; Antineoplastic Agents; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Glutamates; Leukemia L1210; Peptide Synthases; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1995 |
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 |
Novel potent inhibitors of the DNA repair enzyme poly(ADP-ribose)polymerase (PARP).
Topics: Animals; Benzoxazoles; Binding Sites; Enzyme Inhibitors; Humans; Leukemia L1210; Poly(ADP-ribose) Polymerase Inhibitors; Quinazolines | 1995 |
Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series.
Topics: Animals; Antineoplastic Agents; Folic Acid; Folic Acid Antagonists; Glutamic Acid; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1995 |
5,10-Dideazatetrahydrofolic acid reduces toxicity and deoxyadenosine triphosphate pool, expansion in cultured L1210 cells treated with inhibitors of thymidylate synthase.
Topics: Animals; Cell Survival; Deoxyadenine Nucleotides; Drug Interactions; Floxuridine; Folic Acid; Hypoxanthine; Hypoxanthines; Leukemia L1210; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1995 |
Benzimidazo[1,2-c]quinazolines: a new class of antitumor compounds.
Topics: Animals; Antineoplastic Agents; Benzimidazoles; Breast Neoplasms; Cell Division; Colonic Neoplasms; Crystallography, X-Ray; DNA; Humans; Intercalating Agents; Leukemia L1210; Molecular Conformation; Molecular Structure; Osteosarcoma; Quinazolines; Tumor Cells, Cultured | 1994 |
[Synthesis and biological activities of 2,4-diamino-5-fluoro-6-substituted benzylamino quinazolines].
Topics: Animals; Antimalarials; Antineoplastic Agents; Leukemia L1210; Malaria; Mice; Plasmodium berghei; Quinazolines; Tumor Cells, Cultured | 1994 |
Synthesis and preliminary biological evaluation of analogues of 5,8-dideazaisofolic acid and its 2-desamino-2-methyl derivative containing fluorine at position five.
Topics: Animals; Cell Survival; Fluorine; Folic Acid Antagonists; Leukemia L1210; Liver; Methotrexate; Mice; Peptide Synthases; Quinazolines; Structure-Activity Relationship; Swine; Tumor Cells, Cultured | 1993 |
Synthesis and biological evaluation of analogues of 5,8-dideazaisofolic acid (IAHQ) modified at positions 2, 4 and 9.
Topics: Animals; Cell Survival; Folic Acid Antagonists; Kinetics; Leukemia L1210; Liver; Mice; Peptide Synthases; Quinazolines; Structure-Activity Relationship; Swine; Tumor Cells, Cultured | 1993 |
Gamma-linked dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8- dideazafolate as antitumour agents.
Topics: Animals; Antineoplastic Agents; Dipeptides; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase | 1993 |
Substituted-2-desamino-2-methyl-quinazolinones. A series of novel antitumour agents.
Topics: Animals; Antineoplastic Agents; Cell Division; Drug Screening Assays, Antitumor; Folic Acid; Leukemia L1210; Mice; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
Quinazoline antifolates inhibiting thymidylate synthase: synthesis of gamma-linked peptide and amide analogues of 2-desamino-2-methyl-N10-propargyl- 5,8-dideazafolic acid (ICI 198583).
Topics: Animals; Cell Division; Drug Screening Assays, Antitumor; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Molecular Structure; Peptides; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
The duration of the inhibition of thymidylate synthase in intact L1210 cells exposed to two different classes of quinazoline analogues.
Topics: Animals; Antineoplastic Agents; Cell Division; Deoxyuracil Nucleotides; Drug Screening Assays, Antitumor; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Thymine Nucleotides | 1993 |
The reduced folate/methotrexate carrier and a membrane-associated folate binding protein as transport routes for novel antifolates: structure-activity relationships.
Topics: Animals; Biological Transport; Carrier Proteins; Folate Receptors, GPI-Anchored; Folic Acid Antagonists; Kinetics; Leukemia L1210; Mice; Quinazolines; Receptors, Cell Surface; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase.
