quinazolines has been researched along with methotrexate in 190 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 75 (39.47) | 18.7374 |
| 1990's | 56 (29.47) | 18.2507 |
| 2000's | 23 (12.11) | 29.6817 |
| 2010's | 32 (16.84) | 24.3611 |
| 2020's | 4 (2.11) | 2.80 |
| Authors | Studies |
|---|---|
| Crippen, GM; Ghose, AK | 1 |
| Hynes, JB; McCullough, JL; Weinstein, GD | 1 |
| Donsback, RC; Sirotnak, FM | 1 |
| Bertino, JR; Chello, PL; DeAngelis, LM; McQueen, CA | 1 |
| 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 |
| Ohnuma, T; Takemura, Y | 1 |
| Bartkowiak, J; Gaczyński, M; Kiliańska, Z; Krajewska, WM; Kłyszejko-Stefanowicz, L; Lipińska, A | 1 |
| Assaraf, YG; Schimke, RT; Sharma, RC | 1 |
| Miyachi, H; Ohnuma, T; Sekiguchi, S; Takemura, Y | 1 |
| Aschele, C; Bertino, JR; Nicolin, A; Rosso, R; Sobrero, A | 1 |
| Goldman, ID; Mikulecky, DC; Rape, TJ; Seither, RL; Trent, DF | 2 |
| Bertino, JR; Chang, YM; Li, WW; Lin, JT; Schweitzer, B | 1 |
| Chmurzyńska, W; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M | 1 |
| Brown, M; Calvert, AH; Gibson, W; Hughes, LR; Jackman, AL; Judson, IR; Kimbell, R; Taylor, GA | 1 |
| Duch, DS; Freisheim, JH; Hagan, RL; Hanlon, MH; Hynes, JB; Shane, B; Smith, GK | 1 |
| Bertino, JR | 1 |
| Assaraf, YG; Molina, A; Schimke, RT; Sherwood, SW | 1 |
| Jackman, AL; Jansen, G; Newell, DR; Rijksen, G; Schornagel, JH; Westerhof, GR | 1 |
| Barlowe, CK; Goldman, ID; Matherly, LH | 1 |
| Allegra, CJ; Baram, J; Drake, JC; Hoang, K; Yeh, GC | 1 |
| Cashmore, AR; Coronnello, M; Dreyer, RN; Lin, JT; Mazzei, T; McGuire, JJ; Mini, E; Moroson, BA; Periti, P; Pizzorno, G | 1 |
| Bertino, JR; McGuire, JJ; Sobrero, AF | 1 |
| Bertino, JR; Chang, YM; McGuire, JJ; Pizzorno, G | 1 |
| Assaraf, YG; Molina, A; Schimke, RT | 3 |
| Bertino, JR; Nicolin, A; Romanini, A; Rosso, R; Russello, O; Sobrero, A | 1 |
| Jansen, G; Rijksen, G; Schornagel, JH; van der Veer, LJ; Westerhof, GR | 1 |
| Bertino, JR; Chou, TC; Romanini, A | 1 |
| Arkin, H; Holland, JF; Kamen, BA; Ohnuma, T; Vallabhajosula, S | 1 |
| Cole, A; Freisheim, JH; Hagan, RL; Hynes, JB; Kohler, W; Patil, SA | 1 |
| Goldman, ID; Matherly, LH; Schuetz, JD; Westin, EH | 1 |
| Balis, FM; Lester, CM; Poplack, DG | 1 |
| Griswold, DP; Hook, KE; Leopold, WR; Nelson, JM; Roberts, BJ | 1 |
| Bertino, JR; Sobrero, AF | 1 |
| Besserer, JA; Fry, DW; Klohs, WD; Steinkampf, RW | 1 |
| Holland, JF; Kano, Y; Ohnuma, T | 1 |
| Bertino, JR; McGuire, JJ; Narayanan, R; Rodenhuis, S | 1 |
| Allegra, CJ; Chabner, BA; Drake, JC; Kovacs, JA; Masur, H; Swan, JC | 1 |
| Branda, RF; Carney, JK; McCormack, JJ; Moore, AL; Perlmutter, CA | 1 |
| Galivan, J; Nimec, Z; Rhee, M | 1 |
| Cody, V; Sutton, PA | 1 |
| Bertino, JR; McGuire, JJ; Rodenhuis, S; Sawicki, WL | 1 |
| Ackermann, MF; Germolec, DR; Lamm, KR; Luster, MI; Rosenthal, GJ | 1 |
| Blank, JA; Germolec, DR; Luster, MI; Rosenthal, GJ; Weigand, GW | 1 |
| Bertino, JR; Handschumacher, RE; Sobrero, AF | 1 |
| Borst, P; Calafat, J; Fase-Fowler, F; van Luenen, H; White, TC | 1 |
| Boiocchi, M; Broggini, M; D'Incalci, M; Erba, E; Lorico, A; Rappa, G; Toffoli, G | 2 |
| Asleson, GL; Barron, DA; Doig, MT; Hynes, JB; Priest, DG; Stratton, LP | 1 |
| Gale, GR; Hynes, JB; Smith, AB | 1 |
| Cheng, YC; Dutschman, GE; Fisher, MH; Nair, MG; Nanavathi, NT; Starnes, MC | 1 |
| Camerman, A; Camerman, N; Mastropaolo, D; Smith, HW | 1 |
| Dedhar, S; Freisheim, JH; Goldie, JH; Hynes, JB | 2 |
| Freisheim, JH; Hynes, JB; Kumar, A; Susten, SS | 1 |
| Maley, F; Maley, GF | 1 |
| Albrecht, AM; Hutchison, DJ | 1 |
| Albrecht, AM; Biedler, JL; Hutchison, DJ | 1 |
| Donsbach, RC; Sirotnak, FM | 2 |
| Hutchison, DJ; Philips, FS; Sirotnak, FM; Sodergren, JE | 1 |
| Burchall, JJ | 1 |
| Hutchison, DJ; Philips, FS; Rader, JI; Sodergren, JE; Vidal, P | 1 |
| Philips, FS; Sodergren, JE; Sternberg, SS; Vidal, P | 1 |
| Hutchison, DJ | 2 |
| Albrecht, AM; Biedler, JL; Hutchison, DJ; Spengler, BA | 1 |
| Hutchison, DJ; Rader, JI | 1 |
| Bertino, JR; Capizzi, RL; Cashmore, AR; Johns, DG; Nahas, A | 1 |
| Abboud, G; Bertino, JR; Fölsch, E; Gralla, E | 1 |
| Hutchison, DJ; Schmid, FA; Shimoyama, M | 1 |
| Cheng, CC; Roth, B | 1 |
| Diddens, H; Jackson, RC; Niethammer, D | 2 |
| Elslager, E; Lathan, B; Von Hoff, DD | 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 |
| Marsh, JC | 1 |
| Bertino, JR; Cashmore, AR; Chang, PK; Mini, E; Moroson, BA; Schornagel, JH; Sciarini, LJ | 1 |
| Calvert, AH; Jackman, AL; Jackson, RC | 1 |
| Bertino, JR; Cardenas, RM; Fernandes, DJ; Hynes, JB | 1 |
| Harmon, SJ; Hynes, JB; McGill, JE; Washtien, WL; Yang, YC | 1 |
| Bertino, JR; Fernandes, DJ; Hynes, JB | 1 |
| Fudenberg, HH; Hynes, JB; Tsang, KY | 1 |
| Holland, JF; Kamen, BA; Ohnoshi, T; Ohnuma, T; Scanlon, K; Takahashi, I | 1 |
| McCormack, JJ | 1 |
| Calvert, AH; Dady, PJ; Grzelakowska-Sztabert, B; Harrap, KR; Jones, TR; Paine, RM; Taylor, GA | 1 |
| Chen, G; Rosowsky, A; Wright, JE | 1 |
| Boyle, FT; Brown, M; Brunton, L; Jackman, AL; Kimbell, R | 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 |
| Boyle, FT; Brown, M; Brunton, L; Harrap, KR; Jackman, AL; Kimbell, R; Wardleworth, JM | 1 |
| Banks, SD; Barrett, LL; Dickerson, S; Pendergast, W; Smith, GK; Waters, KA | 1 |
| Lehman, NL; Moran, RG; Smith, SG | 1 |
| Haile, WH; Heitzman, KJ; McCloskey, DE; McGuire, JJ; Piper, JR; Russell, CA | 1 |
| Fetzer, OS; Freisheim, JH; Hynes, JB; Shane, B | 1 |
