quinazolines has been researched along with folic acid in 225 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 82 (36.44) | 18.7374 |
| 1990's | 95 (42.22) | 18.2507 |
| 2000's | 30 (13.33) | 29.6817 |
| 2010's | 11 (4.89) | 24.3611 |
| 2020's | 7 (3.11) | 2.80 |
| Authors | Studies |
|---|---|
| Bertino, JR; Hynes, JB; Moroson, BA; Scanlon, KJ | 1 |
| McCuen, RW; Sirotnak, FM | 1 |
| Colvin, PL; Eason, DE; Garrett, CM; Hynes, JB | 1 |
| Hynes, JB; Oatis, JE | 1 |
| Garrett, CM; Hynes, JB | 1 |
| Finer-Moore, JS; Kamb, A; Stroud, RM | 1 |
| Bader, H; Beardsley, GP; DeYarman, MT; Freisheim, JH; Galivan, J; Kerwar, SS; Moroson, BA; O'Connor, BM; Rosowsky, A; Russello, O | 1 |
| Calvert, AH; Finer-Moore, J; Kamb, A; Stroud, RM | 1 |
| Ohnuma, T; Takemura, Y | 1 |
| Barker, AJ; Bishop, JA; Burrows, KD; Hughes, LR; Jackman, AL; O'Connor, BM; Roberts, N; Warner, P | 1 |
| Gaumont, Y; Greco, WR; Kisliuk, RL; Parsons, JC | 1 |
| Seitz, DE | 1 |
| Miyachi, H; Ohnuma, T; Sekiguchi, S; Takemura, Y | 1 |
| Galivan, J; Malik, ND; Piper, JR; Rhee, MS; Sirotnak, FM | 1 |
| Goldman, ID; Seither, RL; Trent, DF | 2 |
| Adkins, DA; Houghton, JA; Houghton, PJ; Rahman, A | 1 |
| Dev, IK; Duch, DS; Edwards, DM; Ferone, R; Gaumont, Y; Humphreys, J; Kisliuk, RL; Li, SW; Nair, MG; Smith, GK | 1 |
| Chmurzyńska, W; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M | 2 |
| Brown, M; Calvert, AH; Gibson, W; Hughes, LR; Jackman, AL; Judson, IR; Kimbell, R; Taylor, GA | 1 |
| Calvert, AH; Gibson, W; Hughes, LR; Jodrell, DI; Newell, DR | 1 |
| Bensted, JP; Calvert, AH; Clinton, S; Hughes, LR; Jodrell, DI; Morgan, SE; Newell, DR | 1 |
| Berman, EM; Werbel, LM | 1 |
| Calvert, AH; Flinn, A; Jackman, AL; Jones, TR; O'Connor, BM; Thornton, TJ; Warner, P | 1 |
| Aherne, GW; Curtin, NJ; Harris, AL | 1 |
| Keyomarsi, K; Moran, RG | 1 |
| Balinska, M; Bunni, M; Galivan, J; Maley, F; Maley, GF; Priest, DG; Rhee, MS | 1 |
| Appelt, K; Matthews, DA; Oatley, SJ; Xuong, NH | 1 |
| Fauman, EB; Finer-Moore, JS; Hardy, L; Maley, F; Maley, GF; Montfort, WR; Perry, KM; Stroud, RM | 1 |
| Finer-Moore, JS; Montfort, WR; Stroud, RM | 1 |
| Bishop, JA; Burrows, KD; Calvert, AH; Hughes, LR; Jackman, AL; Jones, TR; Marsham, PR; O'Connor, BM; Oldfield, J; Smith, RC | 1 |
| Bishop, JA; Calvert, AH; Hughes, LR; Jackman, AL; Jones, TR; Marsham, PR; O'Connor, BM; Thornton, TJ | 1 |
| Jackman, AL; Jansen, G; Newell, DR; Rijksen, G; Schornagel, JH; Westerhof, GR | 1 |
| Buamah, PK; Cornell, C; Harris, AL; James, OF; Skillen, AW | 1 |
| Buamah, PK; Harris, AL; James, OF; Skillen, AW | 1 |
| Bassendine, MF; Curtin, NJ; Harris, AL; James, OF; Loose, H | 1 |
| Allegra, CJ; Baram, J; Drake, JC; Hoang, K; Yeh, GC | 1 |
| Calvert, AH; Jackman, AL; Jones, TR; Newell, DR; Sikora, E; Simmonds, AJ | 1 |
| Calvert, AH; Jackman, AL; Newell, DR; Sikora, E | 1 |
| Gaumont, Y; Kisliuk, RL; Murthy, BR; Nair, MG; Piper, JR; Sirotnak, FM; Thorndike, J | 1 |
| Bunni, M; Dilwith, R; Galivan, J; Johnson, TB; Nair, MG; Priest, DG; Rhee, MS | 1 |
| Allegra, CJ; Beaver, J; Boarman, D; Chabner, B; Kovacs, JA; Lewis, M; Masur, H; Parrillo, JE | 1 |
| Danenberg, KD; Danenberg, PV | 1 |
| Bertino, JR; Chou, TC; Romanini, A; Sherwood, RF; Sobrero, AF | 1 |
| Goldman, ID; Mikulecky, DC; Rape, TJ; Seither, RL; Trent, DF | 1 |
| Jansen, G; Rijksen, G; Schornagel, JH; van der Veer, LJ; Westerhof, GR | 1 |
| Balmanno, K; Calvert, AH; Hughes, LR; Jackman, AL; Taylor, GA | 1 |
| Bunni, M; Chou, TC; Galivan, J; Johnson, TB; Nair, MG; Priest, D; Rhee, MS | 1 |
| Calvert, AH; Harrap, KR; Hughes, LR; Jackman, AL; Newell, DR; Taylor, GA | 1 |
| Appelt, K; Matthews, DA; Oatley, SJ | 1 |
| Calvert, AH; Flinn, A; Jackman, AL; Jones, TR; Newell, DR; Thornton, TJ | 1 |
| Cole, A; Freisheim, JH; Hagan, RL; Hynes, JB; Kohler, W; Patil, SA | 1 |
| Aherne, GW; Curtin, NJ; Harris, AL; Marks, V; Piall, EM | 1 |
| Curtin, NJ; Harris, AL; Newell, DR | 1 |
| Buamah, PK; Cassells-Smith, AJ; Harris, AL; James, OF; Skillen, AW | 1 |
| Jackman, AL; Jones, TR; Kempny, M; Krzyzanowski, L; Newell, DR; Pawelczak, K; Rzeszotarska, B | 1 |
| Alison, DL; Calvert, AH; Harrap, KR; Jackman, AL | 1 |
| Holland, JF; Kano, Y; Ohnuma, T | 1 |
| Galivan, J; Nimec, Z; Rhee, M | 1 |
| Boschelli, D; Galivan, J; Kerwar, SS; Nimec, Z; Oronsky, AL; Rhee, M | 1 |
| Bassendine, MF; Curtin, NJ; Harris, AL; James, OF | 1 |
| Bennett, M; Buamah, PK; James, OF; Lendrum, R; McArdle, P | 1 |
| Gaumont, Y; Hsiao, MC; Kalman, TI; Kisliuk, RL; Nair, IG; Nair, MG; Nanavati, NT | 1 |
| Abels, J; Ermens, AA; Lindemans, J | 1 |
| Cantwell, BM; Harris, AL | 1 |
| Borst, P; Calafat, J; Fase-Fowler, F; van Luenen, H; White, TC | 1 |
| Maley, F; Maley, GF | 2 |
| Boiocchi, M; Broggini, M; D'Incalci, M; Erba, E; Lorico, A; Rappa, G; Toffoli, G | 2 |
| Bork, E; Hansen, HH; Vest, S | 1 |
| Curtin, NJ; Harris, AL | 1 |
| Calvert, AH; Cantwell, BM; Harris, AL; Kaye, SB; Macaulay, V; Milsted, RA; Smith, IE | 1 |
| Cavalli, F; D'Incalci, M; Ginier, M; Sessa, C; Willems, Y; Zucchetti, M | 1 |
| Cantwell, BM; Harding, MJ; Harris, AL; Kaye, SB; Milstead, RA | 1 |
| Bishop, JA; Calvert, AH; Grzelakowska-Sztabert, B; Gumbrell, LA; Harland, SJ; Harrap, KR; Jackman, AL; Judson, IR; Newell, DR; Sikora, E | 1 |
| Crossley, PH; Imam, AM; Jackman, AL; Little, PF | 1 |
| Garvey, EP; Santi, DV | 1 |
| Dhawan, R; Ferone, R; Gaumont, Y; Ghazala, M; Kalman, TI; Kisliuk, RL; Nair, MG | 1 |
| Alison, DL; Calvert, AH; Harrap, KR; Jarman, M; Jones, TR; Manteuffel-Cymborowska, M; Newell, DR; O'Connor, P | 1 |
| Alison, DL; Calvert, AH; Harland, SJ; Jackman, AL; Jones, TR; McElwain, TJ; Newell, DR; Robinson, BA; Siddik, ZH; Wiltshaw, E | 1 |
| Calvert, AH; Harland, SJ; Harrap, KR; Jackman, AL; Jones, TR; Smithers, MJ; Taylor, MA | 1 |
| Danenberg, PV; Pogolotti, AL; Santi, DV | 1 |
| Cantwell, BM; Earnshaw, M; Harris, AL | 1 |
| Xu, B | 1 |
| Cheng, YC; Dutschman, GE; Fisher, MH; Nair, MG; Nanavathi, NT; Starnes, MC | 1 |
| Camerman, A; Camerman, N; Mastropaolo, D; Smith, HW | 1 |
| Alison, DL; Calvert, AH; Harland, SJ; Harrap, KR; Hart, LI; Newell, DR; Sessa, C | 1 |
| Coderre, JA; Garvey, EP; Santi, DV | 1 |
| Dunlap, RB; Ellis, PD; Lyon, JA | 1 |
| Donsbach, RC; Sirotnak, FM | 1 |
| Bayles, A; Olszewski, B; Thompson, PE | 1 |
| Hutchison, DJ; Rader, JI | 1 |
| Davoll, J; Johnson, AM | 1 |
| Dewey, VC; Kidder, GW | 1 |
| Diddens, H; Jackson, RC; Niethammer, D | 2 |
| Danenberg, PV; Lockshin, A; Mondal, K | 1 |
| Besserer, JA; Boritzki, TJ; Elslager, EF; Fry, DW; Jackson, RC; Leopold, WR; Sloan, BJ | 1 |
| Calvert, AH; Harrap, KR; Jackman, AL; Taylor, GA | 2 |
| Benjamin, MB; Hynes, JB; McCue, GH; Yang, YC | 1 |
| Calvert, AH; Jackman, AL; Jackson, RC | 1 |
| Calvert, AH; Harrap, KR; Hart, LI; Jackman, AL | 1 |
| Grzelakowska-Sztabert, B; Sikora, F | 1 |
| Grzelakowska-Sztabert, B; Sikora, E | 1 |
| McCormack, JJ | 1 |
| Brown, SJ; Calvert, AH; Harrap, KR; Jackman, AL; Jones, M; Jones, TR | 1 |
| Calvert, AH; Dady, PJ; Grzelakowska-Sztabert, B; Harrap, KR; Jones, TR; Paine, RM; Taylor, GA | 1 |
| Boyle, FT; Brown, M; Brunton, L; Jackman, AL; Kimbell, R | 1 |
| Aherne, GW; Boyle, FT; Brown, M; Gibson, W; Hardcastle, A; Jackman, AL; Kelland, LR; Kimbell, R | 1 |
| Calvert, AH; Freemantle, SJ; Jackman, AL; Kelland, LR; Lunec, J | 1 |
| Jansen, G; Peters, GJ; Pinedo, HM; Rijnboutt, S; Schornagel, JH; Westerhof, GR | 1 |
| Aherne, GW; Hardcastle, A; Jackman, AL; Kelland, LR; Kimbell, R | 1 |
| Barker, AJ; Boyle, FT; Calvert, AH; Hughes, LR; Jackman, AL; Kimbell, R; Marsham, PR; O'Connor, BM; Pegg, SJ; Wardleworth, JM | 1 |
| Chong, LK; Tattersall, MH | 1 |