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 |
Quinazoline antifolate thymidylate synthase inhibitors: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
Topics: Animals; Antineoplastic Agents; Cell Division; Dipeptides; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Molecular Structure; Quinazolines; Stereoisomerism; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1996 |
Quinazoline antifolates thymidylate synthase inhibitors: lipophilic analogues with modification to the C2-methyl substituent.
Topics: Animals; Folic Acid Antagonists; Leukemia L1210; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured; X-Ray Diffraction | 1996 |
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 |
Structure-based design of lipophilic quinazoline inhibitors of thymidylate synthase.
Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Binding Sites; Cell Line; Crystallography, X-Ray; Drug Design; Enzyme Inhibitors; Escherichia coli; Folic Acid Antagonists; Humans; Leukemia; Leukemia L1210; Mice; Models, Molecular; Molecular Conformation; Molecular Structure; Protein Conformation; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1996 |
Cellular pharmacology and in vivo activity of a new anticancer agent, ZD9331: a water-soluble, nonpolyglutamatable, quinazoline-based inhibitor of thymidylate synthase.
Topics: Animals; Antineoplastic Agents; Biological Transport; Cell Division; Female; Humans; Kinetics; Leucovorin; Leukemia L1210; Leukemia L5178; Methotrexate; Mice; Mice, Inbred DBA; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured; Tumor Stem Cell Assay | 1997 |
Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064.
Topics: Amides; Animals; Antimetabolites, Antineoplastic; Antineoplastic Agents; Antineoplastic Agents, Alkylating; Benzimidazoles; Bleomycin; Cell Death; Dacarbazine; DNA Damage; DNA Methylation; DNA Repair; Dose-Response Relationship, Drug; Drug Interactions; Drug Resistance, Neoplasm; Drug Synergism; Enzyme Inhibitors; Gamma Rays; Leukemia L1210; Mice; Poly(ADP-ribose) Polymerase Inhibitors; Poly(ADP-ribose) Polymerases; Quinazolines; Tumor Cells, Cultured | 1998 |
Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP).
Topics: Alkylating Agents; Animals; Antineoplastic Agents; Cell Survival; Dacarbazine; DNA Repair; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Drug Synergism; Enzyme Inhibitors; Gamma Rays; Leukemia L1210; Mice; Poly(ADP-ribose) Polymerase Inhibitors; Quinazolines; Structure-Activity Relationship; Tumor Cells, Cultured | 1998 |
A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus.
Topics: Animals; Antineoplastic Agents; Cell Cycle; Cell Division; Cell Survival; Chemical Precipitation; Colony-Forming Units Assay; Cytoprotection; DNA, Neoplasm; Folic Acid; Humans; Leukemia L1210; Lipid Metabolism; Mice; Quinazolines; Solubility; Tumor Cells, Cultured | 1999 |
Potentiation of the cytotoxicity of thymidylate synthase (TS) inhibitors by dipyridamole analogues with reduced alpha1-acid glycoprotein binding.
Topics: Animals; Antineoplastic Agents; Biological Transport; Cell Division; Cell Survival; Dipyridamole; Drug Synergism; Enzyme Inhibitors; Folic Acid; Leukemia L1210; Mice; Molecular Structure; Orosomucoid; Protein Binding; Quinazolines; Structure-Activity Relationship; Thymidine; Thymidylate Synthase; Tumor Cells, Cultured | 1999 |
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.
Topics: Animals; Antineoplastic Agents; Drug Design; Enzyme Inhibitors; Folic Acid Antagonists; Leukemia L1210; Mice; Models, Chemical; Quinazolines; Thymidylate Synthase | 1999 |
Potent and selective activity of a combination of thymidine and 1843U89, a folate-based thymidylate synthase inhibitor, against Plasmodium falciparum.
Topics: Animals; Cell Division; Enzyme Inhibitors; Erythrocytes; Folic Acid Antagonists; Indoles; Isoindoles; Kinetics; Leukemia L1210; Mice; Plasmodium falciparum; Quinazolines; Thymidine; Thymidylate Synthase | 2000 |
Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).