| Jansen, G; Pinedo, HM; Rijnboutt, S; 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 |
| Ando, K; Ando, Y; Kobayashi, H; Miyachi, H; Takemura, Y | 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 |
| Ando, Y; Kobayashi, H; Miyachi, H; Takemura, Y | 1 |
| DeGoeij, K; Mester, J; Sluyser, 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 |
| Beverley, SM; Hardy, LW; Matthews, W; Nare, B | 1 |
| Kamen, B | 1 |
| Kobayashi, H; Ohnuma, T; Takemura, Y | 1 |
| Kinsella, AR; Smith, D | 1 |
| Kobayashi, H; Miyachi, H; Takemura, Y | 1 |
| Andis, SL; Bewley, JR; Chen, VJ; Iversen, PW; Mendelsohn, LG; Schultz, RM; Seitz, DE; Shih, C; Tonkinson, JL | 2 |
| Loney, TL; Maybaum, J; Parsels, JD; Parsels, LA; Radany, EH; Wagner, LM | 1 |
| Aherne, GW; Boyle, FT; Brunton, L; Jackman, AL; Jansen, G; Kimbell, R; Smith, MN; Stephens, TC; Wardleworth, JM | 1 |
| 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 |
| Canestrari, JG; McGuire, JJ; Nagel, GS | 1 |
| Newell, DR | 1 |
| Bavetsias, V; Boyle, FT; Jackman, AL; Kimbell, R; Marriott, JH; Matusiak, ZS; Melin, C | 1 |
| Strømhaug, A; Warren, DJ | 1 |
| Assaraf, YG; Drori, S; Jansen, G; Mauritz, R; Peters, GJ | 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 |
| Cetkovic-Cvrlje, M; Liu, XP; Roers, BA; Uckun, FM; Waurzyniak, B | 1 |
| Belpomme, D; Clendeninn, N; Domenge, C; Humblet, Y; Johnston, A; Kelly, C; Penning, C; Pivot, X; Ruxer, R; Schneider, M; Stern, J; Tortochaux, J; Wadler, S | 1 |
| 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 |
| Griffiths, TR; Kriajevska, M; McHugh, LA; Mellon, JK; Symonds, RP | 1 |
| Banerjee, D; Bertino, JR; Li, WW; Magro, PG; Russo, AJ | 1 |
| Cetkovic-Cvrlje, M; Uckun, FM | 1 |
| Avery, MA; Carvalho, P; Gibellini, F; Hunter, WN; McLuskey, K | 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 |
| Ambudkar, SV; Ashby, CR; Bates, SE; Chen, ZS; Fu, LW; Kim, IW; Peng, XX; Robey, RW; Shen, T; Shi, Z; Shukla, S; Si, QS | 1 |
| De Mattia, E; Toffoli, G | 1 |
| Armour, A; Cohen, EE; Garin, AM; Ghiorghiu, S; Hargreaves, L; Hirsch, FR; Khorprasert, C; Licitra, L; Rischin, D; Soulieres, D; Speake, G; Stewart, JS; Swaisland, A; Van Herpen, CM; Varella-Garcia, M; Vodvarka, P; Vokes, EE | 1 |
| Teng, KY; Xu, RH | 1 |
| Amano, O; Chu, Q; Kanda, Y; Kunii, S; Sakagami, H; Wang, Q | 1 |
| Botchkina, G; Formentini, A; Ju, J; Kornmann, M; Song, B; Titmus, MA; Wang, Y | 1 |
| DeRyckere, D; Gore, L; Macy, ME | 1 |
| Guzi, TJ; Parry, D; Pierce, RH; Shanahan, F; Taricani, L | 1 |
| Banerjee, D; Bertino, JR; Blasberg, RG; Cai, S; de Stanchina, E; Kochetkov, T; Moroz, MA; Nair, J; Schwartz, GK; Serganova, I; Shamis, M; Wu, J | 1 |
| Ait-Tihyaty, M; Jean-Claude, BJ; Mihalcioiu, C; Rachid, Z | 1 |
| Kim, JJ | 1 |
| Nagpal, S; Riess, J; Wakelee, H | 1 |
| Burstein, HJ; Chen, WY; Downing, SR; Gelman, R; Hannagan, K; Isakoff, SJ; Klement, G; Mayer, EL; Winer, EP | 1 |
| Guo, Y; Li, C; Liu, JY; Tian, C; Wang, XW; Zhang, ZL | 1 |
| Gwak, HS; Han, JY; Joo, J; Kim, HT; Kim, S; Lee, JS; Lee, SH; Shin, SH; Yoo, H | 1 |
| Assaraf, YG; Dijkmans, BA; Gerards, AH; Jansen, G; Lems, WF; Oerlemans, R; Scheper, RJ; van der Heijden, JW | 1 |
| Autry, AM | 1 |
| Dimitriadis, E; Gao, Y; Greenall, SA; Horne, AW; Johns, TG; Kaitu'u-Lino, T; Menkhorst, E; Nilsson, UW; Saglam, B; Tong, S; Whitehead, C; Wilmann, T | 1 |
| Critchley, HOD; Duncan, WC; Horne, AW; Johns, TG; Nilsson, UW; Skubisz, MM; Tong, S; Wallace, EM | 1 |
| Duncan, WC; Horne, AW; Johns, TG; Neil, P; Skubisz, MM; Tong, S; Wallace, EM | 1 |
| Cohen, EE; Haddad, RI; Licitra, LF; Machiels, JP; Tahara, M | 1 |
| Horne, AW; Skubisz, MM; Tong, S | 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 |
| Ghatak, A; Gupta, S; Husain, N; Jamal, N; Khan, H; Kushwaha, VS; Negi, MP | 1 |
| Argiris, A | 1 |
| Caponigro, F; Clement, PM; Cohen, EE; Cong, XJ; Cupissol, D; de Castro, G; de Souza Viana, L; Del Campo, JM; Ehrnrooth, E; Fayette, J; Gauler, T; Grau, JJ; Guigay, J; Haddad, RI; Keilholz, U; Licitra, LF; Machiels, JP; Tahara, M; Vermorken, JB | 2 |
| Killock, D | 1 |
| Bourhis, J; Economopoulou, P; Psyrri, A | 1 |
| Chernobrovkin, A; Marin-Vicente, C; Visa, N; Zubarev, RA | 1 |
| Specenier, P; Vermorken, J | 1 |
| Kanamitsu, K; Kusuhara, H; Schuetz, JD; Sugiyama, Y; Takeuchi, K | 1 |
| Amrouche, K; Jamin, C | 1 |
| Burtness, B; Clement, PM; Cohen, EEW; Cong, XJ; Del Campo, JM; Dupuis, N; Ehrnrooth, E; Fayette, J; Gauler, T; Geoffrois, L; Gibson, N; Grau, JJ; Guigay, J; Haddad, RI; Krämer, N; Licitra, LF; Machiels, JH; Mailliez, A; Merlano, MC; Solca, F; Tahara, M; Vermorken, JB | 1 |
| Brownfoot, F; Campbell, L; Ellett, L; Hannan, NJ; Hastie, R; Horne, AW; Kaitu'u-Lino, TJ; Lim, E; Sluka, P; Tong, S | 1 |
| Bhattacharya, S; Colin Duncan, W; Doust, A; Horne, AW; Johns, TG; Krzys, N; Mollison, J; Neil, P; Robinson, M; Skubisz, MM; Tong, S; Wallace, E | 1 |
| Clement, PM; Cohen, EEW; Cupissol, D; de Souza Viana, L; Fayette, J; Gauler, T; Geng, Y; Geoffrois, L; Guigay, J; Haddad, R; Keilholz, U; Kornek, G; Licitra, L; Machiels, JP; Melichar, B; Rauch, D; Ribaldo Nicolau, U; Rolland, F; Tahara, M; Vermorken, J; Zanetta-Devauges, S; Zografos, E | 1 |
| El-Subbagh, HI; Sabry, MA | 1 |
| Chen, G; Maiti, S; MaitiDutta, S | 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 |
16 review(s) available for quinazolines and methotrexate
| Article | Year |
|---|---|
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 |
Recent progress in the medicinal chemistry of 2,4-diaminopyrimidines.