| Cieśla, J; Maley, F; Montfort, WR; Weichsel, A | 1 |
| Chmurzyńska, W; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M; Peska, M | 1 |
| Allegra, CJ | 1 |
| Erlichman, C; Mandelbaum, S; Mitrovski, B; Pressacco, J | 1 |
| Connick, TJ; Dunlap, RB; Ellis, PD; Reilly, RT | 2 |
| Erlichman, C; Mitrovski, B | 1 |
| Clarke, SJ; Jackman, AL; Judson, IR | 1 |
| Jackman, A; Judson, I | 1 |
| Dallas, WS; Dev, IK; Ferone, R; Hanlon, M; McKee, DD; Yates, BB | 1 |
| Taylor, EC | 1 |
| Bavetsias, V; Bisset, GM; Calvert, AH; Gibson, W; Harrap, KR; Jackman, AL; Jodrell, DI; Kimbell, R; Smith, MN; Stephens, TC | 1 |
| Boyle, FT; Brown, M; Hughes, LR; Jackman, AL; Kimbell, R; Matusiak, ZS; Slater, AM; Smith, MN; Stephens, TC | 1 |
| Boyle, FT; Jackman, AL; McCloskey, ML; Smith, MN; Stephens, TC; Waterman, SE | 1 |
| Bavetsias, V; Bisset, GM; Boyle, FT; Jackman, AL; Pawelczak, K; Thornton, TJ | 1 |
| Aherne, W; Boyle, FT; Hardcastle, A; Jackman, AL; Kimbell, R | 1 |
| Jansen, G; Pinedo, HM; Rijnboutt, S; Schornagel, JH; Westerhof, GR | 1 |
| Aherne, GW; Dive, C; Fisher, TC; Gregory, CD; Hartley, JA; Hickman, JA; Jackman, AL; Milner, AE | 1 |
| Bagnara, AS; Nott, SE | 1 |
| Ando, K; Ando, Y; Kobayashi, H; Miyachi, H; Takemura, Y | 1 |
| Attard, J; Bleckman, TM; Deal, JG; Janson, CA; Kathardekar, V; Matthews, DA; Smith, WW; Webber, S; Webber, SE; Welsh, KM | 1 |
| Amyx, H; Boytos, CM; Duch, DS; Ferone, R; Smith, GK; Wilson, HR | 1 |
| Jackman, AL; Kobayashi, H; Miyachi, H; Skelton, L; Takemura, Y | 1 |
| Bavetsias, V; Bisset, GM; Boyle, FT; Gibson, W; Jackman, AL; Kimbell, R | 1 |
| Birdsall, DL; Finer-Moore, J; Stroud, RM | 1 |
| Gibson, W; Jackman, AL; Kimbell, R; Kobayashi, H; Miyachi, H; Takemura, Y | 1 |
| Calvert, AH; Jackman, AL | 1 |
| Jansen, G; Jolivet, J; Kathmann, I; Molthoff, C; Pinard, MF; Ratnam, M; Schornagel, JH; Westerhof, R | 1 |
| Ferone, R; Hanlon, MH | 1 |
| Beechem, JM; Bradrick, TD; Howell, EE | 1 |
| Ando, Y; Kobayashi, H; Miyachi, H; Takemura, Y | 1 |
| Dabrowska, M; Michalski, R; Pawelczak, K; Rode, W; Wranicz, M; Zieliñski, Z | 1 |
| Rutenber, EE; Stroud, RM | 1 |
| Rutenber, EE; Sage, CR; Stout, TJ; Stroud, RM | 1 |
| Bavetsias, V; Bisset, GM; Boyle, FT; Jackman, AL; Marshall, D; Pedley, RB; Springer, CJ | 1 |
| Appleman, JR; Spencer, HT; Villafranca, JE | 1 |
| Aherne, W; Clarke, S; Hardcastle, A | 1 |
| Cook, RJ | 1 |
| Dousa, TP; Grande, JP; Matousovic, K; Tsuboi, Y; Walker, H | 1 |
| Changchien, L; Maley, F; Montfort, WR; Strop, P | 1 |
| Kamen, B | 1 |
| Kobayashi, H; Ohnuma, T; Takemura, Y | 1 |
| Changchien, L; Lobo, AP; Maley, F; Montfort, WR; Nair, MG; Weichsel, A | 1 |
| Banerjee, D; Bertino, JR; Capiaux, GM; Ercikan-Abali, EA; Liu-Chen, X; Tong, Y; Zhao, SC | 1 |
| Loriga, M; Paglietti, G; Vitale, G | 1 |
| Birdsall, DL; Finer-Moore, J; Huang, W; Santi, DV; Stroud, RM | 1 |
| Sage, CR; Stout, TJ; Stroud, RM | 1 |
| Andis, SL; Bewley, JR; Chen, VJ; Iversen, PW; Mendelsohn, LG; Schultz, RM; Seitz, DE; Shih, C; Tonkinson, JL | 2 |
| Jackman, AL; Ormerod, MG; Skelton, LA; Titley, JC | 1 |
| Biermann, D; Finer-Moore, J; Michelitsch, MD; Nissen, R; Sage, CR; Stout, TJ; Stroud, RM | 1 |
| Loney, TL; Maybaum, J; Parsels, JD; Parsels, LA; Radany, EH; Wagner, LM | 1 |
| Banerjee, D; Bertino, JR; Ercikan-Abali, EA; Liu-Chen, X; Maley, F; Tong, Y; Zhao, SC | 1 |
| Brunton, LA; Jackman, AL; Kimbell, R; Ormerod, MG; Skelton, LA; Titley, J | 1 |
| Chmurzyńska, W; Dudkowska, M; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M | 1 |
| Bowman, KJ; Calvert, AH; Curtin, NJ; Golding, BT; Griffin, RJ; Huang, B; Loughlin, PJ; Newell, DR; Turner, RN | 1 |
| Anderson, AC; DeLano, WL; O'Neil, RH; Stroud, RM | 1 |
| Newell, DR | 1 |
| Danenberg, PV; Malli, H; Swenson, S | 1 |
| Aherne, GW; Benstead, J; Clarke, SJ; Farrugia, DC; Jackman, AL; Pritchard, DM | 1 |
| Anderson, AC; Freymann, DM; Perry, KM; Stroud, RM | 1 |
| Strømhaug, A; Warren, DJ | 1 |
| Assaraf, YG; Drori, S; Jansen, G; Mauritz, R; Peters, GJ | 1 |
| Cassidy, J | 1 |
| Chmurzyska, W; Dudkowska, M; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M; Stachurska, A | 1 |
| DeRose, EF; Gabel, SA; Howell, EE; Lebetkin, MS; Levy, LA; Li, D; London, RE; Wall, MJ | 1 |
| Krupenko, SA; Vlasov, AP; Wagner, C | 1 |
| Backus, HH; Bunni, MA; Comijn, L; Jackman, AL; Jansen, G; Mitchell, F; Peters, GJ; Priest, DG; Smid, K; van der Wilt, CL; Veerman, G; Voorn, DA; Wouters, D | 1 |
| Burris, H; Goetz, A; Hohneker, JA; Johnson, TR; Lampkin, T; Rowinsky, EK; Sailstad, J; Schwartz, G; Smetzer, L; Von Hoff, DD | 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 |
| Finer-Moore, JS; Fritz, TA; Liu, L; Stroud, RM | 1 |
| Dudkowska, M; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M; Stachurska, A | 1 |
| Anderson, KS; Atreya, CE; Chang, SY; Johnson, EF; Liang, PH; Williamson, J | 1 |
| Bavetsias, V; Gibbs, D; Jackman, AL; Jansen, G; Skelton, LA; Theti, DS; Titley, J | 1 |
| Faessel, HM; Greco, WR; Rustum, YM; Slocum, HK | 1 |
| Jackman, AL; Theti, DS | 1 |
| Alfieri, S; Cellini, N; De Paoli, A; Di Miceli, D; Doglietto, GB; Gambacorta, MA; Mantini, G; Miccichè, F; Morganti, AG; Ratto, C; Rossi, C; Rotondi, F; Valentini, V; Vargas, JG | 1 |
| Goldman, ID; Wang, Y; Zhao, R | 1 |
| Fukushima, M; Hoogeland, MF; Peters, GJ; Temmink, OH | 1 |
| Caperelli, CA; Dahms, TE; Giroux, EL; Sainz, G; Smith, JL | 1 |
| Assaraf, YG; Ifergan, I; Kadry, WN; Pinter, RY | 1 |
| Bavetsias, V; Forster, MD; Gibbs, DD; Green, M; Henderson, E; Jackman, AL; Mitchell, F; Raynaud, F; Theti, DS; Valenti, M; Wood, N | 1 |
| Dudkowska, M; Grzelakowska-Sztabert, B; Manteuffel-Cymborowska, M | 1 |
| Dudkowska, M; Grzelakowska-Sztabert, B; Jaworski, T; Manteuffel-Cymborowska, M | 1 |
| Anderson, KS; Atreya, CE; Doan, LT; Martucci, WE; Vargo, MA | 1 |
| Waldman, AS; Wyatt, MD; Yang, Z | 1 |
| Bajer, S; Dudkowska, M; Grzelakowska-Sztabert, B; Jaworski, T; Manteuffel-Cymborowska, M; Zielińska, J | 1 |
| Calhau, C; Giovannetti, E; Jansen, G; Kathmann, I; Lemos, C; Peters, GJ | 1 |
| Aispuro-Hernandez, E; Arvizu-Flores, AA; Garcia-Orozco, KD; Maley, F; Rojo-Domínguez, A; Sotelo-Mundo, RR; Valenzuela-Soto, E; Varela-Romero, A; Velazquez-Contreras, EF; Yepiz-Plascencia, G | 1 |
| Leamon, CP; Müller, C; Reddy, JA; Schibli, R | 1 |
| AVAKIAN, S; MARTIN, GJ; MOSS, J | 1 |
| Bayliss, G; He, S; Liu, N; Zhuang, S | 1 |
| Li, X; Lu, Y; Yin, Z; Yu, Y; Zhao, X | 1 |
| Ali, IA; Elfekki, IM; Elshihawy, HE; Eltamany, EH; Hassan, WF | 1 |
| Cui, W; Feng, B; Li, H; Liu, L; Liu, M; Shi, Y; Su, C; Su, R; Zhao, L | 1 |
| Matsumoto, K; Onda, T; Yaegashi, N | 1 |
| Goldman, ID; Visentin, M; Zhao, R | 1 |
| Finer-Moore, JS; Lee, TT; Stroud, RM | 1 |
| Liu, H; Shi, L; Tong, G; Wang, D; Wu, J; Xu, L; Yan, D; Yu, C; Zhu, X | 1 |
| Berciano, MT; Casafont, I; Cuadrado, A; Lafarga, M; Mata-Garrido, J; Tapia, O | 1 |
| Bhatt, JD; Chudasama, CJ; Dixit, BC; Dixit, RB; Patel, BD; Patel, TS | 1 |
| Bratton, BP; Gitai, Z; Kim, H; Li, SH; Martin, JK; Mateus, A; Moore, GM; Rabinowitz, JD; Savitski, MM; Sheehan, JP; Typas, A; Wilson, MZ | 1 |
| Adam, V; Heger, Z; Michalkova, H; Pribyl, J; Rex, S; Skladal, P; Skubalova, Z; Sukupova, M; Weerasekera, A; Zahalka, M | 1 |
| Huang, G; Li, W; Liu, H; Luo, S; Lv, X; Wang, Y; Zhou, D | 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 |
| Bedi, PMS; Bhagat, K; Kaur Gulati, H; Kaur, A; Kumar, N; Sharma, A; Singh, H; Singh, JV | 1 |
| Charushin, VN; Kovalev, IS; Majee, A; Santra, S; Varaksin, MV; Zyryanov, GV | 1 |
12 review(s) available for quinazolines and folic acid
| Article | Year |
|---|---|
The renewed potential for folate antagonists in contemporary cancer chemotherapy.