Topics: Animals; Antineoplastic Agents; Cell Division; Drug Design; Enzyme Inhibitors; Folic Acid Antagonists; Glutamates; Leukemia L1210; Methotrexate; Mice; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tritium; Tumor Cells, Cultured | 2000 |
Leucovorin rescue from raltitrexed (tomudex)-induced antiproliferative effects: in vitro cell line and in vivo mouse studies.
Topics: Animals; Antimetabolites, Antineoplastic; Body Weight; Cell Division; Cell Line; Drug Interactions; Humans; Intestinal Mucosa; Intestine, Small; Leucovorin; Leukemia L1210; Lymphocytes; Male; Mice; Mice, Inbred BALB C; Neutropenia; Polyglutamic Acid; Quinazolines; Thiophenes; Thrombocytopenia | 2000 |
Expeditious synthesis and cytotoxic activity of new cyanoindolo[3,2-c]quinolines and benzimidazo[1,2-c]quinazolines.
Topics: Animals; Cell Division; HT29 Cells; Humans; Leukemia L1210; Mice; Molecular Structure; Quinazolines; Quinolines | 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 |
Differential effects of the poly (ADP-ribose) polymerase (PARP) inhibitor NU1025 on topoisomerase I and II inhibitor cytotoxicity in L1210 cells in vitro.
Topics: Animals; Antineoplastic Agents, Phytogenic; Apoptosis; Camptothecin; DNA Damage; DNA, Neoplasm; Drug Screening Assays, Antitumor; Drug Synergism; Enzyme Inhibitors; Etoposide; Leukemia L1210; Nucleic Acid Synthesis Inhibitors; Proteins; Quinazolines; Topoisomerase I Inhibitors; Topoisomerase II Inhibitors | 2001 |
Multivariate analysis and quantitative structure-activity relationships. Inhibition of dihydrofolate reductase and thymidylate synthetase by quinazolines.
Topics: Analysis of Variance; Animals; Factor Analysis, Statistical; Folic Acid Antagonists; Humans; In Vitro Techniques; Lacticaseibacillus casei; Leukemia L1210; Leukemia, Lymphoid; Methyltransferases; Mice; Models, Biological; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1979 |
Quinazoline analogues of folic acid as inhibitors of thymidylate synthetase from bacterial and mammalian sources.
Topics: Animals; Cell Division; Folic Acid; In Vitro Techniques; Lacticaseibacillus casei; Leukemia L1210; Methyltransferases; Mice; Neoplasms, Experimental; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1979 |
Inhibition of dihydrofolate reductases by derivatives of 2,4-diaminopyrroloquinazoline.
Topics: Animals; Crithidia; Folic Acid Antagonists; In Vitro Techniques; Kinetics; Lacticaseibacillus casei; Leukemia L1210; Liver; Quinazolines; Rats | 1979 |
2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline (tmq), a potent non-classical folate antagonist inhibitor--I effect on dihydrofolate reductase and growth of rodent tumors in vitro and in vivo.
Topics: Animals; Antineoplastic Agents; Folic Acid Antagonists; Humans; In Vitro Techniques; Leukemia L1210; Mice; Neoplasms, Experimental; Quinazolines | 1979 |
[Research on substances with antiblastic activity. LXII. Synthesis and antineoplastic activity of pyrrolo-[2,1-b] quinazoline derivatives and of 4H-pyrrolo[2,1-b] [1,3] benzodiazepine derivatives].
Topics: Animals; Antineoplastic Agents; Benzodiazepines; Drug Evaluation, Preclinical; Leukemia L1210; Mice; Pyrroles; Quinazolines | 1978 |
Quinazolines as inhibitors of dihydrofolate reductase. 3. Analogs of pteroic and isopteroic acids.
Topics: Animals; Enterococcus faecalis; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Liver; Malaria; Mice; Plasmodium berghei; Pterins; Quinazolines; Rats | 1975 |
Quinazolines as inhibitors of dihydrofolate reductase. 4. Classical analogues of folic and isofolic acids.