Topics: Amino Acid Sequence; Animals; Folic Acid Antagonists; Glutamates; Glutamic Acid; Malaria; Mathematics; Methotrexate; Microbial Sensitivity Tests; Models, Chemical; Pyrimethamine; Pyrimidines; Quinazolines; Stereoisomerism; Triazines | 1982 |
Dihydrofolate reductase inhibitors as potential drugs.
Topics: Aminopterin; Animals; Antimalarials; Bacterial Infections; Biological Transport; Drug Interactions; Folic Acid; Folic Acid Antagonists; Helminthiasis; Humans; Immunosuppressive Agents; Leukemia, Experimental; Liver; Methotrexate; Mice; Mycoses; Neoplasms; Protozoan Infections; Psoriasis; Quinazolines; Rats; Receptors, Drug; Trypanosoma cruzi | 1981 |
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 |
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 |
Tyrosine kinase inhibitors of the epidermal growth factor receptor as adjuncts to systemic chemotherapy for muscle-invasive bladder cancer.
Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Chemotherapy, Adjuvant; Cisplatin; Combined Modality Therapy; Doxorubicin; Enzyme Inhibitors; ErbB Receptors; Gefitinib; Genes, erbB-1; Humans; Methotrexate; Muscle Neoplasms; Neoadjuvant Therapy; Oncogene Proteins v-erbB; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-akt; Quinazolines; Receptor Protein-Tyrosine Kinases; Receptor, ErbB-2; Urinary Bladder Neoplasms; Vinblastine | 2004 |
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 |
[Progress in chemotherapy for advanced gastric cancer].
Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Camptothecin; Capecitabine; Cisplatin; Clinical Trials, Phase III as Topic; Deoxycytidine; Docetaxel; Doxorubicin; Drug Combinations; Fluorouracil; Gefitinib; Humans; Irinotecan; Methotrexate; Neoadjuvant Therapy; Neoplasm Staging; Organoplatinum Compounds; Oxaliplatin; Oxonic Acid; Paclitaxel; Quinazolines; Stomach Neoplasms; Survival Rate; Taxoids; Tegafur; Trastuzumab | 2009 |
Recent advances in treatment of advanced urothelial carcinoma.
Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Cancer Vaccines; Carcinoma, Transitional Cell; Cetuximab; Cisplatin; Doxorubicin; Female; Gefitinib; Humans; Immunotherapy; Male; Methotrexate; Molecular Targeted Therapy; Neoplasm Invasiveness; Neoplasm Staging; Prognosis; Quality Improvement; Quinazolines; Risk Assessment; Survival Analysis; Treatment Outcome; Urinary Bladder Neoplasms; Vinblastine | 2012 |
Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.
Topics: Afatinib; Antineoplastic Agents; Carcinoma, Squamous Cell; Early Detection of Cancer; Head and Neck Neoplasms; Humans; Immunotherapy; Meta-Analysis as Topic; Methotrexate; Molecular Diagnostic Techniques; Molecular Targeted Therapy; Multicenter Studies as Topic; Neoplasm Metastasis; Neoplasm Recurrence, Local; Neoplasm Staging; Oropharyngeal Neoplasms; Papillomavirus Vaccines; Postoperative Care; Precision Medicine; Quinazolines; Radiotherapy, Adjuvant; Randomized Controlled Trials as Topic; Squamous Cell Carcinoma of Head and Neck; Therapies, Investigational | 2015 |
Afatinib in squamous cell carcinoma of the head and neck.
Topics: Afatinib; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Cetuximab; Chemoradiotherapy; Disease-Free Survival; Head and Neck Neoplasms; Humans; Maximum Tolerated Dose; Methotrexate; Neoplasm Recurrence, Local; Quinazolines; Squamous Cell Carcinoma of Head and Neck; Treatment Outcome | 2016 |
Influence of drug molecules on regulatory B cells.
Topics: Adrenal Cortex Hormones; Animals; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; B-Cell Activating Factor; B-Lymphocytes, Regulatory; CD40 Antigens; Cytokines; Humans; Immunosuppressive Agents; Methotrexate; Mycophenolic Acid; Pyrroles; Quinazolines; Receptors, Antigen, B-Cell; Semaphorins; Sirolimus; Toll-Like Receptors; Tretinoin; Vitamin D; Vitamins | 2017 |
2-Substituted-mercapto-quinazolin-4(3H)-ones as DHFR Inhibitors.
Topics: Folic Acid Antagonists; Methotrexate; Quinazolines; Tetrahydrofolate Dehydrogenase | 2021 |
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 |
13 trial(s) available for quinazolines and methotrexate
| Article | Year |
|---|---|
Folate antagonists: toward improving the therapeutic index and development of new analogs.
Topics: Cell Line; Chemical Phenomena; Chemistry; Clinical Trials as Topic; Drug Resistance; Folic Acid Antagonists; Gene Amplification; Humans; Methotrexate; Mutation; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate | 1990 |
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 |
Result of two randomized trials comparing nolatrexed (Thymitaq) versus methotrexate in patients with recurrent head and neck cancer.
Topics: Adult; Aged; Aged, 80 and over; Antimetabolites, Antineoplastic; Carcinoma, Squamous Cell; Diarrhea; Enzyme Inhibitors; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Middle Aged; Neoplasm Recurrence, Local; Neutropenia; Quinazolines; Thymidylate Synthase; Treatment Outcome | 2001 |
Phase III study of gefitinib compared with intravenous methotrexate for recurrent squamous cell carcinoma of the head and neck [corrected].
Topics: Administration, Oral; Aged; Antineoplastic Agents; Carcinoma, Squamous Cell; Female; Gefitinib; Head and Neck Neoplasms; Humans; Infusions, Intravenous; Male; Methotrexate; Middle Aged; Neoplasm Recurrence, Local; Quality of Life; Quinazolines; Survival Analysis; Treatment Outcome | 2009 |
Combination antiangiogenic therapy in advanced breast cancer: a phase 1 trial of vandetanib, a VEGFR inhibitor, and metronomic chemotherapy, with correlative platelet proteomics.
Topics: Administration, Metronomic; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Biomarkers, Pharmacological; Blood Platelets; Breast Neoplasms; Combined Modality Therapy; Cyclophosphamide; Drug-Related Side Effects and Adverse Reactions; Female; Gene Expression Regulation, Neoplastic; Humans; Methotrexate; Middle Aged; Neoplasm Staging; Neovascularization, Pathologic; Piperidines; Platelet Factor 4; Proteomics; Quinazolines; Vascular Endothelial Growth Factor A; Vascular Endothelial Growth Factor Receptor-1 | 2012 |
Combination gefitinib and methotrexate compared with methotrexate alone to treat ectopic pregnancy.
Topics: Abortifacient Agents, Nonsteroidal; Adult; Antineoplastic Agents; Drug Therapy, Combination; Female; Gefitinib; Humans; Injections, Intramuscular; Methotrexate; Pregnancy; Pregnancy, Ectopic; Quinazolines | 2013 |
Rationale and design of LUX-Head & Neck 1: a randomised, Phase III trial of afatinib versus methotrexate in patients with recurrent and/or metastatic head and neck squamous cell carcinoma who progressed after platinum-based therapy.
Topics: Afatinib; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Clinical Protocols; Disease Progression; Head and Neck Neoplasms; Humans; Methotrexate; Neoplasm Metastasis; Neoplasm Recurrence, Local; Platinum; Quinazolines; Retreatment; Squamous Cell Carcinoma of Head and Neck | 2014 |
Gefitinib, Methotrexate and Methotrexate plus 5-Fluorouracil as palliative treatment in recurrent head and neck squamous cell carcinoma.
Topics: Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Female; Fluorouracil; Gefitinib; Head and Neck Neoplasms; Humans; Male; Methotrexate; Middle Aged; Neoplasm Recurrence, Local; Palliative Care; Quality of Life; Quinazolines; Squamous Cell Carcinoma of Head and Neck; Treatment Outcome | 2015 |
Afatinib versus methotrexate as second-line treatment in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 1): an open-label, randomised phase 3 trial.
Topics: Adult; Afatinib; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Disease-Free Survival; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Middle Aged; Neoplasm Metastasis; Neoplasm Recurrence, Local; Platinum; Quinazolines; Squamous Cell Carcinoma of Head and Neck; Treatment Outcome | 2015 |
Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.
Topics: Afatinib; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Disease-Free Survival; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Neoplasm Metastasis; Neoplasm Recurrence, Local; Platinum; Quinazolines; Squamous Cell Carcinoma of Head and Neck; Treatment Outcome | 2016 |
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.