Topics: Antineoplastic Agents; Folic Acid; Folic Acid Antagonists; Humans; Neoplasms; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1991 |
[New trends in antineoplastic drug research].
Topics: Antibodies, Monoclonal; Antineoplastic Agents; Carboplatin; Danazol; Fluorouracil; Folic Acid; Harringtonines; Humans; Organoplatinum Compounds; Quinazolines; Thymine Nucleotides | 1985 |
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 |
Design and synthesis of inhibitors of folate-dependent enzymes as antitumor agents.
Topics: Acyltransferases; Animals; Antineoplastic Agents; Drug Design; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Hydroxymethyl and Formyl Transferases; Indicators and Reagents; Molecular Structure; Pemetrexed; Phosphoribosylglycinamide Formyltransferase; Pyrroles; Quinazolines; Structure-Activity Relationship; Tetrahydrofolates | 1993 |
Folate-based thymidylate synthase inhibitors as anticancer drugs.
Topics: Antineoplastic Agents; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Indoles; Isoindoles; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase | 1995 |
Folate and antifolate pharmacology.
Topics: Antimetabolites, Antineoplastic; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Methotrexate; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Trimetrexate | 1997 |
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 |
Thymidylate synthase inhibitors.
Topics: Animals; Antimetabolites, Antineoplastic; Colorectal Neoplasms; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Indoles; Isoindoles; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase | 1999 |
Thymidylate synthase inhibitors in colorectal cancer.
Topics: Antineoplastic Agents; Clinical Trials as Topic; Colorectal Neoplasms; Enzyme Inhibitors; Folic Acid; Glutamates; Guanine; Humans; Pemetrexed; Quinazolines; Thiophenes; Thymidylate Synthase | 2000 |
Pharmacotherapy for recurrent ovarian cancer: current status and future perspectives.
Topics: Angiogenesis Inhibitors; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antimetabolites, Antineoplastic; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzimidazoles; Carboplatin; Carcinoma, Ovarian Epithelial; Deoxycytidine; Doxorubicin; Everolimus; Female; Folic Acid; Gemcitabine; Humans; Indazoles; Neoplasm Recurrence, Local; Neoplasms, Glandular and Epithelial; Nivolumab; Ovarian Neoplasms; Paclitaxel; Phthalazines; Piperazines; Poly(ADP-ribose) Polymerase Inhibitors; Polyethylene Glycols; Pyrimidines; Quinazolines; Recombinant Fusion Proteins; Sirolimus; Sulfonamides; Topotecan; TOR Serine-Threonine Kinases; Vinca Alkaloids | 2015 |
Dihydrofolate reductase inhibitors: patent landscape and phases of clinical development (2001-2021).
Topics: Amino Acids; Folic Acid; Folic Acid Antagonists; Humans; Niacinamide; Patents as Topic; Phosphates; Quinazolines; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates | 2022 |
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 |
3 trial(s) available for quinazolines and folic acid
| Article | Year |
|---|---|
Phase II study of a novel antifolate, N10-propargyl-5,8 dideazafolic acid (CB3717), in malignant mesothelioma.
Topics: Adult; Drug Evaluation; Folic Acid; Folic Acid Antagonists; Humans; Mesothelioma; Middle Aged; Quinazolines | 1986 |
A phase I and pharmacokinetic study of 1843U89, a noncompetitive inhibitor of thymidylate synthase, in patients with advanced solid malignancies.
Topics: Adult; Aged; Antineoplastic Agents; Area Under Curve; Dose-Response Relationship, Drug; Enzyme Inhibitors; Exanthema; Female; Folic Acid; Humans; Indoles; Infusions, Intravenous; Isoindoles; Male; Middle Aged; Mouth Mucosa; Neoplasms; Neutropenia; Quinazolines; Stomatitis; Thymidylate Synthase | 2001 |
Chemoradiation with raltitrexed (Tomudex) in preoperative treatment of stage II-III resectable rectal cancer: a phase II study.
Topics: Aged; Antimetabolites, Antineoplastic; Female; Fluorouracil; Folic Acid; Follow-Up Studies; Hematinics; Humans; Male; Middle Aged; Neoplasm Staging; Quinazolines; Radiotherapy, Conformal; Rectal Neoplasms; Thiophenes | 2004 |
210 other study(ies) available for quinazolines and folic acid
| Article | Year |
|---|---|
Quinazoline analogues of folic acid as inhibitors of thymidylate synthetase from bacterial and mammalian sources.
Topics: Animals; Cell Division; Folic Acid; In Vitro Techniques; Lacticaseibacillus casei; Leukemia L1210; Methyltransferases; Mice; Neoplasms, Experimental; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1979 |
Thymidylate synthetase from Diplococcus pneumoniae, properties and inhibition by folate analogs.
Topics: Chromatography, Gel; Folic Acid; Folic Acid Antagonists; Hydrogen-Ion Concentration; Kinetics; Magnesium; Methyltransferases; Molecular Weight; Quinazolines; Streptococcus pneumoniae; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase | 1975 |
Quinazolines as inhibitors of dihydrofolate reductase. 4. Classical analogues of folic and isofolic acids.
Topics: Animals; Antineoplastic Agents; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Liver; Mice; Quinazolines; Rats; Streptococcus; Structure-Activity Relationship | 1977 |
Sycnthesis of quinazoline analogues of folic acid modified at postion 10.
Topics: Animals; Antineoplastic Agents; Folic Acid; Leukemia L1210; Mice; Quinazolines | 1977 |
Synthesis of quinazoline analogs of isofolic acid.
Topics: Animals; Folic Acid; Folic Acid Antagonists; In Vitro Techniques; Leukemia L1210; Liver; Mice; Quinazolines; Rats; Structure-Activity Relationship | 1975 |
Cofactor triggers the conformational change in thymidylate synthase: implications for an ordered binding mechanism.
Topics: Binding Sites; Crystallization; Deoxyuracil Nucleotides; Escherichia coli; Folic Acid; Models, Molecular; Molecular Structure; Polyglutamic Acid; Protein Conformation; Quinazolines; Thymidylate Synthase; X-Ray Diffraction | 1992 |
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 |
Structural basis for recognition of polyglutamyl folates by thymidylate synthase.
Topics: Amino Acid Sequence; Animals; Binding Sites; Chemical Phenomena; Chemistry, Physical; Crystallization; Deoxyuracil Nucleotides; Electrochemistry; Escherichia coli; Folic Acid; Humans; Kinetics; Mice; Models, Molecular; Molecular Sequence Data; Molecular Structure; Protein Conformation; Quinazolines; Sequence Homology, Amino Acid; Structure-Activity Relationship; Thymidylate Synthase; X-Ray Diffraction | 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 |
Quinoline antifolate thymidylate synthase inhibitors: variation of the C2- and C4-substituents.
Topics: Animals; Cell Survival; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1992 |
Quantitation of folic acid enhancement of antifolate synergism.
Topics: Cell Division; Dose-Response Relationship, Drug; Drug Synergism; Folic Acid; Folic Acid Antagonists; Humans; Lymphoma; Quinazolines; Tetrahydrofolates; Trimetrexate; Tumor Cells, Cultured | 1992 |
Oncology drug discovery and clinical trial testing: who's listening?
Topics: Antineoplastic Agents; Clinical Trials as Topic; Drug Evaluation; Fluorouracil; Folic Acid; Humans; Neoplasms; Quinazolines; Thymidylate Synthase | 1992 |
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 |
Synthesis and antifolate evaluation of the 10-propargyl derivatives of 5-deazafolic acid, 5-deazaaminopterin, and 5-methyl-5-deazaaminopterin.
Topics: Aminopterin; Animals; Cell Division; Folic Acid; Folic Acid Antagonists; Humans; Leukemia L1210; Mammary Neoplasms, Experimental; Mice; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1992 |
Rate and extent of interconversion of tetrahydrofolate cofactors to dihydrofolate after cessation of dihydrofolate reductase activity in stationary versus log phase L1210 leukemia cells.
Topics: Animals; Cell Cycle; DNA, Neoplasm; Flow Cytometry; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Thermodynamics; Trimetrexate; Tumor Cells, Cultured | 1991 |
Compartmentation of intracellular folates. Failure to interconvert tetrahydrofolate cofactors to dihydrofolate in mitochondria of L1210 leukemia cells treated with trimetrexate.