Topics: Animals; Antineoplastic Agents; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Liver; Mice; Quinazolines; Rats; Streptococcus; Structure-Activity Relationship | 1977 |
Sycnthesis of quinazoline analogues of folic acid modified at postion 10.
Topics: Animals; Antineoplastic Agents; Folic Acid; Leukemia L1210; Mice; Quinazolines | 1977 |
Synthesis of quinazoline analogs of isofolic acid.
Topics: Animals; Folic Acid; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Liver; Mice; Quinazolines; Rats; Structure-Activity Relationship | 1975 |
Further evidence for a basis of selective activity and relative responsiveness during antifolate therapy of murine tumors.
Topics: Aminopterin; Animals; Aspartic Acid; Carcinoma, Ehrlich Tumor; Chick Embryo; DNA, Neoplasm; Folic Acid Antagonists; Intestine, Small; Leukemia L1210; Liver; Lymphoma; Methotrexate; Mice; Mice, Inbred C57BL; Neoplasms, Experimental; Quinazolines; Sarcoma 180; Tetrahydrofolate Dehydrogenase; Time Factors | 1975 |
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 |
Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents.
Topics: Animals; Cell Survival; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1992 |
Kinetic characteristics of ICI D1694: a quinazoline antifolate which inhibits thymidylate synthase.
Topics: Animals; Binding Sites; Cell Division; Kinetics; Leukemia L1210; Mice; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1992 |
Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogues.
Topics: Animals; Antineoplastic Agents; Benzene; Cell Division; Fluorine; Folic Acid Antagonists; Leukemia L1210; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1992 |
Synthesis and antifolate evaluation of the 10-propargyl derivatives of 5-deazafolic acid, 5-deazaaminopterin, and 5-methyl-5-deazaaminopterin.
Topics: Aminopterin; Animals; Cell Division; Folic Acid; Folic Acid Antagonists; Humans; Leukemia L1210; Mammary Neoplasms, Experimental; Mice; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1992 |
ICI D1694, an inhibitor of thymidylate synthase for clinical study.
Topics: Animals; Breast Neoplasms; Cell Line; Cell Survival; Drug Screening Assays, Antitumor; Female; Folic Acid Antagonists; Humans; Leukemia L1210; Mice; Neoplasms, Experimental; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1991 |
[Synthesis and biological activities of 2,4-diamino-5-chloro-6-substituted quinazolines].
Topics: Animals; Anti-Bacterial Agents; Antimalarials; Antineoplastic Agents; Leukemia L1210; Melanoma, Experimental; Mice; Microbial Sensitivity Tests; Plasmodium berghei; Quinazolines; Streptococcus pneumoniae; Tumor Cells, Cultured | 1991 |
Effect of direct suppression of thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site on the interconversion of tetrahydrofolate cofactors to dihydrofolate by antifolates. Influence of degree of dihydrofolate reductase inhibition.
Topics: Animals; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Methotrexate; Mice; Quinazolines; Quinazolinones; Tetrahydrofolates; Thermodynamics; Thymidylate Synthase; Trimetrexate; Tumor Cells, Cultured | 1991 |
Rate and extent of interconversion of tetrahydrofolate cofactors to dihydrofolate after cessation of dihydrofolate reductase activity in stationary versus log phase L1210 leukemia cells.
Topics: Animals; Cell Cycle; DNA, Neoplasm; Flow Cytometry; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Thermodynamics; Trimetrexate; Tumor Cells, Cultured | 1991 |
Compartmentation of intracellular folates. Failure to interconvert tetrahydrofolate cofactors to dihydrofolate in mitochondria of L1210 leukemia cells treated with trimetrexate.
Topics: Animals; Cell Compartmentation; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Mitochondria; Quinazolines; Tetrahydrofolates; Trimetrexate; Tumor Cells, Cultured | 1991 |
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 |
[Synthesis and antibacterial as well as antineoplastic activities of 2,4-diamino-5-methyl-6-(N-methyl-substituted benzyl) aminoquinazolines].