Topics: Administration, Intravenous; Administration, Oral; Afatinib; Antimetabolites, Antineoplastic; Biomarkers, Tumor; Biopsy; Carcinoma, Squamous Cell; Disease-Free Survival; Head and Neck Neoplasms; Humans; Methotrexate; Neoplasm Metastasis; Neoplasm Recurrence, Local; Predictive Value of Tests; Quinazolines; Squamous Cell Carcinoma of Head and Neck | 2017 |
Gefitinib and Methotrexate to Treat Ectopic Pregnancies with a Pre-Treatment Serum hCG 1000-10,000 IU/L: Phase II Open Label, Single Arm Multi-Centre Trial.
Topics: Administration, Intranasal; Administration, Oral; Adult; Chorionic Gonadotropin; Drug Therapy, Combination; Female; Gefitinib; Humans; Methotrexate; Pregnancy; Pregnancy, Ectopic; Quinazolines; Treatment Outcome | 2018 |
Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.
Topics: Afatinib; Aged; Antineoplastic Combined Chemotherapy Protocols; Disease-Free Survival; ErbB Receptors; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Neoplasm Recurrence, Local; Quinazolines; Squamous Cell Carcinoma of Head and Neck; Treatment Adherence and Compliance; Treatment Outcome | 2019 |
161 other study(ies) available for quinazolines and methotrexate
| Article | Year |
|---|---|
General distance geometry three-dimensional receptor model for diverse dihydrofolate reductase inhibitors.
Topics: Animals; Binding Sites; Chemical Phenomena; Chemistry, Physical; Crystallography; Folic Acid Antagonists; Liver; Models, Chemical; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Rats; Structure-Activity Relationship; Triazines | 1984 |
In vitro screening of biochemical activity of folic acid antagonists in skin.
Topics: Animals; Animals, Newborn; Chlorobenzenes; Depression, Chemical; DNA; Folic Acid Antagonists; Methotrexate; Psoriasis; Pyrimethamine; Pyrimidines; Quinazolines; Rats; Skin; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim | 1977 |
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 |
Elevation of dihydrofolate reductase, thymidylate synthetase, and thymidine kinase in cultured mammalian cells after exposure to folate antagonists.
Topics: Aspartic Acid; Cells, Cultured; Dose-Response Relationship, Drug; Folic Acid Antagonists; Kinetics; Leukocytes; Methotrexate; Methyltransferases; Quinazolines; Temperature; Tetrahydrofolate Dehydrogenase; Thymidine Kinase; Thymidylate Synthase; Triazines | 1976 |
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 |
N10-propargyl-5,8-dideazafolic acid (CB3717): inhibitory effects on human leukemia cell lines resistant to methotrexate or trimetrexate.
Topics: Antineoplastic Agents; Cell Division; Cell Line; Cell Survival; Dose-Response Relationship, Drug; Drug Resistance; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines; Thymidylate Synthase; Trimetrexate; Tumor Cells, Cultured | 1992 |
Nuclear proteins of hamster hepatoma after administration of antitumour agents.
Topics: Animals; Antimetabolites, Antineoplastic; Cricetinae; Depression, Chemical; Electrophoresis, Gel, Two-Dimensional; Electrophoresis, Polyacrylamide Gel; Gene Expression Regulation, Neoplastic; Liver Neoplasms, Experimental; Male; Mesocricetus; Methotrexate; Molecular Weight; Neoplasm Proteins; Neoplasms, Hormone-Dependent; Nuclear Proteins; Quinazolines; Testosterone | 1992 |
A phenotype conferring selective resistance to lipophilic antifolates in Chinese hamster ovary cells.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Binding, Competitive; Cell Line; Cricetinae; Drug Resistance; Folic Acid Antagonists; Gene Amplification; Membrane Glycoproteins; Methotrexate; Phenotype; Pyrimidines; Quinazolines; RNA, Messenger; Tetrahydrofolate Dehydrogenase; Trimetrexate; Verapamil | 1991 |
A human leukemia cell line made resistant to two folate analogues, trimetrexate and N10-propargyl-5,8-dideazafolic acid (CB3717).
Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cell Division; Cell Line; Cisplatin; Cross Reactions; Dactinomycin; Dose-Response Relationship, Drug; Doxorubicin; Drug Resistance; Etoposide; Fluorouracil; Folic Acid; Humans; Leucovorin; Membrane Glycoproteins; Methotrexate; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines; RNA, Messenger; Thymidylate Synthase; Trimetrexate; Vincristine | 1991 |
Rapid development of resistance to antifolates in vitro: possible clinical implication.
Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Colonic Neoplasms; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug Resistance; Female; Folic Acid Antagonists; Leukemia P388; Methotrexate; Mice; Quinazolines; Trimetrexate; 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 |
Prediction of antifolate efficacy in a rat sarcoma model.
Topics: Aminopterin; Animals; Drug Screening Assays, Antitumor; Folic Acid Antagonists; Male; Methotrexate; Methylcholanthrene; Quinazolines; Rats; Sarcoma, Experimental; Thymidylate Synthase; Trimetrexate | 1991 |
Ornithine decarboxylase induction in mouse kidney as indicator of renal damage. Differential nephrotoxic effect of anticancer antifolate drugs.
Topics: Animals; Antimetabolites, Antineoplastic; Biomarkers; Enzyme Induction; Female; Folic Acid; Folic Acid Antagonists; Indomethacin; Kidney; Kidney Diseases; Methotrexate; Mice; Organ Size; Ornithine Decarboxylase; Quinazolines | 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 |
Studies on the mechanism of antitumor action of 2-desamino-2-methyl-5,8-dideazaisofolic acid.
Topics: Animals; Antineoplastic Agents; Carrier Proteins; Drug Screening Assays, Antitumor; Folate Receptors, GPI-Anchored; Folic Acid Antagonists; Kinetics; Methotrexate; Peptide Synthases; Quinazolines; Receptors, Cell Surface; Thymidylate Synthase; Tumor Cells, Cultured | 1991 |
Flow cytometric characterization of antifolate resistance in cultured mammalian cells using fluoresceinated methotrexate and daunorubicin.
Topics: Animals; Cell Line; Colchicine; Cricetinae; Cricetulus; Daunorubicin; Drug Resistance; Female; Flow Cytometry; Folic Acid Antagonists; Kinetics; Methotrexate; Ovary; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate; Verapamil | 1990 |
Multiple membrane transport systems for the uptake of folate-based thymidylate synthase inhibitors.
Topics: Antineoplastic Agents; Biological Transport; Cell Division; Cells, Cultured; Drug Carriers; Folic Acid; Folic Acid Antagonists; Humans; In Vitro Techniques; Leukemia; Methotrexate; Quinazolines; Thymidylate Synthase | 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 |
Evidence for direct inhibition of de novo purine synthesis in human MCF-7 breast cells as a principal mode of metabolic inhibition by methotrexate.
Topics: Acyltransferases; Antineoplastic Agents; Breast Neoplasms; Carbon Radioisotopes; Cell Line; Female; Floxuridine; Folic Acid; Glycine; Humans; Hydroxymethyl and Formyl Transferases; Kinetics; Methotrexate; Phosphoribosylaminoimidazolecarboxamide Formyltransferase; Polyglutamic Acid; Purines; Quinazolines; Trimetrexate | 1987 |
Impaired polyglutamylation of methotrexate as a cause of resistance in CCRF-CEM cells after short-term, high-dose treatment with this drug.
Topics: Drug Resistance; Humans; Methotrexate; Peptides; Polyglutamic Acid; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate; Tumor Cells, Cultured | 1988 |
Uptake and metabolism of 5,8-dideazaisofolic acid in human colon carcinoma cells.
Topics: Adenocarcinoma; Biotransformation; Colonic Neoplasms; Folic Acid Antagonists; Humans; Methotrexate; Polyglutamic Acid; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1988 |
Inherent resistance of human squamous carcinoma cell lines to methotrexate as a result of decreased polyglutamylation of this drug.
Topics: Antineoplastic Agents; Carcinoma, Squamous Cell; Drug Resistance; Head and Neck Neoplasms; Humans; Methotrexate; Peptide Synthases; Peptides; Polyglutamic Acid; Quinazolines; Thymidylate Synthase; Time Factors; Trimetrexate; Tumor Cells, Cultured | 1989 |
Cross-resistance to the lipid-soluble antifolate trimetrexate in human carcinoma cells with the multidrug-resistant phenotype.