Topics: Animals; Cell Compartmentation; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Mitochondria; Quinazolines; Tetrahydrofolates; Trimetrexate; Tumor Cells, Cultured | 1991 |
Interaction between 5-fluorouracil, [6RS]leucovorin, and recombinant human interferon-alpha 2a in cultured colon adenocarcinoma cells.
Topics: Adenocarcinoma; Cell Survival; Colonic Neoplasms; Drug Synergism; Fluorouracil; Folic Acid; Interferon Type I; Leucovorin; Quinazolines; Recombinant Proteins; Thymidylate Synthase; Tumor Cells, Cultured | 1991 |
Folate analogues. 35. Synthesis and biological evaluation of 1-deaza, 3-deaza, and bridge-elongated analogues of N10-propargyl-5,8-dideazafolic acid.
Topics: Biological Transport; Folic Acid; Humans; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 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 |
The pharmacokinetics of the quinazoline antifolate ICI D 1694 in mice and rats.
Topics: Animals; Antineoplastic Agents; Blood Proteins; Chromatography, High Pressure Liquid; Female; Folic Acid; Folic Acid Antagonists; Male; Mice; Mice, Inbred C57BL; Mice, Inbred DBA; Protein Binding; Quinazolines; Rats; Rats, Inbred Strains; Thiophenes; Time Factors; Tissue Distribution | 1991 |
The renal effects of N10-propargyl-5,8-dideazafolic acid (CB3717) and a non-nephrotoxic analogue ICI D1694, in mice.
Topics: Animals; Carbon Radioisotopes; Cisplatin; Creatinine; Female; Folic Acid; Glomerular Filtration Rate; Inulin; Kidney; Kidney Diseases; Male; Mice; Mice, Inbred BALB C; Mice, Inbred DBA; Quinazolines; Thiophenes; Thymidylate Synthase; Urea | 1991 |
Quinazoline antifolates inhibiting thymidylate synthase: 4-thio-substituted analogues.
Topics: Animals; Cell Division; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1991 |
Mechanism of cell death following thymidylate synthase inhibition: 2'-deoxyuridine-5'-triphosphate accumulation, DNA damage, and growth inhibition following exposure to CB3717 and dipyridamole.
Topics: Cell Division; Cell Survival; Deoxyuracil Nucleotides; Dipyridamole; DNA Damage; Drug Synergism; Folic Acid; Humans; Lung Neoplasms; Quinazolines; Thymidine; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured | 1991 |
Quinazoline folate analogs inhibit the catalytic activity of thymidylate synthase but allow binding of 5-fluorodeoxyuridylate.
Topics: Animals; Binding Sites; Cytidine Monophosphate; Floxuridine; Fluorodeoxyuridylate; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Mice; Models, Structural; Protein Binding; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
Role of substrate depletion in the inhibition of thymidylate biosynthesis by the dihydrofolate reductase inhibitor trimetrexate in cultured hepatoma cells.
Topics: Carcinoma, Hepatocellular; Folic Acid; Liver Neoplasms; Pteroylpolyglutamic Acids; Quinazolines; Thymidine Monophosphate; Thymidylate Synthase; Thymine Nucleotides; Trimetrexate; Tumor Cells, Cultured | 1990 |
Crystal structure of Escherichia coli thymidylate synthase containing bound 5-fluoro-2'-deoxyuridylate and 10-propargyl-5,8-dideazafolate.
Topics: Amino Acid Sequence; Binding Sites; Deoxyuracil Nucleotides; Escherichia coli; Fluorodeoxyuridylate; Folic Acid; Folic Acid Antagonists; Ligands; Models, Molecular; Molecular Sequence Data; Protein Binding; Protein Conformation; Quinazolines; Thymidylate Synthase | 1990 |
Structure, multiple site binding, and segmental accommodation in thymidylate synthase on binding dUMP and an anti-folate.
Topics: Binding Sites; Crystallization; Deoxyuracil Nucleotides; Escherichia coli; Folic Acid; Folic Acid Antagonists; Models, Molecular; Molecular Conformation; Quinazolines; Thymidylate Synthase | 1990 |
Pairwise specificity and sequential binding in enzyme catalysis: thymidylate synthase.
Topics: Binding Sites; Deoxyuracil Nucleotides; Escherichia coli; Folic Acid; Models, Chemical; Models, Molecular; Molecular Conformation; Quinazolines; Stereoisomerism; Substrate Specificity; Thymidylate Synthase | 1990 |
Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C2 position.
Topics: Animals; Antineoplastic Agents; Cell Division; Chemical Phenomena; Chemistry; Chemistry, Physical; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Liver; Mice; Molecular Structure; Quinazolines; Rats; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
Quinazoline antifolate thymidylate synthase inhibitors: 2'-fluoro-N10-propargyl-5,8-dideazafolic acid and derivatives with modifications in the C2 position.
Topics: Animals; Antineoplastic Agents; Cell Division; Chemical Phenomena; Chemistry; Drug Resistance; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1990 |
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 |
Serial serum AFP heterogeneity changes in patients with hepatocellular carcinoma during chemotherapy.
Topics: alpha-Fetoproteins; Carcinoma, Hepatocellular; Concanavalin A; Folic Acid; Humans; Liver Neoplasms; Quinazolines | 1986 |
Serum vitamin B12 levels in patients with primary hepatocellular carcinoma during treatment with CB3717.
Topics: Adult; Aged; alpha-Fetoproteins; Carcinoma, Hepatocellular; Female; Folic Acid; Follow-Up Studies; Humans; L-Lactate Dehydrogenase; Liver Cirrhosis; Liver Neoplasms; Male; Middle Aged; Quinazolines; Vitamin B 12 | 1987 |
Induction of remission in hepatocellular carcinoma with a new thymidylate synthase inhibitor, CB3717. A phase II study.
Topics: Adult; Aged; alpha-Fetoproteins; Carcinoma, Hepatocellular; Drug Evaluation; Female; Folic Acid; Follow-Up Studies; Humans; Liver Neoplasms; Male; Middle Aged; Quinazolines; Remission Induction | 1987 |
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 |
Development of an assay for the estimation of N10-propargyl-5,8-dideazafolic acid polyglutamates in tumor cells.
Topics: Animals; Chromatography, High Pressure Liquid; Folic Acid; Leukemia L1210; Mice; Neoplasms; Peptides; Polyglutamic Acid; Quinazolines; Thymidylate Synthase | 1988 |
Formation and retention and biological activity of N10-propargyl-5,8-dideazafolic acid (CB3717) polyglutamates in L1210 cells in vitro.
Topics: Animals; Biotransformation; Chromatography, High Pressure Liquid; Folic Acid; Leukemia L1210; Mice; Peptides; Polyglutamic Acid; Quinazolines; Thymidylate Synthase; Time Factors | 1988 |
Inhibition of glycinamide ribonucleotide formyltransferase and other folate enzymes by homofolate polyglutamates in human lymphoma and murine leukemia cell extracts.
Topics: Acyltransferases; Animals; Folic Acid; Humans; Hydroxymethyl and Formyl Transferases; Kinetics; Leukemia L1210; Lymphoma; Mice; Molecular Conformation; Phosphoribosylaminoimidazolecarboxamide Formyltransferase; Phosphoribosylglycinamide Formyltransferase; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Trimetrexate | 1989 |
The role of cellular folates in the enhancement of activity of the thymidylate synthase inhibitor 10-propargyl-5,8-dideazafolate against hepatoma cells in vitro by inhibitors of dihydrofolate reductase.
Topics: Animals; Antineoplastic Agents; Cell Division; Cell Line; Folic Acid; Folic Acid Antagonists; Kinetics; Liver Neoplasms, Experimental; Pyrimethamine; Quinazolines; Rats; Thymidylate Synthase; Trimetrexate | 1989 |
Characterization of de novo folate synthesis in Pneumocystis carinii and Toxoplasma gondii: potential for screening therapeutic agents.
Topics: 4-Aminobenzoic Acid; Animals; Drug Combinations; Drug Evaluation, Preclinical; Folic Acid; Pneumocystis; Quinazolines; Rats; Sulfamethoxazole; Toxoplasma; Trimethoprim; Trimethoprim, Sulfamethoxazole Drug Combination; Trimetrexate | 1989 |
Activity of thymidylate synthetase and its inhibition by 5-fluorouracil in highly enzyme-overproducing cells resistant to 10-propargyl-5,8-dideazafolate.
Topics: Animals; Blotting, Southern; Drug Resistance; Floxuridine; Fluorouracil; Folic Acid; Gene Amplification; Mice; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1989 |
Enhancement of trimetrexate cytotoxicity in vitro and in vivo by carboxypeptidase G2.
Topics: Animals; Cell Line; Cell Survival; Clone Cells; Cysteine Endopeptidases; Drug Resistance; Drug Synergism; Folic Acid; gamma-Glutamyl Hydrolase; Humans; Leukemia L1210; Mice; Mice, Inbred Strains; Quinazolines; Trimetrexate; Tumor Stem Cell Assay | 1989 |
Folate-pool interconversions and inhibition of biosynthetic processes after exposure of L1210 leukemia cells to antifolates. Experimental and network thermodynamic analyses of the role of dihydrofolate polyglutamylates in antifolate action in cells.
Topics: Animals; Computer Simulation; Deoxyuridine; Floxuridine; Folic Acid; Folic Acid Antagonists; Formates; Leukemia L1210; Methotrexate; Mice; Purines; Pyrimidines; Quinazolines; Tetrahydrofolates; Thermodynamics; Thymidylate Synthase; Trimetrexate | 1989 |
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 |
Estimation of the in vitro and in vivo inhibitory effects of antifolates upon thymidylate synthase (TS) in whole cells.
Topics: Animals; Dose-Response Relationship, Drug; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Mice, Inbred DBA; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Time Factors; Tumor Cells, Cultured | 1989 |
The enhancement of the activity of 10-propargyl-5,8-dideazafolate and 5,10-dideazatetrahydrofolate by inhibitors of dihydrofolate reductase.
Topics: Animals; Cell Line; Cell Survival; Folic Acid; Folic Acid Antagonists; Hypoxanthine; Hypoxanthines; Liver Neoplasms, Experimental; Quinazolines; Rats; Tetrahydrofolates; Thymidine; Tumor Cells, Cultured | 1989 |
Thymidylate synthase: a target for anticancer drug design.
Topics: Animals; Antimetabolites, Antineoplastic; Drug Design; Folic Acid; Kidney; Liver; Male; Mice; Mice, Inbred DBA; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1989 |
Crystal structure of Escherichia coli thymidylate synthase with FdUMP and 10-propargyl-5,8-dideazafolate.