Topics: Animals; Anti-Bacterial Agents; Antineoplastic Agents; Leukemia L1210; Quinazolines; Staphylococcus; Tumor Cells, Cultured | 1991 |
Heterocyclic quinones. 17. A new in vivo active antineoplastic drug: 6,7-bis(1-aziridinyl)-4-[[3-(N,N-dimethylamino)propyl]amino]-5,8- quinazolinedione.
Topics: Animals; Antineoplastic Agents; Aziridines; Breast Neoplasms; Cell Division; Cell Line; Drug Screening Assays, Antitumor; Female; Humans; Leukemia L1210; Leukemia, Experimental; Melanoma, Experimental; Mice; Mice, Inbred C57BL; Mice, Inbred DBA; Molecular Structure; Neoplasms, Experimental; Quinazolines; Sarcoma, Experimental; Structure-Activity Relationship | 1991 |
Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogues.
Topics: Animals; Cell Division; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1991 |
Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications.
Topics: Animals; Antineoplastic Agents; Cell Division; Chemical Phenomena; Chemistry; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1991 |
Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogues in the C2-methyl series.
Topics: Animals; Bridged-Ring Compounds; Cell Line; Chemical Phenomena; Chemistry; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1991 |
Synthesis and biological evaluation of 2-styrylquinazolin-4(3H)-ones, a new class of antimitotic anticancer agents which inhibit tubulin polymerization.
Topics: Animals; Antineoplastic Agents; Humans; Leukemia L1210; Mice; Microtubules; Quinazolines; Structure-Activity Relationship; Styrenes; Tubulin; Tumor Cells, Cultured | 1990 |
Evidence for a localized conversion of endogenous tetrahydrofolate cofactors to dihydrofolate as an important element in antifolate action in murine leukemia cells.
Topics: Animals; Antineoplastic Agents; Chromatography, High Pressure Liquid; Folic Acid Antagonists; Leucovorin; Leukemia L1210; Mice; Quinazolines; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Trimetrexate; Tumor Cells, Cultured | 1990 |
Quinazoline folate analogs inhibit the catalytic activity of thymidylate synthase but allow binding of 5-fluorodeoxyuridylate.
Topics: Animals; Binding Sites; Cytidine Monophosphate; Floxuridine; Fluorodeoxyuridylate; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Mice; Models, Structural; Protein Binding; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
Cytotoxic synergism between trimetrexate and etoposide. Evidence that trimetrexate potentiates etoposide-induced protein-associated DNA strand breaks in L1210 leukemia cells through alterations in intracellular ATP concentrations.
Topics: Adenosine Triphosphate; Animals; Antineoplastic Combined Chemotherapy Protocols; Cell Survival; DNA Damage; DNA, Neoplasm; Etoposide; Leukemia L1210; Mice; Quinazolines; Trimetrexate; Tumor Cells, Cultured | 1990 |
Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C2 position.
Topics: Animals; Antineoplastic Agents; Cell Division; Chemical Phenomena; Chemistry; Chemistry, Physical; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Liver; Mice; Molecular Structure; Quinazolines; Rats; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
Quinazoline antifolate thymidylate synthase inhibitors: 2'-fluoro-N10-propargyl-5,8-dideazafolic acid and derivatives with modifications in the C2 position.
Topics: Animals; Antineoplastic Agents; Cell Division; Chemical Phenomena; Chemistry; Drug Resistance; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
Quinazoline antifolate thymidylate synthase inhibitors: benzoyl ring modifications in the C2-methyl series.
Topics: Animals; Antineoplastic Agents; Arginine; Cell Division; Folic Acid Antagonists; Leukemia L1210; Mice; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
Potent inhibition of thymidylate synthase by two series of nonclassical quinazolines.
Topics: Animals; Antineoplastic Agents; Cell Division; Cell Line; Enzyme Inhibitors; Folic Acid Antagonists; Humans; Indicators and Reagents; Leukemia L1210; Magnetic Resonance Spectroscopy; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1990 |
Antifolate polyglutamylation and competitive drug displacement at dihydrofolate reductase as important elements in leucovorin rescue in L1210 cells.