Topics: Animals; Antineoplastic Agents; Breast Neoplasms; Carcinoma; Cell Line; Drug Resistance; Female; Genes; Humans; Methotrexate; Ovarian Neoplasms; Phenotype; Quinazolines; Quinidine; RNA, Messenger; Trimetrexate; Tumor Cells, Cultured; Verapamil | 1989 |
A fluorescein-methotrexate-based flow cytometric bioassay for measurement of plasma methotrexate and trimetrexate levels.
Topics: Flow Cytometry; Fluorescein; Fluoresceins; Humans; Indicators and Reagents; Methotrexate; Quinazolines; Trimetrexate | 1989 |
Sequence-dependent enhancement of HCT-8 cell kill by trimetrexate and fluoropyrimidines: implications for the mechanism of this interaction.
Topics: Adenocarcinoma; Antineoplastic Combined Chemotherapy Protocols; Colonic Neoplasms; Colony-Forming Units Assay; Drug Interactions; Drug Synergism; Floxuridine; Fluorouracil; Folic Acid Antagonists; Humans; Methotrexate; Quinazolines; Trimetrexate; Tumor Cells, Cultured; 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 |
Cytotoxicity of methotrexate and trimetrexate and its reversal by folinic acid in human leukemic CCRF-CEM cells with carrier-mediated and receptor-mediated folate uptake.
Topics: Biological Transport; Carrier Proteins; Folate Receptors, GPI-Anchored; Folic Acid; Humans; In Vitro Techniques; Leucovorin; Leukemia; Methotrexate; Quinazolines; Receptors, Cell Surface; Trimetrexate; Tumor Cells, Cultured | 1989 |
Carboxypeptidase G2 enhances trimetrexate cytotoxicity in CCRF-CEM cell lines sensitive and resistant to methotrexate.
Topics: Antineoplastic Agents; Cell Line; Cell Survival; Clone Cells; Cysteine Endopeptidases; Drug Resistance; Drug Synergism; gamma-Glutamyl Hydrolase; Humans; Methotrexate; Quinazolines; Trimetrexate; Tumor Cells, Cultured | 1989 |
Sequential amplification of dihydrofolate reductase and multidrug resistance genes in Chinese hamster ovary cells selected for stepwise resistance to the lipid-soluble antifolate trimetrexate.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cell Line; Cricetinae; Drug Resistance; Fluorescein; Fluoresceins; Folic Acid Antagonists; Gene Amplification; Gene Expression; Membrane Glycoproteins; Methotrexate; Pyrimidines; Quinazolines; RNA, Messenger; Tetrahydrofolate Dehydrogenase; Trimetrexate | 1989 |
Multidrug resistance in a human leukemic cell line selected for resistance to trimetrexate.
Topics: ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Doxorubicin; Drug Resistance; Humans; In Vitro Techniques; Leukemia; Membrane Glycoproteins; Methotrexate; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate; Tumor Cells, Cultured; Verapamil; Vincristine | 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 |
Pharmacokinetics of trimetrexate (NSC 352122) in monkeys.
Topics: Animals; Folic Acid Antagonists; Macaca mulatta; Male; Metabolic Clearance Rate; Methotrexate; Protein Binding; Quinazolines; Trimetrexate | 1986 |
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 |
Endogenous thymidine and hypoxanthine are a source of error in evaluating methotrexate cytotoxicity by clonogenic assays using undialyzed fetal bovine serum.
Topics: Adenocarcinoma; Animals; Cattle; Cell Adhesion; Colonic Neoplasms; Colony-Forming Units Assay; Culture Media; Dose-Response Relationship, Drug; Humans; Hypoxanthines; Leucovorin; Methotrexate; Neoplastic Stem Cells; Quinazolines; Thymidine; Trimetrexate | 1986 |
Cross resistance of pleiotropically drug resistant P338 leukemia cells to the lipophilic antifolates trimetrexate and BW 301U.
Topics: Animals; Drug Resistance; Folic Acid Antagonists; Leukemia P388; Methotrexate; Mice; Pyrimidines; Quinazolines; Trimetrexate | 1986 |
Folate requirements of methotrexate-resistant human acute lymphoblastic leukemia cell lines.
Topics: Biological Transport; Cell Line; Drug Resistance; Folic Acid; Humans; Leukemia, Experimental; Leukemia, Lymphoid; Methotrexate; Nutritional Requirements; Quinazolines; Trimetrexate | 1986 |
Development of an assay system for the detection and classification of methotrexate resistance in fresh human leukemic cells.
Topics: Adolescent; Adult; Aged; Cell Line; Deoxyuridine; DNA, Neoplasm; Drug Resistance; Female; Humans; Leukemia; Male; Methotrexate; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate; Tritium | 1986 |
Activity of antifolates against Pneumocystis carinii dihydrofolate reductase and identification of a potent new agent.
Topics: Biological Transport; Folic Acid Antagonists; Kinetics; Methotrexate; NADP; Pneumocystis; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate | 1987 |
Inhibition of lymphocyte nucleic acid metabolism and antibody production by trimetrexate.
Topics: Antibody Formation; Deoxyuridine; DNA; Humans; Interphase; Lymphocytes; Methotrexate; Nucleic Acids; Quinazolines; Thymidine; Trimetrexate | 1987 |
Synergistic growth inhibition of rat hepatoma cells exposed in vitro to N10-propargyl-5,8-dideazafolate with methotrexate or the lipophilic antifolates trimetrexate or metoprine.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Cell Cycle; Deoxyuridine; Folic Acid; Folic Acid Antagonists; Liver Neoplasms, Experimental; Methotrexate; Pyrimethamine; Quinazolines; Rats; Thymidine; Thymidylate Synthase; Trimetrexate | 1987 |
Conformational analysis of antineoplastic antifolates: the crystal structure of trimetrexate and the aminopterine derivative 4-[N-[(2,4-diamino-6-pteridinyl)methyl]amino]benzoic acid.
Topics: Antineoplastic Agents; Crystallization; Folic Acid Antagonists; Methotrexate; Models, Molecular; Quinazolines; Trimetrexate; X-Ray Diffraction | 1987 |
Effects of methotrexate and of the "nonclassical" folate antagonist trimetrexate on human leukemia cells.
Topics: Adenocarcinoma; Colonic Neoplasms; DNA Replication; DNA, Neoplasm; Dose-Response Relationship, Drug; Humans; Leukemia; Methotrexate; Quinazolines; Trimetrexate; Tumor Cells, Cultured | 1987 |
Comparative effects on the immune system of methotrexate and trimetrexate.
Topics: Animals; Antibody Formation; Antibody-Producing Cells; Antineoplastic Agents; Cytotoxicity, Immunologic; Dose-Response Relationship, Drug; Female; Folic Acid Antagonists; Immunity; Killer Cells, Natural; Lymphocyte Activation; Methotrexate; Mice; Mice, Inbred Strains; Quinazolines; Trimetrexate | 1987 |
Suppression of B cell function by methotrexate and trimetrexate. Evidence for inhibition of purine biosynthesis as a major mechanism of action.
Topics: Animals; Antibody Formation; B-Lymphocytes; Cell Differentiation; Female; Folic Acid Antagonists; Immunoglobulins; Immunosuppressive Agents; Kinetics; Lymphocyte Activation; Methotrexate; Mice; Purines; Quinazolines; Trimetrexate | 1988 |
Highly selective drug combinations for human colon cancer cells resistant in vitro to 5-fluoro-2'-deoxyuridine.
Topics: Adenocarcinoma; Antineoplastic Combined Chemotherapy Protocols; Biological Transport; Cell Line; Colonic Neoplasms; Drug Resistance; Floxuridine; Humans; Hypoxanthine; Hypoxanthines; Methotrexate; Nucleosides; Quinazolines; Thymidine | 1985 |
The H circles of Leishmania tarentolae are a unique amplifiable system of oligomeric DNAs associated with drug resistance.
Topics: Animals; Cloning, Molecular; DNA; DNA, Circular; Drug Resistance; Folic Acid; Leishmania; Methotrexate; Microscopy, Electron; Quinazolines; Thymidylate Synthase | 1988 |
Accumulation of DNA strand breaks in cells exposed to methotrexate or N10-propargyl-5,8-dideazafolic acid.