Topics: Deoxyuracil Nucleotides; Escherichia coli; Fluorodeoxyuridylate; Folic Acid; Folic Acid Antagonists; Kinetics; Models, Molecular; Protein Binding; Protein Conformation; Quinazolines; Structure-Activity Relationship; Substrate Specificity; Thymidylate Synthase; X-Ray Diffraction | 1989 |
Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency.
Topics: Animals; Antineoplastic Agents; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Hydrogen Bonding; Leukemia L1210; Liver; Quinazolines; Rats; Solubility; Structure-Activity Relationship; Thymidylate Synthase | 1989 |
Comparison of the biological effects of selected 5,8-dideazafolate analogues with their 2-desamino counterparts.
Topics: Animals; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Humans; Leukemia L1210; Methotrexate; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1989 |
The quantitation by radioimmunoassay of 2'-deoxyuridine 5'-triphosphate in extracts of thymidylate synthase-inhibited cells.
Topics: Antineoplastic Agents; Cell Line; Cross Reactions; Deoxyuracil Nucleotides; Folic Acid; Humans; Immune Sera; Lung Neoplasms; Quinazolines; Radioimmunoassay; Thymidylate Synthase; Tumor Cells, Cultured | 1989 |
Modulation of dipyridamole action by alpha 1 acid glycoprotein. Reduced potentiation of quinazoline antifolate (CB3717) cytotoxicity by dipyridamole.
Topics: Biological Transport; Cell Division; Dipyridamole; Drug Synergism; Folic Acid; Folic Acid Antagonists; Humans; Nucleosides; Orosomucoid; Quinazolines; Thymidine; Tumor Cells, Cultured | 1989 |
Intestinal alkaline phosphatase isoenzyme in patients with primary liver cancer during treatment with N10-propargyl 5, 8-dideazafolic acid (CB 3717).
Topics: Adult; Aged; Alkaline Phosphatase; Aspartate Aminotransferases; Female; Folic Acid; gamma-Glutamyltransferase; Humans; Intestinal Mucosa; Isoenzymes; Liver Neoplasms; Male; Middle Aged; Quinazolines; Time Factors | 1988 |
Quinazoline antifolates inhibiting thymidylate synthase: synthesis of four oligo(L-gamma-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition.
Topics: Cell Line; Chemical Phenomena; Chemistry; Folic Acid; Humans; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1989 |
Increased thymidylate synthase in L1210 cells possessing acquired resistance to N10-propargyl-5,8-dideazafolic acid (CB3717): development, characterization, and cross-resistance studies.
Topics: Animals; Antineoplastic Agents; Cells, Cultured; Deoxyuridine; Drug Resistance; Floxuridine; Fluorouracil; Folic Acid; Folic Acid Antagonists; Hypoxanthine; Hypoxanthines; Kinetics; Leukemia L1210; Mice; Quinazolines; Thymidylate Synthase; Tritium | 1986 |
Folate 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 |
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 |
Antifolate drug interactions: enhancement of growth inhibition due to the antipurine 5,10-dideazatetrahydrofolic acid by the lipophilic dihydrofolate reductase inhibitors metoprine and trimetrexate.
Topics: Acyltransferases; Animals; Drug Synergism; Folic Acid; Folic Acid Antagonists; Hydroxymethyl and Formyl Transferases; Liver Neoplasms, Experimental; Phosphoribosylglycinamide Formyltransferase; Pyrimethamine; Quinazolines; Tetrahydrofolates; Thymidine Monophosphate; Trimetrexate; Tumor Cells, Cultured | 1988 |
Inhibition of the growth of human hepatocellular carcinoma in vitro and in athymic mice by a quinazoline inhibitor of thymidylate synthase, CB3717.
Topics: Animals; Antineoplastic Agents; Carcinoma, Hepatocellular; Deoxyuridine; Dose-Response Relationship, Drug; Folic Acid; Humans; In Vitro Techniques; Liver Neoplasms; Mice; Mice, Nude; Neoplasm Transplantation; Quinazolines; Thymidine | 1986 |
A pleomorphic hepatocellular carcinoma with biochemical features of fibrolamellar hepatocellular carcinoma.
Topics: Adult; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Hepatocellular; Combined Modality Therapy; Doxorubicin; Etoposide; Female; Folic Acid; Humans; Liver Neoplasms; Neurotensin; Quinazolines; Vitamin B 12 | 1986 |
Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).
Topics: Animals; Chemical Phenomena; Chemistry; Folic Acid; Folic Acid Antagonists; Lacticaseibacillus casei; Leukemia L1210; Quinazolines; Streptococcus; Structure-Activity Relationship; Thymidylate Synthase | 1986 |
Moderate antiproliferative effect of the antifolate CB3717 in the BN myeloid leukaemia model.
Topics: Animals; Antineoplastic Agents; Deoxyuridine; DNA; Fluorouracil; Folic Acid; Folic Acid Antagonists; Leukemia, Myeloid, Acute; Quinazolines; Rats; Thymidine Monophosphate; Thymidylate Synthase | 1988 |
The efficacy of 5-fluorouracil in human colorectal cancer is not enhanced by thymidylate synthetase inhibition with CB3717 (N10-propargyl-5,8 dideazafolic acid).
Topics: Adenocarcinoma; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Colonic Neoplasms; Fluorouracil; Folic Acid; Humans; Middle Aged; Quinazolines; Rectal Neoplasms; Thymidylate Synthase | 1988 |
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 |
Properties of a defined mutant of Escherichia coli thymidylate synthase.
Topics: Amino Acids; Cysteine; Escherichia coli; Fluorodeoxyuridylate; Folic Acid; Mutation; Peptide Mapping; Quinazolines; Structure-Activity Relationship; Tetrahydrofolates; Thymidylate Synthase; Tyrosine | 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 |
A phase I evaluation of N10-propargyl-5,8-dideazafolic acid.
Topics: Adult; Aged; Dose-Response Relationship, Drug; Drug Evaluation; Folic Acid; Humans; Middle Aged; Neoplasms; Quinazolines | 1988 |
Potentiation of quinazoline antifolate (CB3717) toxicity by dipyridamole in human lung carcinoma, A549, cells.
Topics: Carcinoma; Cell Survival; Dipyridamole; DNA; Drug Synergism; Folic Acid; Folic Acid Antagonists; Humans; Lung Neoplasms; Quinazolines; Thymidine; Thymidylate Synthase; Tumor Cells, Cultured | 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 |
Phase II study of the antifolate N10-propargyl-5,8-dideazafolic acid (CB 3717) in advanced breast cancer.
Topics: Acute Kidney Injury; Adult; Aged; Antineoplastic Agents; Breast Neoplasms; Chemical and Drug Induced Liver Injury; Drug Evaluation; Female; Folic Acid; Folic Acid Antagonists; Humans; Middle Aged; Quinazolines; Thymidylate Synthase | 1988 |
Phase I study of the antifolate N10-propargyl-5,8-dideazafolic acid, CB 3717.
Topics: Adult; Aged; Alanine Transaminase; Antineoplastic Agents; Aspartate Aminotransferases; Creatinine; Drug Evaluation; Fatigue; Female; Folic Acid; Folic Acid Antagonists; Humans; Male; Middle Aged; Neoplasms; Quinazolines; Thymidylate Synthase | 1988 |
Phase II study of the thymidylate synthetase inhibitor CB3717 (N10-propargyl-5,8-dideazafolic acid) in colorectal cancer.
Topics: Adult; Aged; Antineoplastic Agents; Colonic Neoplasms; Drug Evaluation; Female; Folic Acid; Humans; Male; Middle Aged; Quinazolines; Rectal Neoplasms | 1988 |
Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB 3717).
Topics: Adult; Aged; Chemical and Drug Induced Liver Injury; Diuresis; Drug Evaluation; Folic Acid; Folic Acid Antagonists; Humans; Hydrogen-Ion Concentration; Kidney Diseases; Middle Aged; Quinazolines; Thymidylate Synthase | 1987 |
Analysis of thymidylate synthase gene amplification and of mRNA levels in the cell cycle.
Topics: Animals; Cell Cycle; Cell Line; DNA; Folic Acid; Folic Acid Antagonists; Gene Amplification; Leukemia L1210; Mice; Nucleic Acid Hybridization; Quinazolines; RNA, Messenger; Tetrahydrofolate Dehydrogenase; Thymidylate Synthase | 1987 |
A stable binary complex between Leishmania major thymidylate synthase and the substrate deoxyuridylate. A slow-binding interaction.
Topics: Animals; Binding, Competitive; Deoxyuracil Nucleotides; Fluorodeoxyuridylate; Folic Acid; Kinetics; Leishmania tropica; Quinazolines; Thymidine Monophosphate; Thymidylate Synthase | 1987 |
Folate analogues. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds.
Topics: Folic Acid; Folic Acid Antagonists; Quinazolines; Structure-Activity Relationship; Tetrahydrofolates; Thymidylate Synthase | 1987 |
Pharmacokinetics of the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB3717) in the mouse.
Topics: Animals; Cecum; Chromatography, High Pressure Liquid; Feces; Folic Acid; Kinetics; Male; Mass Spectrometry; Mice; Mice, Inbred C57BL; Protein Binding; Quinazolines; Scintillation Counting; Thymidylate Synthase; Tissue Distribution | 1986 |
A phase I evaluation of the quinazoline antifolate thymidylate synthase inhibitor, N10-propargyl-5,8-dideazafolic acid, CB3717.
Topics: Acetylglucosaminidase; Acid Phosphatase; Alanine Transaminase; Antineoplastic Agents; Chemical and Drug Induced Liver Injury; Dose-Response Relationship, Drug; Drug Administration Schedule; Drug Evaluation; Folic Acid; Folic Acid Antagonists; Glomerular Filtration Rate; Hematologic Diseases; Hyperbilirubinemia; Kidney Diseases; Leucyl Aminopeptidase; Neoplasms; Quinazolines; Skin Diseases; Thymidylate Synthase | 1986 |
Quinazoline antifolates inhibiting thymidylate synthase: benzoyl ring modifications.
Topics: Folic Acid; Folic Acid Antagonists; Quinazolines; Spectrophotometry, Ultraviolet; Structure-Activity Relationship; Thymidylate Synthase | 1986 |
Kinetics and mechanism of interaction of 10-propargyl-5,8-dideazafolate with thymidylate synthase.
Topics: Antineoplastic Agents; Carbon Radioisotopes; Deoxyuracil Nucleotides; Folic Acid; Kinetics; Leukemia, Experimental; Protein Denaturation; Quinazolines; Spectrophotometry, Ultraviolet; Thymidylate Synthase; Tritium | 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 |
The clinical pharmacokinetics of the novel antifolate N10-propargyl-5,8-dideazafolic acid (CB 3717).