Topics: Animals; Cell Survival; Folic Acid Antagonists; Leucovorin; Leukemia L1210; Methotrexate; Mice; Polyglutamic Acid; Quinazolines; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Trimetrexate | 1986 |
Development of an assay for the estimation of N10-propargyl-5,8-dideazafolic acid polyglutamates in tumor cells.
Topics: Animals; Chromatography, High Pressure Liquid; Folic Acid; Leukemia L1210; Mice; Neoplasms; Peptides; Polyglutamic Acid; Quinazolines; Thymidylate Synthase | 1988 |
Formation and retention and biological activity of N10-propargyl-5,8-dideazafolic acid (CB3717) polyglutamates in L1210 cells in vitro.
Topics: Animals; Biotransformation; Chromatography, High Pressure Liquid; Folic Acid; Leukemia L1210; Mice; Peptides; Polyglutamic Acid; Quinazolines; Thymidylate Synthase; Time Factors | 1988 |
Inhibition of glycinamide ribonucleotide formyltransferase and other folate enzymes by homofolate polyglutamates in human lymphoma and murine leukemia cell extracts.
Topics: Acyltransferases; Animals; Folic Acid; Humans; Hydroxymethyl and Formyl Transferases; Kinetics; Leukemia L1210; Lymphoma; Mice; Molecular Conformation; Phosphoribosylaminoimidazolecarboxamide Formyltransferase; Phosphoribosylglycinamide Formyltransferase; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Trimetrexate | 1989 |
Enhancement of trimetrexate cytotoxicity in vitro and in vivo by carboxypeptidase G2.
Topics: Animals; Cell Line; Cell Survival; Clone Cells; Cysteine Endopeptidases; Drug Resistance; Drug Synergism; Folic Acid; gamma-Glutamyl Hydrolase; Humans; Leukemia L1210; Mice; Mice, Inbred Strains; Quinazolines; Trimetrexate; Tumor Stem Cell Assay | 1989 |
Folate-pool interconversions and inhibition of biosynthetic processes after exposure of L1210 leukemia cells to antifolates. Experimental and network thermodynamic analyses of the role of dihydrofolate polyglutamylates in antifolate action in cells.
Topics: Animals; Computer Simulation; Deoxyuridine; Floxuridine; Folic Acid; Folic Acid Antagonists; Formates; Leukemia L1210; Methotrexate; Mice; Purines; Pyrimidines; Quinazolines; Tetrahydrofolates; Thermodynamics; Thymidylate Synthase; Trimetrexate | 1989 |
Estimation of the in vitro and in vivo inhibitory effects of antifolates upon thymidylate synthase (TS) in whole cells.
Topics: Animals; Dose-Response Relationship, Drug; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Mice, Inbred DBA; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured | 1989 |
[Synthesis and antimalarial as well as antitumor activities of 2,4-diamino-6-(N-methyl-substituted benzylamino) quinazolines].
Topics: Animals; Antimalarials; Antineoplastic Agents; Leukemia L1210; Malaria; Mice; Plasmodium berghei; Quinazolines | 1989 |
[Synthesis and antimalarial as well as antitumor activities of 1-methyl-2,4-diamino-6-(N-methyl-substituted benzylamion) quinazolinium iodides].
Topics: Animals; Antimalarials; Antineoplastic Agents; Benzylamines; Chemical Phenomena; Chemistry; Diamines; Leukemia L1210; Mice; Plasmodium berghei; Quinazolines; Tumor Cells, Cultured | 1989 |
Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency.
Topics: Animals; Antineoplastic Agents; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Hydrogen Bonding; Leukemia L1210; Liver; Quinazolines; Rats; Solubility; Structure-Activity Relationship; Thymidylate Synthase | 1989 |
Comparison of the biological effects of selected 5,8-dideazafolate analogues with their 2-desamino counterparts.
Topics: Animals; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Humans; Leukemia L1210; Methotrexate; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1989 |
Evidence for a functional defect in the translocation of the methotrexate transport carrier in a methotrexate-resistant murine L1210 leukemia cell line.