Topics: Cell Cycle; Cell Survival; Cycloheximide; DNA; DNA Damage; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Proteins; Quinazolines; Thymidine | 1988 |
Early DNA damage induced in cells exposed to N10-propargyl 5,8-dideazafolic acid (CB 3717) or methotrexate.
Topics: Animals; Cell Division; Cell Line; Cell Survival; DNA; DNA Damage; Folic Acid; Methotrexate; Mice; Quinazolines; Thymidylate Synthase | 1988 |
Micellar high-performance liquid chromatographic determination of folylpolyglutamate hydrolase activity.
Topics: Animals; Chromatography, High Pressure Liquid; Kidney; Methotrexate; Mice; Mice, Inbred CBA; Micelles; Peptide Synthases; Quinazolines; Sodium Dodecyl Sulfate; Substrate Specificity | 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 |
Crystal structure of quinespar, a quinazoline analogue of methotrexate.
Topics: Folic Acid; Folic Acid Antagonists; Methotrexate; Molecular Conformation; Quinazolines; Tetrahydrofolate Dehydrogenase; X-Ray Diffraction | 1986 |
Further studies on substituted quinazolines and triazines as inhibitors of a methotrexate-insensitive murine dihydrofolate reductase.
Topics: Animals; Cell Line; Chemical Phenomena; Chemistry; Leukemia L5178; Methotrexate; Mice; Quinazolines; Tetrahydrofolate Dehydrogenase; Triazines | 1986 |
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 |
The apparent induction of thymidylate synthetase by amethopterin.
Topics: Animals; Aspartic Acid; Benzoates; Carcinoma, Hepatocellular; Enzyme Induction; Folic Acid; Hepatectomy; Liver; Liver Neoplasms; Liver Regeneration; Methotrexate; Methyltransferases; Neoplasms, Experimental; Quinazolines; Rats; Thymine Nucleotides; Uracil Nucleotides | 1971 |
Folate reductase of the amethopterin-resistant Streptococcus faecium var. durans-Ak. I. Inhibition by amethopterin and methasquin, a new quinazoline antifolate.
Topics: Aspartic Acid; Chromatography, DEAE-Cellulose; Electrophoresis; Folic Acid Antagonists; Hydrogen-Ion Concentration; Kinetics; Methotrexate; Molecular Weight; NADP; Potassium Chloride; Quinazolines; Streptococcus; Tetrahydrofolate Dehydrogenase | 1970 |
Two different species of dihydrofolate reductase in mammalian cells differentially resistant to amethopterin and methasquin.
Topics: Animals; Cell Line; Cricetinae; Drug Resistance; Folic Acid Antagonists; Hydrogen-Ion Concentration; In Vitro Techniques; Isoenzymes; Kinetics; Methotrexate; Molecular Weight; Mutagens; NADP; Quinazolines; Tetrahydrofolate Dehydrogenase | 1972 |
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 |
Uptake of methotrexate, aminopterin, and methasquin and inhibition of dihydrofolate reductase and of DNA synthesis in mouse small intestine.
Topics: Aminopterin; Animals; Deoxyuridine; DNA; Dose-Response Relationship, Drug; Folic Acid Antagonists; Injections, Intravenous; Intestinal Mucosa; Intestine, Small; Male; Methotrexate; Methylation; Mice; Quinazolines | 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 |
Comparative biochemistry of dihydrofolate reductase.
Topics: Animals; Anura; Biochemical Phenomena; Biochemistry; Escherichia coli; Fishes; Folic Acid Antagonists; Humans; Hydrogen-Ion Concentration; Kinetics; Liver; Malaria; Methotrexate; Nephropidae; Proteus vulgaris; Pyridines; Pyrimidines; Quinazolines; Rana pipiens; Rats; Staphylococcus; Taenia; Tetrahydrofolate Dehydrogenase; Triazines; Trimethoprim; Turtles | 1971 |
Urinary and biliary excretion of the 2,4-diaminoquinazoline antifolate, methasquin, in rats and dogs.
Topics: Animals; Bile; Biological Assay; Chromatography, Paper; Creatinine; Dogs; Enterococcus faecalis; Female; Folic Acid Antagonists; Glomerular Filtration Rate; Intestinal Absorption; Kidney Concentrating Ability; Male; Methotrexate; Protein Binding; Quinazolines; Rats | 1971 |
Toxicologic studies of the 2,4-diamino-quinazoline antifolate, methasquin (NSC-122870).
Topics: Administration, Oral; Animals; Blood Cells; Body Weight; Bone Marrow; Bone Marrow Cells; Dogs; Female; Folic Acid Antagonists; Haplorhini; Injections, Intraperitoneal; Injections, Intravenous; Intestines; Macaca; Male; Methotrexate; Mice; Quinazolines; Rats | 1971 |
Drug response, dihydrofolate reductase, and cytogenetics of amethopterin-resistant Chinese hamster cells in vitro.
Topics: Animals; Aspartic Acid; Benzoates; Cell Line; Chromosome Aberrations; Cricetinae; Drug Resistance; Folic Acid Antagonists; In Vitro Techniques; Karyotyping; Methotrexate; Pharmacogenetics; Quinazolines; Tetrahydrofolate Dehydrogenase | 1972 |
Selection and characterization of mutant strains of Streptococcus faecium var. durans resistant to methasquin and amethopterin.
Topics: Culture Media; Depression, Chemical; Drug Antagonism; Drug Resistance, Microbial; Drug Synergism; Folic Acid; Folic Acid Antagonists; Genetics, Microbial; Methotrexate; Mutation; Purines; Quinazolines; Serine; Streptococcus; Tetrahydrofolates; Thymine Nucleotides | 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: dosage schedules and toxicity.
Topics: Aminopterin; Animals; Antineoplastic Agents; Body Weight; Dosage Forms; Folic Acid Antagonists; Leucovorin; Leukemia, Experimental; Male; Methotrexate; Mice; Quinazolines | 1971 |
Quinazoline antifolates: biologic activities.
Topics: Animals; Cell Line; Culture Techniques; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Streptococcus | 1968 |
Patterns of cross-resistance to the antifolate drugs trimetrexate, metoprine, homofolate, and CB3717 in human lymphoma and osteosarcoma cells resistant to methotrexate.
Topics: Antineoplastic Agents; Biological Transport; Burkitt Lymphoma; Cell Line; Drug Resistance; Folic Acid; Folic Acid Antagonists; Humans; Kinetics; Leukemia, Lymphoid; Lymphoma; Methotrexate; Osteosarcoma; Pyrimethamine; Quinazolines; Structure-Activity Relationship; T-Lymphocytes; Tetrahydrofolate Dehydrogenase; Trimetrexate | 1983 |
Use of a human tumor cloning system to evaluate analogs of methotrexate and mitoxantrone.
Topics: Anthraquinones; Antineoplastic Agents; Cell Line; Colony-Forming Units Assay; Drug Evaluation, Preclinical; Humans; Methotrexate; Mitoxantrone; Neoplasms; Quinazolines; Trimetrexate; Tumor Stem Cell Assay | 1984 |
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 |
Resistance of human tumor cell lines to antifolates.
Topics: B-Lymphocytes; Biological Transport; Cell Line; Drug Resistance; Folic Acid; Folic Acid Antagonists; Humans; Karyotyping; Methotrexate; Osteosarcoma; Pyrimethamine; Quinazolines; T-Lymphocytes; Tetrahydrofolate Dehydrogenase; 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 |
Comparative effects of methotrexate, two nonclassic folic acid antagonists, and cytarabine on hematopoietic precursor cells.
Topics: Animals; Cell Survival; Colony-Forming Units Assay; Cytarabine; Dogs; Dose-Response Relationship, Drug; Folic Acid Antagonists; Hematopoietic Stem Cells; Humans; In Vitro Techniques; Methotrexate; Mice; Quinazolines; Species Specificity; Triazines; Trimetrexate | 1982 |
Synthesis and evaluation of 2,4-diaminoquinazoline antifolates with activity against methotrexate-resistant human tumor cells.
Topics: Animals; Cell Line; DNA, Neoplasm; Drug Resistance; Female; Folic Acid Antagonists; Humans; Leukemia; Methotrexate; Mice; Mice, Inbred Strains; Quinazolines | 1984 |
Biochemical effects of a quinazoline inhibitor of thymidylate synthetase, N-(4-(N-(( 2-amino-4-hydroxy-6-quinazolinyl)methyl)prop-2-ynylamino) benzoyl)-L-glutamic acid (CB3717), on human lymphoblastoid cells.