Topics: Antineoplastic Agents; Folic Acid; Folic Acid Antagonists; Humans; Kinetics; Liver; Protein Binding; Quinazolines; Tissue Distribution | 1985 |
Selection and properties of Leishmania tropica resistant to 10-propargyl-5,8-dideazafolate, an inhibitor of thymidylate synthetase.
Topics: Animals; Drug Resistance; Folic Acid; Folic Acid Antagonists; Gene Amplification; Leishmania tropica; Quinazolines; Tetrahydrofolate Dehydrogenase | 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 |
Assignment of the carbon-13 nuclear magnetic resonance spectrum of folic acid.
Topics: Aminobenzoates; Benzamides; Carbon Isotopes; Chemical Phenomena; Chemistry; Deuterium; Folic Acid; Glutamates; Magnetic Resonance Spectroscopy; Protons; Pteridines; Purines; Quinazolines; Quinoxalines; Ribonucleosides | 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 |
Antimalarial activity of 2,4-diamino-6-[(3,4-dichlorobenzyl) nitros-amino] quinazoline (CI-679 base) and CI-679 acetate. Laboratory studies in mice and rhesus monkeys.
Topics: Acetates; Aminobenzoates; Animals; Antimalarials; Dapsone; Drug Synergism; Female; Folic Acid; Haplorhini; Hydrocarbons, Halogenated; Male; Mice; Nitrosamines; Plasmodium; Quinazolines | 1970 |
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 analogues of folic acid.
Topics: Folic Acid; Folic Acid Antagonists; Models, Chemical; Quinazolines | 1970 |
2,4-diamino-5, 6,7,8-tetrahydroquinazoline, a new pteridine antagonist.
Topics: Animals; Depression, Chemical; Eukaryota; Folic Acid; Growth; Pteridines; Pterins; Quinazolines; Thymidine; Thymine | 1969 |
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 |
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 |
Spectroscopic studies of ternary complexes of thymidylate synthetase, deoxyribonucleotides, and folate analogs.
Topics: Deoxyribonucleotides; Floxuridine; Folic Acid; Methyltransferases; Protein Conformation; Pteroylpolyglutamic Acids; Quinazolines; Spectrophotometry; Thymidine Monophosphate; Thymidylate Synthase; Uridine Monophosphate | 1984 |
Biochemical pharmacology of the lipophilic antifolate, trimetrexate.
Topics: Animals; Cell Line; Culture Techniques; Deoxyuridine; Drug Resistance; Folic Acid; Folic Acid Antagonists; Humans; Kinetics; Leucovorin; Leukemia L1210; Lymphocytes; Methotrexate; Mice; Mice, Inbred Strains; Quinazolines; Ribonucleotides; Thymidine; Trimetrexate | 1984 |
Modulation of anti-metabolite effects. Effects of thymidine on the efficacy of the quinazoline-based thymidylate synthetase inhibitor, CB3717.
Topics: Animals; Antimetabolites, Antineoplastic; Cells, Cultured; Deoxyuridine; Folic Acid; Leukemia L1210; Male; Methyltransferases; Mice; Mice, Inbred DBA; Quinazolines; Thymidine; Thymidylate Synthase | 1984 |
Improved synthetic routes to 5,8-dideazapteroylglutamates amenable to the formation of poly-gamma-L-glutamyl derivatives.
Topics: Cell Line; Cell Survival; Chromatography, High Pressure Liquid; Colonic Neoplasms; Drug Evaluation, Preclinical; Folic Acid; Humans; Indicators and Reagents; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship | 1983 |
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 |
Inhibition of thymidylate synthetase by the new quinazoline antifolate, CB 3717; enzyme purification and kinetics.
Topics: Animals; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Methyltransferases; Mice; Quinazolines; Thymidylate Synthase | 1984 |
Plasma nucleoside and base levels following treatment with the new thymidylate synthetase inhibitor CB 3717.
Topics: Animals; Folic Acid; Folic Acid Antagonists; Kinetics; Leukemia L1210; Methyltransferases; Mice; Mice, Inbred Strains; Nucleosides; Purines; Pyrimidines; Quinazolines; Thymidylate Synthase | 1984 |
Quinazoline CB 3717 and CB 3703 inhibition of folate retention and metabolism in Ehrlich ascites carcinoma cells and some organs of the host-mouse.
Topics: Animals; Carcinoma, Ehrlich Tumor; Female; Folic Acid; Folic Acid Antagonists; Kidney; Liver; Mice; Quinazolines | 1984 |
A quinazoline antifolate as inhibitor of folate metabolism in mouse L-cells.
Topics: Animals; Folic Acid; Folic Acid Antagonists; Glutamates; L Cells; Lethal Dose 50; Mice; Quinazolines | 1983 |
A potent antitumour quinazoline inhibitor of thymidylate synthetase: synthesis, biological properties and therapeutic results in mice.
Topics: Animals; Antineoplastic Agents; Cell Survival; Cells, Cultured; Dose-Response Relationship, Drug; Female; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Methyltransferases; Mice; Mice, Inbred C57BL; Quinazolines; Thymidylate Synthase | 1981 |
Quinazoline antifolates with dual biochemical loci of action. Biochemical and biological studies directed towards overcoming methotrexate resistance.
Topics: Animals; Cell Survival; Female; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Methotrexate; Mice; Quinazolines; Thymidylate Synthase | 1980 |
Quinazoline thymidylate synthase inhibitors: methods for assessing the contribution of polyglutamation to their in vitro activity.
Topics: Animals; Biological Transport; Cell Division; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Leucovorin; Leukemia L1210; Methotrexate; Peptide Synthases; Polyglutamic Acid; Pteroylpolyglutamic Acids; Quinazolines; Structure-Activity Relationship; Substrate Specificity; Thymidylate Synthase | 1995 |
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 |
Molecular characterisation of two cell lines selected for resistance to the folate-based thymidylate synthase inhibitor, ZD1694.
Topics: Antineoplastic Agents; Base Sequence; Blotting, Southern; Blotting, Western; DNA; DNA, Neoplasm; Drug Resistance; Female; Folic Acid; Humans; Lymphocytes; Molecular Sequence Data; Neoplasm Proteins; Ovarian Neoplasms; Polymerase Chain Reaction; Proteins; Quinazolines; RNA; RNA, Neoplasm; Thiophenes; Thymidylate Synthase; Transcription, Genetic; 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 |
Relationships between resistance to cisplatin and antifolates in sensitive and resistant tumour cell lines.
Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cisplatin; Drug Resistance; Female; Folic Acid; Folic Acid Antagonists; Humans; Male; Ovarian Neoplasms; Quinazolines; Testicular Neoplasms; Thiophenes; Tumor Cells, Cultured; Uterine Cervical Neoplasms | 1995 |
Quinazoline antifolate thymidylate synthase inhibitors: replacement of glutamic acid in the C2-methyl series.
Topics: Animals; Antineoplastic Agents; Folic Acid; Folic Acid Antagonists; Glutamic Acid; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1995 |
5,10-Dideazatetrahydrofolic acid reduces toxicity and deoxyadenosine triphosphate pool, expansion in cultured L1210 cells treated with inhibitors of thymidylate synthase.
Topics: Animals; Cell Survival; Deoxyadenine Nucleotides; Drug Interactions; Floxuridine; Folic Acid; Hypoxanthine; Hypoxanthines; Leukemia L1210; Quinazolines; Tetrahydrofolates; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1995 |
Promotion of purine nucleotide binding to thymidylate synthase by a potent folate analogue inhibitor, 1843U89.
Topics: Circular Dichroism; Crystallography, X-Ray; Escherichia coli; Folic Acid; Hydrogen Bonding; Indoles; Isoindoles; Models, Molecular; Molecular Sequence Data; Purine Nucleotides; Quinazolines; Recombinant Proteins; Thymidylate Synthase | 1995 |
Arginine and ornithine metabolizing enzymes in testosterone-induced hypertrophic mouse kidney.
Topics: Animals; Arginase; Arginine; Eflornithine; Enzyme Induction; Female; Folic Acid; Hypertrophy; Kidney; Male; Mice; Mice, Inbred Strains; Ornithine; Ornithine Decarboxylase; Ornithine-Oxo-Acid Transaminase; Putrescine; Quinazolines; Sex Factors; Testosterone | 1995 |
New therapeutic strategies for patients with gastrointestinal malignancies using biochemical modulation of fluorouracil.
Topics: Adenocarcinoma; Antineoplastic Combined Chemotherapy Protocols; Biomarkers; Colonic Neoplasms; Fatal Outcome; Fluorouracil; Folic Acid; Folic Acid Antagonists; Gastrointestinal Neoplasms; Gene Expression Regulation, Enzymologic; Humans; Interferon-alpha; Leucovorin; Liver Neoplasms; Male; Middle Aged; Prognosis; Quinazolines; RNA, Messenger; RNA, Neoplasm; Thymidylate Synthase | 1995 |
Biochemical effects of folate-based inhibitors of thymidylate synthase in MGH-U1 cells.
Topics: Cell Survival; Deoxyuracil Nucleotides; Deoxyuridine; Folic Acid; Folic Acid Antagonists; Glutamates; Humans; In Vitro Techniques; Indoles; Isoindoles; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured; Urinary Bladder Neoplasms | 1994 |
Phosphorus-31 nuclear magnetic resonance studies of complexes of thymidylate synthase.
Topics: Deoxyuracil Nucleotides; Fluorodeoxyuridylate; Folic Acid; Magnetic Resonance Spectroscopy; Phosphorus Isotopes; Quinazolines; Tetrahydrofolates; Thymidine Monophosphate; Thymidylate Synthase | 1994 |
Comparative cytotoxicity of folate-based inhibitors of thymidylate synthase and 5-fluorouracil +/- leucovorin in MGH-U1 cells.
Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cell Survival; Drug Screening Assays, Antitumor; Fluorouracil; Folic Acid; Glutamates; Humans; Indoles; Isoindoles; Leucovorin; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured; Urinary Bladder Neoplasms | 1994 |
The history of the development and clinical use of CB 3717 and ICI D1694.
Topics: Animals; Antimetabolites, Antineoplastic; Clinical Trials, Phase I as Topic; Folic Acid; History, 20th Century; Molecular Structure; Quinazolines; Thiophenes; Thymidylate Synthase; United Kingdom | 1993 |
Re: "Oncology drug discovery and clinical trial testing: who's listening?".
Topics: Animals; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Folic Acid; Humans; Kidney; Mice; Neoplasms; Quinazolines; Thymidylate Synthase | 1994 |
Mode of binding of folate analogs to thymidylate synthase. Evidence for two asymmetric but interactive substrate binding sites.
Topics: Binding Sites; Carbon Radioisotopes; Deoxyuracil Nucleotides; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Isoindoles; Kinetics; Macromolecular Substances; Mathematics; Protein Binding; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1994 |
Gamma-linked dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8- dideazafolate as antitumour agents.