Topics: Animals; Biological Transport; Carrier Proteins; Cell Membrane; Drug Resistance; Electrophoresis, Polyacrylamide Gel; Folate Receptors, GPI-Anchored; Gene Amplification; Leucovorin; Leukemia L1210; Methotrexate; Mice; Phenotype; Quinazolines; Receptors, Cell Surface; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase; Trimetrexate | 1988 |
Quinazoline antifolate thymidylate synthase inhibitors: nitrogen, oxygen, sulfur, and chlorine substituents in the C2 position.
Topics: Animals; Chemical Phenomena; Chemistry; Chlorine; Folic Acid Antagonists; Leukemia L1210; Mice; Nitrogen; Oxygen; Quinazolines; Structure-Activity Relationship; Sulfur; Thymidylate Synthase; Tumor Cells, Cultured | 1989 |
Quinazoline antifolates inhibiting thymidylate synthase: computer modelling of the N10 substituent.
Topics: Animals; Chemical Phenomena; Chemistry; Computer Simulation; Drug Design; Drug Evaluation, Preclinical; Folic Acid Antagonists; Leukemia L1210; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1989 |
Cell cycle effects of trimetrexate (CI-898).
Topics: Animals; Antineoplastic Agents; Cell Cycle; Cell Survival; Cells, Cultured; Cricetinae; Demecolcine; Drug Evaluation, Preclinical; Female; Flow Cytometry; Injections, Intraperitoneal; Interphase; Leukemia L1210; Methotrexate; Mice; Neoplasms, Experimental; Ovary; Quinazolines; Trimetrexate | 1986 |
Increased thymidylate synthase in L1210 cells possessing acquired resistance to N10-propargyl-5,8-dideazafolic acid (CB3717): development, characterization, and cross-resistance studies.
Topics: Animals; Antineoplastic Agents; Cells, Cultured; Deoxyuridine; Drug Resistance; Floxuridine; Fluorouracil; Folic Acid; Folic Acid Antagonists; Hypoxanthine; Hypoxanthines; Kinetics; Leukemia L1210; Mice; Quinazolines; Thymidylate Synthase; Tritium | 1986 |
Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).
Topics: Animals; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Lacticaseibacillus casei; Leukemia L1210; Quinazolines; Streptococcus; Structure-Activity Relationship; Thymidylate Synthase | 1986 |
A new antitumour agent, batracylin, selected by a preclinical solid tumour model.
Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Colonic Neoplasms; Drug Screening Assays, Antitumor; Leukemia L1210; Leukemia P388; Melanoma, Experimental; Mice; Quinazolines | 1988 |
Analysis of thymidylate synthase gene amplification and of mRNA levels in the cell cycle.
Topics: Animals; Cell Cycle; Cell Line; DNA; Folic Acid; Folic Acid Antagonists; Gene Amplification; Leukemia L1210; Mice; Nucleic Acid Hybridization; Quinazolines; RNA, Messenger; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase | 1987 |
Quinazoline antifolates inhibiting thymidylate synthase: variation of the amino acid.
Topics: Animals; Folic Acid Antagonists; Leukemia L1210; Mice; Models, Molecular; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1986 |
Effects of 5,8-dideazaisopteroylglutamate (IAHQ) on L1210 leukemia in mice when given alone and in combination with methotrexate, probenecid, or verapamil.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Folic Acid Antagonists; Leukemia L1210; Male; Methotrexate; Mice; Mice, Inbred DBA; Probenecid; Quinazolines; Time Factors; Verapamil | 1986 |
Activity of the new antifolate N10-propargyl-5,8-dideazafolate and its polyglutamates against human dihydrofolate reductase, human thymidylate synthetase, and KB cells containing different levels of dihydrofolate reductase.