Topics: Animals; Antimetabolites, Antineoplastic; Antineoplastic Agents; Cell Line; Deoxyribonucleotides; Deoxyuridine; Folic Acid; Folic Acid Antagonists; Humans; Kinetics; Lymphocytes; Methotrexate; Methyltransferases; Quinazolines; Ribonucleotides; Thymidylate Synthase | 1983 |
Effects of 5,8-dideazaisopteroylglutamate and its possible tri-gamma-glutamyl metabolite (5,8-dideazaisoPteGlu3) on colon adenocarcinoma, and the folate dependent enzymes thymidylate synthase and dihydrofolate reductase.
Topics: Adenocarcinoma; Animals; Cell Line; Colonic Neoplasms; DNA Replication; Drug Resistance; Female; Humans; Kinetics; Leukemia; Methotrexate; Methyltransferases; Mice; Mice, Inbred C57BL; Neoplasms, Experimental; Peptide Synthases; Quinazolines; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase | 1983 |
Improved synthesis and antitumor evaluation of 5,8-dideazaisofolic acid and closely related analogues.
Topics: Adenocarcinoma; Antineoplastic Agents; Cell Line; Chemical Phenomena; Chemistry; Folic Acid Antagonists; Gastrointestinal Neoplasms; Humans; Methotrexate; Quinazolines; Stereoisomerism; Structure-Activity Relationship | 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 |
Inhibition of a methotrexate-insensitive dihydrofolate reductase from L5178Y cells by substituted triazines and quinazolines.
Topics: Animals; Cells, Cultured; Folic Acid Antagonists; Leukemia L5178; Leukemia, Experimental; Methotrexate; Mice; Quinazolines; Triazines | 1983 |
Effects of 5,8-dideazaisofolic acid (IAHQ) on human tumor cells in culture and on normal and tumor-bearing hamsters.
Topics: Animals; Cell Division; Cell Line; Cricetinae; Cytotoxicity, Immunologic; Drug Resistance; Female; Folic Acid Antagonists; Humans; Lymphocyte Activation; Methotrexate; Neoplasms; Osteosarcoma; Pregnancy; Quinazolines; Sarcoma, Experimental | 1982 |
Establishment of methotrexate-resistant human acute lymphoblastic leukemia cells in culture and effects of folate antagonists.
Topics: Animals; Biological Transport; Cells, Cultured; Drug Interactions; Drug Resistance; Folic Acid Antagonists; Humans; Kinetics; Leucovorin; Leukemia, Experimental; Leukemia, Lymphoid; Methotrexate; Quinazolines; Tetrahydrofolate Dehydrogenase | 1982 |
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 |
Dihydrofolate reductase binding and cellular uptake of nonpolyglutamatable antifolates: correlates of cytotoxicity toward methotrexate-sensitive and -resistant human head and neck squamous carcinoma cells.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Agents; Carcinoma, Squamous Cell; Cell Division; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Folic Acid Antagonists; Head and Neck Neoplasms; Humans; Kinetics; Methotrexate; Ornithine; Pterins; Pteroylpolyglutamic Acids; Quinazolines; Tetrahydrofolate Dehydrogenase; Tritium; Tumor Cells, Cultured | 1995 |
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 |
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 |
Destruction of WiDr multicellular tumor spheroids with the novel thymidylate synthase inhibitor 1843U89 at physiological thymidine concentrations.
Topics: Antineoplastic Agents; Carcinoma; Cell Division; Colonic Neoplasms; Humans; Indoles; Isoindoles; Methotrexate; Quinazolines; Thymidine; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured | 1994 |
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 |
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 |
Identification of a reduced folate/methotrexate carrier in human KB-cells expressing high levels of membrane associated folate binding protein.
Topics: Aminopterin; Biological Transport; Carrier Proteins; Cell Division; Cell Membrane; Folate Receptors, GPI-Anchored; Folic Acid; Folic Acid Antagonists; Humans; KB Cells; Kinetics; Leucovorin; Methotrexate; Quinazolines; Receptors, Cell Surface; Structure-Activity Relationship | 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 |
Differential alterations of dihydrofolate reductase gene in human leukemia cell lines made resistant to various folate analogues.
Topics: Antineoplastic Agents; Base Sequence; Blotting, Southern; DNA, Neoplasm; Drug Resistance; Folic Acid; Folic Acid Antagonists; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; Humans; Leukemia; Methotrexate; Molecular Sequence Data; Oligonucleotide Probes; Polymerase Chain Reaction; Quinazolines; Tetrahydrofolate Dehydrogenase; Trimetrexate; 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 |
Amplification of the thymidylate synthase gene in an N10-propargyl-5,8-dideazafolic-acid-resistant human leukemia, MOLT-3 cell line developed in pteroylglutamic acid, but not in leucovorin.
Topics: Biological Transport; Drug Resistance; Enzyme Inhibitors; Folic Acid; Gene Amplification; Genes; Humans; Leucovorin; Leukemia; Methotrexate; Quinazolines; Thymidylate Synthase; 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 |
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 |
Biochemical and genetic tests for inhibitors of Leishmania pteridine pathways.
Topics: Animals; Cell Division; Drug Resistance; Folic Acid Antagonists; Humans; Leishmania; Methotrexate; Microbial Sensitivity Tests; Multienzyme Complexes; Mutation; Oxidoreductases; Pteridines; Pyrimidines; Quinazolines; Species Specificity; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase | 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 |
Molecular characterization of human acute leukemia cell line resistant to ZD9331, a non-polyglutamatable thymidylate synthase inhibitor.
Topics: Acute Disease; Antimetabolites, Antineoplastic; Antineoplastic Agents; Carrier Proteins; Drug Resistance, Neoplasm; Humans; Leukemia; Membrane Proteins; Membrane Transport Proteins; Methotrexate; Peptide Synthases; Quinazolines; Thymidylate Synthase; 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 |
Mechanism and pharmacological specificity of dUTPase-mediated protection from DNA damage and cytotoxicity in human tumor cells.
Topics: Antineoplastic Agents; DNA Damage; DNA Fragmentation; DNA, Neoplasm; DNA, Single-Stranded; Escherichia coli; Folic Acid; Humans; Methotrexate; Nucleic Acid Synthesis Inhibitors; Pyrophosphatases; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1998 |
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 |
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 |
Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines.
Topics: Cell Cycle; Cell Division; Culture Media; Drug Resistance; Enzyme Inhibitors; Fetal Blood; Head and Neck Neoplasms; Humans; Hypoxanthine; Inhibitory Concentration 50; Leucovorin; Leukemia; Methotrexate; Quinazolines; Thymidine; Thymidine Phosphorylase; Thymidylate Synthase; Tumor Cells, Cultured | 1999 |
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 |
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 |
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 |
Clustering of mutations in the first transmembrane domain of the human reduced folate carrier in GW1843U89-resistant leukemia cells with impaired antifolate transport and augmented folate uptake.
Topics: Antimetabolites, Antineoplastic; Biological Transport; Blotting, Northern; Blotting, Southern; Blotting, Western; Carrier Proteins; Cell Division; Cell Membrane; Chlorides; DNA Mutational Analysis; DNA, Complementary; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Enzyme Inhibitors; Exons; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Inhibitory Concentration 50; Isoindoles; Kinetics; Leucovorin; Leukemia; Membrane Proteins; Membrane Transport Proteins; Methotrexate; Mutagenesis, Site-Directed; Mutation; Polymorphism, Single-Stranded Conformational; Protein Structure, Secondary; Protein Structure, Tertiary; Quinazolines; Recombinant Proteins; Reduced Folate Carrier Protein; Thymidylate Synthase; Time Factors; Transfection; Trimetrexate; Tumor Cells, Cultured | 2000 |
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 |
Targeting Janus kinase 3 to attenuate the severity of acute graft-versus-host disease across the major histocompatibility barrier in mice.