Topics: Animals; Antineoplastic Agents; Dipeptides; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase | 1993 |
Substituted-2-desamino-2-methyl-quinazolinones. A series of novel antitumour agents.
Topics: Animals; Antineoplastic Agents; Cell Division; Drug Screening Assays, Antitumor; Folic Acid; Leukemia L1210; Mice; Molecular Structure; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
Use of murine L5178Y lymphoma thymidine kinase mutants for in vitro and in vivo antitumour efficacy evaluation of novel thymidylate synthase inhibitors.
Topics: Animals; Antineoplastic Agents; Cell Survival; Drug Screening Assays, Antitumor; Folic Acid; Folic Acid Antagonists; Leukemia L5178; Mice; Mice, Inbred DBA; Mutation; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
Quinazoline antifolates inhibiting thymidylate synthase: synthesis of gamma-linked peptide and amide analogues of 2-desamino-2-methyl-N10-propargyl- 5,8-dideazafolic acid (ICI 198583).
Topics: Animals; Cell Division; Drug Screening Assays, Antitumor; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Molecular Structure; Peptides; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1993 |
The duration of the inhibition of thymidylate synthase in intact L1210 cells exposed to two different classes of quinazoline analogues.
Topics: Animals; Antineoplastic Agents; Cell Division; Deoxyuracil Nucleotides; Drug Screening Assays, Antitumor; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Mice; Quinazolines; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Thymine Nucleotides | 1993 |
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 |
bcl-2 modulation of apoptosis induced by anticancer drugs: resistance to thymidylate stress is independent of classical resistance pathways.
Topics: Apoptosis; Burkitt Lymphoma; DNA Damage; DNA, Neoplasm; Drug Resistance; Floxuridine; Folic Acid; Humans; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-bcl-2; Quinazolines; Thymidylate Synthase; Transfection; Tumor Cells, Cultured | 1993 |
Polyamines in testosterone-induced hypertrophic and antifolate-induced hyperplastic mouse kidney. Differential effect of alpha-difluoromethylornithine.
Topics: Animals; Eflornithine; Female; Folic Acid; Hyperplasia; Hypertrophy; Kidney; Kidney Diseases; Mice; Organ Size; Ornithine Decarboxylase Inhibitors; Polyamines; Quinazolines; Testosterone | 1993 |
The toxicity of antifolates in Babesia bovis.
Topics: Animals; Babesia bovis; Folic Acid; Folic Acid Antagonists; Pyrimethamine; Pyrimidines; Quinazolines; Trimethoprim; Trimetrexate | 1993 |
Fluorine-19 nuclear magnetic resonance studies of binary and ternary complexes of thymidylate synthase utilizing a fluorine-labeled folate analogue.
Topics: Fluorine; Fluorodeoxyuridylate; Folic Acid; Lacticaseibacillus casei; Macromolecular Substances; Magnetic Resonance Spectroscopy; Protein Binding; Protein Conformation; Protein Denaturation; Quinazolines; 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 |
Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones.
Topics: Crystallography; Drug Design; Escherichia coli; Folic Acid; Humans; Pyridines; Quinazolines; Structure-Activity Relationship; Thymidylate Synthase | 1993 |
Enhanced antitumor activity for the thymidylate synthase inhibitor 1843U89 through decreased host toxicity with oral folic acid.
Topics: Animals; Body Weight; Dogs; Dose-Response Relationship, Drug; Enzyme Inhibitors; Folic Acid; Humans; Indoles; Intestinal Diseases; Isoindoles; Leucovorin; Mice; Neoplasms, Experimental; Osteosarcoma; Quinazolines; Thymidylate Synthase; Tumor Cells, Cultured | 1995 |
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 |
Quinazoline antifolate thymidylate synthase inhibitors: gamma-linked L-D, D-D, and D-L dipeptide analogues of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583).
Topics: Animals; Antineoplastic Agents; Cell Division; Dipeptides; Folic Acid; Folic Acid Antagonists; Leukemia L1210; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Molecular Structure; Quinazolines; Stereoisomerism; Structure-Activity Relationship; Thymidylate Synthase; Tumor Cells, Cultured | 1996 |
Entropy in bi-substrate enzymes: proposed role of an alternate site in chaperoning substrate into, and products out of, thymidylate synthase.
Topics: Binding Sites; Crystallography, X-Ray; Deoxyuracil Nucleotides; Folic Acid; Lacticaseibacillus casei; Models, Molecular; Protein Conformation; Quinazolines; Tetrahydrofolates; Thermodynamics; Thymidylate Synthase | 1996 |
Cellular pharmacokinetics of ZD1694 in cultured human leukaemia cells sensitive, or made resistant, to this drug.
Topics: Antimetabolites, Antineoplastic; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Folic Acid; Humans; Intracellular Fluid; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Polyglutamic Acid; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines; Tetrahydrofolate Dehydrogenase; Thiophenes; Thymidylate Synthase; Tritium; 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 |
In vitro uptake, anabolism, and cellular retention of 1843U89 and other benzoquinazoline inhibitors of thymidylate synthase.
Topics: Animals; Carcinoma; Enzyme Inhibitors; Folic Acid; Folic Acid Antagonists; Humans; Indoles; Intestinal Neoplasms; Isoindoles; Leucovorin; Liver; Metabolic Clearance Rate; Peptide Synthases; Polyglutamic Acid; Quinazolines; Swine; Thymidylate Synthase; Tumor Cells, Cultured | 1996 |
Unusual binding stoichiometries and cooperativity are observed during binary and ternary complex formation in the single active pore of R67 dihydrofolate reductase, a D2 symmetric protein.
Topics: Allosteric Regulation; Binding Sites; Calorimetry; Fluorescence Polarization; Folic Acid; Kinetics; Ligands; NADP; Protein Binding; Quinazolines; R Factors; Tetrahydrofolate Dehydrogenase | 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 |
Trichinella spiralis thymidylate synthase: developmental pattern, isolation, molecular properties, and inhibition by substrate and cofactor analogues.
Topics: Animals; Chromatography, Affinity; Enzyme Inhibitors; Fluorodeoxyuridylate; Folic Acid; Gene Expression Regulation, Developmental; Gene Expression Regulation, Enzymologic; Humans; Kinetics; Larva; Liver; Liver Regeneration; Muscles; Quinazolines; Rats; Structure-Activity Relationship; Thiophenes; Thymidylate Synthase; Trichinella spiralis | 1996 |
Binding of the anticancer drug ZD1694 to E. coli thymidylate synthase: assessing specificity and affinity.
Topics: Antimetabolites, Antineoplastic; Binding Sites; Computer Simulation; Crystallography, X-Ray; Escherichia coli; Folic Acid; Folic Acid Antagonists; Humans; Models, Molecular; Molecular Conformation; Protein Conformation; Protein Structure, Secondary; Quinazolines; Species Specificity; Thiophenes; Thymidylate Synthase | 1996 |
An essential role for water in an enzyme reaction mechanism: the crystal structure of the thymidylate synthase mutant E58Q.
Topics: Amino Acid Sequence; Binding Sites; Crystallization; Crystallography, X-Ray; Deoxyuracil Nucleotides; Enzyme Inhibitors; Escherichia coli; Folic Acid; Glutamic Acid; Hydrogen Bonding; Models, Molecular; Mutagenesis, Site-Directed; Point Mutation; Protein Conformation; Quinazolines; Recombinant Proteins; Thymidylate Synthase; Water | 1996 |
Prodrugs of thymidylate synthase inhibitors: potential for antibody directed enzyme prodrug therapy (ADEPT).
Topics: Antineoplastic Agents; Biotransformation; Carboxypeptidases; Carboxypeptidases A; Drug Delivery Systems; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Folic Acid; Humans; Prodrugs; Quinazolines; Thiophenes; Thymidylate Synthase; Tumor Cells, Cultured | 1996 |
Kinetic scheme for thymidylate synthase from Escherichia coli: determination from measurements of ligand binding, primary and secondary isotope effects, and pre-steady-state catalysis.
Topics: Catalysis; Deoxyuracil Nucleotides; Escherichia coli; Folic Acid; Folic Acid Antagonists; Kinetics; Ligands; Molecular Structure; Mutagenesis, Site-Directed; Protein Binding; Protein Conformation; Quinazolines; Spectrometry, Fluorescence; Spectrophotometry; Tetrahydrofolates; Thermodynamics; Thymidine Monophosphate; Thymidylate Synthase | 1997 |
Interference by antifolate drugs in a folate competitive protein-binding assay.
Topics: Folic Acid; Folic Acid Antagonists; Humans; Protein Binding; Quinazolines; Radioimmunoassay; Thiophenes | 1997 |
Use of 10-formyl-5,8-dideazafolate as substrate for rat 10-formyltetrahydrofolate dehydrogenase.
Topics: Acyltransferases; Animals; Folic Acid; Hydrolysis; Hydroxymethyl and Formyl Transferases; Leucovorin; Molecular Structure; NADP; Oxidoreductases Acting on CH-NH Group Donors; Phosphoribosylglycinamide Formyltransferase; Quinazolines; Rats; Spectrophotometry; Stereoisomerism | 1997 |
Inhibitors of cyclic nucleotide phosphodiesterase isozymes block renal tubular cell proliferation induced by folic acid.
Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Cell Division; Cilostazol; Cyclic AMP; Cyclic AMP-Dependent Protein Kinases; Cyclic Nucleotide Phosphodiesterases, Type 3; Down-Regulation; Folic Acid; Isoenzymes; Kidney Tubules; Male; Phosphodiesterase Inhibitors; Proliferating Cell Nuclear Antigen; Pyrrolidinones; Quinazolines; Quinolones; Rats; Rats, Sprague-Dawley; Rolipram; Signal Transduction; Tetrazoles | 1997 |
Crystal structures of a marginally active thymidylate synthase mutant, Arg 126-->Glu.
Topics: Antineoplastic Agents; Arginine; Binding Sites; Catalysis; Crystallization; Crystallography, X-Ray; Deoxyuracil Nucleotides; Dimerization; Folic Acid; Folic Acid Antagonists; Glutamic Acid; Hydrogen Bonding; Kinetics; Models, Molecular; Molecular Structure; Mutation; Phosphates; Quinazolines; 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 |
Mode of action of site-directed irreversible folate analogue inhibitors of thymidylate synthase.
Topics: Amino Acid Sequence; Binding Sites; Cysteine; Enzyme Inhibitors; Escherichia coli; Folic Acid; Glutamic Acid; Kinetics; Molecular Sequence Data; Pyrimidines; Quinazolines; Thymidylate Synthase | 1998 |
Isolation and characterization of thymitaq (AG337) and 5-fluoro-2-deoxyuridylate-resistant mutants of human thymidylate synthase from ethyl methanesulfonate-exposed human sarcoma HT1080 cells.