Topics: Animals; Cell Division; Drug Resistance; Folic Acid; Folic Acid Antagonists; Humans; KB Cells; Lacticaseibacillus casei; Leukemia L1210; Mathematics; Methotrexate; Methyltransferases; Pteroylpolyglutamic Acids; Quinazolines; Thymidylate Synthase | 1985 |
Inhibition of dihydrofolate reductase, methotrexate transport, and growth of methotrexate-sensitive and -resistant L1210 leukemia cells in vitro by 5-substituted 2,4-diaminoquinazolines.
Topics: Animals; Biological Transport; Cells, Cultured; Drug Resistance; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Structure-Activity Relationship | 1985 |
Quinazoline antifolates inhibiting thymidylate synthase: variation of the N10 substituent.
Topics: Alkylation; Animals; Chemical Phenomena; Chemistry; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1985 |
Inhibition of mammalian dihydrofolate reductase by selected 2,4-diaminiquinazolines and related compounds.
Topics: Animals; Chagas Disease; Diamines; Enterococcus faecalis; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Liver; Malaria; Mice; Plasmodium berghei; Quinazolines; Rats; Trypanosoma cruzi | 1974 |
Comparative studies on the transport of aminopterin, methotrexate, and methasquin by the L1210 leukemia cell.
Topics: Aminopterin; Animals; Antineoplastic Agents; Ascitic Fluid; Aspartic Acid; Benzoates; Binding, Competitive; Biological Transport, Active; Cell Line; Cells, Cultured; Diffusion; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Streptococcus pneumoniae; Temperature; Tetrahydrofolate Dehydrogenase; Time Factors; Tritium | 1972 |
Potential antitumor agents. 13. Bisquaternary salts.
Topics: Aniline Compounds; Animals; Antineoplastic Agents; Hydrogen-Ion Concentration; Leukemia L1210; Methods; Mice; Quinazolines; Quinolines; Structure-Activity Relationship | 1973 |
Stereochemical characteristics of the folate-antifolate transport mechanism in L1210 Leukemia cells.
Topics: Aminopterin; Animals; Biological Transport, Active; Cells, Cultured; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Methotrexate; Mice; Pyrimidines; Quinazolines | 1974 |
Antitumor effects of the antispermatogenic agent, 2,3-dihydro-2-(1-naphthyl)-4(1H)-quinazolinone (NSC-145669).
Topics: Administration, Oral; Animals; Antineoplastic Agents; Benzene Derivatives; Carbon Isotopes; Cells, Cultured; DNA, Neoplasm; Female; Injections, Intraperitoneal; Injections, Subcutaneous; Ketones; Leukemia L1210; Leukemia, Experimental; Mice; Mice, Inbred Strains; Naphthalenes; Neoplasm Proteins; Neoplasm Transplantation; Organ Size; Quinazolines; Quinolines; RNA, Neoplasm; Time Factors | 1972 |
Quinazoline antifolates as inhibitors of dihydrofolate reductase from human leukemia cells.
Topics: Adult; Aged; Animals; Biological Transport; Cell Line; Chemical Precipitation; Chromatography; Chromatography, Gel; Deoxyuridine; DNA, Neoplasm; Female; Folic Acid Antagonists; Humans; Hydroxyapatites; Leukemia L1210; Leukemia, Lymphoid; Leukemia, Myeloid; Leukemia, Myeloid, Acute; Leukocytes; Methotrexate; Mice; Quaternary Ammonium Compounds; Quinazolines; Spectrophotometry; Sulfates; Tetrahydrofolate Dehydrogenase; Tritium; Ultraviolet Rays | 1970 |
Studies with a 2,4-diamino-5-chloro-quinazoline antifolate: in vitro and invivo correlates in normal and lymphosarcoma dogs.
Topics: Animals; Bone Marrow; Bone Marrow Cells; Deoxyuridine; DNA; DNA, Neoplasm; Dogs; Folic Acid Antagonists; Hydrogen-Ion Concentration; Injections, Intravenous; Leukemia L1210; Lymphoma, Non-Hodgkin; Methotrexate; Quinazolines; Thymine Nucleotides; Time Factors; Tritium | 1971 |
Quinazoline antifolates: biologic activities.
Topics: Animals; Cell Line; Culture Techniques; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Streptococcus | 1968 |