Topics: Acute Disease; Animals; Bone Marrow Transplantation; Cell Transplantation; Drug Evaluation, Preclinical; Drug Therapy, Combination; Enzyme Inhibitors; Graft vs Host Disease; H-2 Antigens; Immunosuppressive Agents; Janus Kinase 3; Lymphocyte Activation; Lymphocyte Culture Test, Mixed; Male; Methotrexate; Mice; Mice, Inbred BALB C; Mice, Inbred C57BL; Phytohemagglutinins; Protein-Tyrosine Kinases; Quinazolines; Radiation Chimera; Signal Transduction; Spleen; T-Lymphocytes, Cytotoxic; Whole-Body Irradiation | 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 |
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 |
Dual targeting of Bruton's tyrosine kinase and Janus kinase 3 with rationally designed inhibitors prevents graft-versus-host disease (GVHD) in a murine allogeneic bone marrow transplantation model.
Topics: Acute Disease; Agammaglobulinaemia Tyrosine Kinase; Amides; Animals; Bone Marrow Transplantation; Drug Therapy, Combination; Enzyme Inhibitors; Graft vs Host Disease; Immunosuppressive Agents; Janus Kinase 3; Male; Methotrexate; Mice; Mice, Inbred BALB C; Mice, Inbred C57BL; Nitriles; Protein-Tyrosine Kinases; Quinazolines; Survival Rate; Treatment Outcome | 2004 |
Inhibition of Leishmania major pteridine reductase by 2,4,6-triaminoquinazoline: structure of the NADPH ternary complex.
Topics: Animals; Binding Sites; Crystallography, X-Ray; Electrons; Enzyme Inhibitors; Hydrogen Bonding; Leishmania major; Methotrexate; Models, Chemical; Models, Molecular; NADP; Oxidoreductases; Protein Conformation; Quinazolines | 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 |
Erlotinib (Tarceva, OSI-774) antagonizes ATP-binding cassette subfamily B member 1 and ATP-binding cassette subfamily G member 2-mediated drug resistance.
Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Cell Line, Tumor; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Erlotinib Hydrochloride; Estradiol; Gefitinib; Humans; Methotrexate; Mitoxantrone; Neoplasm Proteins; Neoplasms; Paclitaxel; Protein Binding; Quinazolines | 2007 |
Tumor-specific cytotoxicity and type of cell death induced by gefitinib in oral squamous cell carcinoma cell lines.
Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ascorbic Acid; Autophagy; Carcinoma, Squamous Cell; Caspase 3; Cisplatin; Doxorubicin; Drug Screening Assays, Antitumor; Drug Therapy, Combination; Gefitinib; HL-60 Cells; Humans; Methotrexate; Mitoxantrone; Mouth; Mouth Neoplasms; Phytotherapy; Plant Extracts; Quinazolines; Sodium Fluoride; Tumor Cells, Cultured | 2009 |
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 |
Vandetanib mediates anti-leukemia activity by multiple mechanisms and interacts synergistically with DNA damaging agents.
Topics: Acute Disease; Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Biomarkers, Tumor; Cell Cycle; Cell Proliferation; Cell Survival; DNA Damage; Dose-Response Relationship, Drug; Doxorubicin; Drug Synergism; Etoposide; HL-60 Cells; Humans; Inhibitory Concentration 50; Leukemia; Methotrexate; Piperidines; Protein Kinase Inhibitors; Quinazolines; Topoisomerase II Inhibitors | 2012 |
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 |
Imaging colon cancer response following treatment with AZD1152: a preclinical analysis of [18F]fluoro-2-deoxyglucose and 3'-deoxy-3'-[18F]fluorothymidine imaging.
Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Colonic Neoplasms; Dideoxynucleosides; Fluorine Radioisotopes; Fluorodeoxyglucose F18; Fluorouracil; HCT116 Cells; Humans; Immunoblotting; Ki-67 Antigen; Methotrexate; Mice; Mice, Nude; Organophosphates; Positron-Emission Tomography; Quinazolines; Radiopharmaceuticals; Thymidine; Thymidine Kinase; Xenograft Model Antitumor Assays | 2011 |
Inhibition of EGFR phosphorylation in a panel of human breast cancer cells correlates with synergistic interactions between gefitinib and 5'-DFUR, the bioactive metabolite of Xeloda.
Topics: Antineoplastic Agents; Breast Neoplasms; Capecitabine; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Cell Survival; Deoxycytidine; Drug Synergism; ErbB Receptors; Female; Floxuridine; Fluorouracil; Gefitinib; Gene Expression Regulation, Enzymologic; Humans; Inhibitory Concentration 50; Methotrexate; Phosphorylation; Protein Processing, Post-Translational; Quinazolines; Thymidine Phosphorylase; Thymidylate Synthase | 2012 |
Treatment of leptomeningeal spread of NSCLC: a continuing challenge.
Topics: Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Combined Modality Therapy; Cytarabine; ErbB Receptors; Erlotinib Hydrochloride; Glutamates; Guanine; Humans; Meningeal Neoplasms; Methotrexate; Mutation; Pemetrexed; Quinazolines; Radiation Dosage | 2012 |
[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 |
Analysis of treatment outcomes of intraventricular chemotherapy in 105 patients for leptomeningeal carcinomatosis from non-small-cell lung cancer.
Topics: Adult; Age Factors; Aged; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Cranial Nerve Diseases; Cytarabine; Erlotinib Hydrochloride; Female; Gefitinib; Headache; Humans; Hydrocortisone; Infusions, Intraventricular; Intracranial Pressure; Karnofsky Performance Status; Lung Neoplasms; Male; Meningeal Carcinomatosis; Mental Disorders; Methotrexate; Middle Aged; Nausea; Palliative Care; Protein Kinase Inhibitors; Quinazolines; Retrospective Studies; Vomiting | 2013 |
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 |
Medical treatment of ectopic pregnancy: is there something new?
Topics: Abortifacient Agents, Nonsteroidal; Animals; Antineoplastic Agents; ErbB Receptors; Female; Gefitinib; Humans; Methotrexate; Placenta; Pregnancy; Pregnancy, Ectopic; Quinazolines | 2013 |
Effects of gefitinib, an epidermal growth factor receptor inhibitor, on human placental cell growth.
Topics: Abortifacient Agents, Nonsteroidal; Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Evaluation, Preclinical; Drug Therapy, Combination; ErbB Receptors; Female; Gefitinib; Humans; Methotrexate; Mice; Mice, SCID; Placenta; Pregnancy; Pregnancy Trimester, First; Pregnancy, Ectopic; Quinazolines | 2013 |
Combination gefitinib and methotrexate treatment for non-tubal ectopic pregnancies: a case series.
Topics: Abortifacient Agents, Nonsteroidal; Acneiform Eruptions; Adult; Cesarean Section; Chorionic Gonadotropin; Fallopian Tubes; Female; Gefitinib; Humans; Methotrexate; Pregnancy; Pregnancy Outcome; Pregnancy, Ectopic; Quinazolines; Ultrasonography, Prenatal; Young Adult | 2014 |
Molecular diagnostics and therapeutics for ectopic pregnancy.
Topics: Animals; Biomarkers; Female; Gefitinib; Humans; Methotrexate; Pregnancy; Pregnancy, Ectopic; Quinazolines | 2015 |
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 |
EGFR inhibition for recurrent or metastatic HNSCC.
Topics: Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Neoplasm Recurrence, Local; Quinazolines | 2015 |
Head and neck cancer: second-line afatinib shows promise.
Topics: Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Female; Head and Neck Neoplasms; Humans; Male; Methotrexate; Neoplasm Recurrence, Local; Quinazolines | 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 |
Vinorelbine Potently Induces Placental Cell Death, Does Not Harm Fertility and is a Potential Treatment for Ectopic Pregnancy.
Topics: Animals; Antineoplastic Agents, Phytogenic; Apoptosis; Cell Death; Cell Line; Cell Proliferation; Cell Survival; Disease Models, Animal; Female; Fertility; Gefitinib; Heterografts; Humans; Methotrexate; Mice; Microtubules; Miosis; Placenta; Pregnancy; Pregnancy, Ectopic; Quinazolines; Trophoblasts; Vinblastine; Vinorelbine | 2018 |
Regulations of expressions of rat/human sulfotransferases by anticancer drug, nolatrexed, and micronutrients.
Topics: Animals; Antimetabolites, Antineoplastic; Arylsulfotransferase; Blotting, Western; Cell Cycle; Dose-Response Relationship, Drug; Female; Folic Acid; Hep G2 Cells; Humans; Leucovorin; Male; Methotrexate; Micronutrients; Quinazolines; Rats; Rats, Sprague-Dawley; RNA, Messenger; Sex Factors; Sulfotransferases | 2022 |
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 |