Topics: Cloning, Molecular; Drug Resistance; Enzyme Inhibitors; Escherichia coli; Ethyl Methanesulfonate; Fluorodeoxyuridylate; Folic Acid; Folic Acid Antagonists; Gene Expression Regulation, Enzymologic; Humans; Kinetics; Mutagenesis; Mutagenesis, Site-Directed; Polymorphism, Single-Stranded Conformational; Quinazolines; Recombinant Proteins; Sarcoma; Thymidylate Synthase; Tumor Cells, Cultured | 1998 |
Quinoxaline chemistry. Part 9. Quinoxaline analogues of trimetrexate (TMQ) and 10-propargyl-5,8-dideazafolic acid (CB 3717) and its precursors. Synthesis and evaluation of in vitro anticancer activity.
Topics: Antineoplastic Agents; Folic Acid; Humans; Quinazolines; Quinoxalines; Structure-Activity Relationship; Trimetrexate; Tumor Cells, Cultured | 1998 |
The separate effects of E60Q in Lactobacillus casei thymidylate synthase delineate between mechanisms for formation of intermediates in catalysis.
Topics: Amino Acid Substitution; Asparagine; Binding Sites; Catalysis; Crystallography, X-Ray; Deoxyuracil Nucleotides; Folic Acid; Glutamic Acid; Glutamine; Lacticaseibacillus casei; Mutation; Nucleotides; Protein Binding; Protein Conformation; Pyrimidines; Quinazolines; Structure-Activity Relationship; Substrate Specificity; Thymidylate Synthase | 1998 |
The additivity of substrate fragments in enzyme-ligand binding.
Topics: Crystallography, X-Ray; Deoxyuracil Nucleotides; Deoxyuridine; Escherichia coli; Folic Acid; Models, Molecular; Mutagenesis, Site-Directed; Phosphates; Protein Conformation; Quinazolines; Recombinant Proteins; Ribose; Structure-Activity Relationship; Thymidylate Synthase; Uridine | 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 |
Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action.
Topics: Animals; Bisbenzimidazole; Bromodeoxyuridine; Cell Cycle; Cell Division; DNA, Neoplasm; Flow Cytometry; Folic Acid; Folic Acid Antagonists; Growth Inhibitors; Humans; Mice; Propidium; Pyridines; Quinazolines; Staining and Labeling; Thymidylate Synthase; Tumor Cells, Cultured | 1998 |
D221 in thymidylate synthase controls conformation change, and thereby opening of the imidazolidine.
Topics: Asparagine; Aspartic Acid; Binding Sites; Crystallography, X-Ray; Escherichia coli; Fluorodeoxyuridylate; Folic Acid; Hydrogen Bonding; Imidazoles; Macromolecular Substances; Models, Molecular; Mutagenesis, Site-Directed; Protein Binding; Protein Conformation; Quinazolines; Substrate Specificity; Tetrahydrofolates; Thymidylate Synthase | 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 |
Probing the folate-binding site of human thymidylate synthase by site-directed mutagenesis. Generation of mutants that confer resistance to raltitrexed, Thymitaq, and BW1843U89.
Topics: Animals; Antimetabolites, Antineoplastic; Binding Sites; Bone Marrow Cells; Drug Resistance; Folic Acid; Folic Acid Antagonists; Granulocytes; Humans; Indoles; Isoindoles; Isoleucine; Kinetics; Macrophages; Mice; Models, Molecular; Mutagenesis, Site-Directed; Quinazolines; Recombinant Proteins; Stem Cells; Thiophenes; Thymidylate Synthase | 1998 |
A novel class of lipophilic quinazoline-based folic acid analogues: cytotoxic agents with a folate-independent locus.
Topics: Animals; Antineoplastic Agents; Cell Cycle; Cell Division; Cell Survival; Chemical Precipitation; Colony-Forming Units Assay; Cytoprotection; DNA, Neoplasm; Folic Acid; Humans; Leukemia L1210; Lipid Metabolism; Mice; Quinazolines; Solubility; Tumor Cells, Cultured | 1999 |
Catecholamines participate in the induction of ornithine decarboxylase gene expression in normal and hyperplastic mouse kidney.
Topics: Animals; Catecholamines; Female; Folic Acid; Folic Acid Antagonists; Gene Expression; Hyperplasia; Kidney; Mice; Organ Size; Ornithine Decarboxylase; Quinazolines; Receptors, Catecholamine; Reserpine; RNA, Messenger | 1999 |
Potentiation of the cytotoxicity of thymidylate synthase (TS) inhibitors by dipyridamole analogues with reduced alpha1-acid glycoprotein binding.
Topics: Animals; Antineoplastic Agents; Biological Transport; Cell Division; Cell Survival; Dipyridamole; Drug Synergism; Enzyme Inhibitors; Folic Acid; Leukemia L1210; Mice; Molecular Structure; Orosomucoid; Protein Binding; Quinazolines; Structure-Activity Relationship; Thymidine; Thymidylate Synthase; Tumor Cells, Cultured | 1999 |
The structural mechanism for half-the-sites reactivity in an enzyme, thymidylate synthase, involves a relay of changes between subunits.
Topics: Binding Sites; Crystallography, X-Ray; Deoxyuracil Nucleotides; Dimerization; Enzyme Activation; Enzyme Inhibitors; Folic Acid; Ligands; Models, Molecular; Peptide Fragments; Pneumocystis; Protein Conformation; Quinazolines; Solutions; Spectrometry, Fluorescence; Thymidylate Synthase | 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 |
Balb/c mice as a preclinical model for raltitrexed-induced gastrointestinal toxicity.
Topics: Animals; Antimetabolites, Antineoplastic; Deoxyuridine; Diarrhea; Digestive System; Dose-Response Relationship, Drug; Folic Acid; Intestinal Mucosa; Intestine, Large; Intestine, Small; Male; Maximum Tolerated Dose; Mice; Mice, Inbred BALB C; Mice, Inbred DBA; Quinazolines; Thiophenes; Thymidine; Thymidylate Synthase; Weight Loss | 2000 |
The crystal structure of thymidylate synthase from Pneumocystis carinii reveals a fungal insert important for drug design.
Topics: Amino Acid Sequence; Binding Sites; Crystallography, X-Ray; Deoxyuracil Nucleotides; Dimerization; Drug Design; Enzyme Inhibitors; Folic Acid; Humans; Hydrogen Bonding; Models, Molecular; Molecular Sequence Data; Mutagenesis, Insertional; Pneumocystis; Protein Binding; Protein Conformation; Quinazolines; Sequence Alignment; Species Specificity; Substrate Specificity; Thymidylate Synthase | 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 |
Cross-talk between steroid-receptor-mediated and cell-membrane-receptor-mediated signalling pathways results in the in vivo modulation of c-Met and ornithine decarboxylase gene expression in mouse kidney.
Topics: Androgen Antagonists; Anilides; Animals; Female; Folic Acid; Folic Acid Antagonists; Gene Expression Regulation; Hepatocyte Growth Factor; Kidney; Male; Mice; Nitriles; Ornithine Decarboxylase; Proto-Oncogene Proteins c-met; Quinazolines; Receptors, Cell Surface; Receptors, Steroid; Signal Transduction; Testosterone; Tosyl Compounds | 2001 |
Interligand Overhauser effects in type II dihydrofolate reductase.
Topics: Binding Sites; Catalysis; Escherichia coli; Folic Acid; Kinetics; Ligands; Macromolecular Substances; Nuclear Magnetic Resonance, Biomolecular; Quinazolines; Structure-Activity Relationship; Tetrahydrofolate Dehydrogenase | 2001 |
On the role of conserved histidine 106 in 10-formyltetrahydrofolate dehydrogenase catalysis: connection between hydrolase and dehydrogenase mechanisms.
Topics: Amino Acid Sequence; Animals; Binding Sites; Catalysis; Conserved Sequence; Folic Acid; Histidine; Hydrogen Bonding; Hydrolases; Models, Chemical; Models, Molecular; Molecular Sequence Data; Mutagenesis, Site-Directed; Oxidoreductases Acting on CH-NH Group Donors; Protein Folding; Protein Structure, Tertiary; Quinazolines; Sequence Homology, Amino Acid | 2001 |
Modulation of both endogenous folates and thymidine enhance the therapeutic efficacy of thymidylate synthase inhibitors.
Topics: Animals; Antimetabolites, Antineoplastic; Cell Division; Colonic Neoplasms; Diet; Dose-Response Relationship, Drug; Drug Synergism; Enzyme Inhibitors; Female; Fluorouracil; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Leucovorin; Mice; Mice, Inbred BALB C; Mice, Inbred C3H; Pemetrexed; Quinazolines; Thiophenes; Thymidine; Thymidine Kinase; Thymidylate Synthase | 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 |
Tryptophan 80 and leucine 143 are critical for the hydride transfer step of thymidylate synthase by controlling active site access.
Topics: Binding Sites; Biological Transport; Deoxyuracil Nucleotides; Escherichia coli; Folic Acid; Leucine; Models, Chemical; Point Mutation; Protons; Quinazolines; Tetrahydrofolates; Thymidylate Synthase; Tryptophan | 2002 |
Up-regulation of spermidine/spermine N1-acetyltransferase (SSAT) expression is a part of proliferative but not anabolic response of mouse kidney.
Topics: Acetyltransferases; Animals; Blotting, Northern; Cell Division; Female; Folic Acid; Gene Expression Regulation, Enzymologic; Kidney; Mice; Quinazolines; Reserpine; RNA, Messenger; Testosterone; Time Factors; Up-Regulation | 2002 |
Probing electrostatic channeling in protozoal bifunctional thymidylate synthase-dihydrofolate reductase using site-directed mutagenesis.
Topics: Animals; Binding Sites; Catalysis; Crystallization; Enzyme Stability; Fluorodeoxyuridylate; Folic Acid; Hydrocarbons; Kinetics; Leishmania major; Methane; Models, Molecular; Molecular Structure; Multienzyme Complexes; Mutagenesis, Site-Directed; NADP; Quinazolines; Spectrophotometry; Static Electricity; Structure-Activity Relationship; Substrate Specificity; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Thymidylate Synthase | 2003 |
Selective delivery of CB300638, a cyclopenta[g]quinazoline-based thymidylate synthase inhibitor into human tumor cell lines overexpressing the alpha-isoform of the folate receptor.
Topics: Antineoplastic Agents; Biological Transport; Carcinoma, Squamous Cell; Carrier Proteins; Cell Division; Cyclopentanes; Enzyme Inhibitors; Female; Folate Receptors, GPI-Anchored; Folic Acid; Humans; Kinetics; Quinazolines; Receptors, Cell Surface; Recombinant Proteins; Thymidylate Synthase; Transfection; Tumor Cells, Cultured; Vulvar Neoplasms | 2003 |
Thymidine and hypoxanthine protection patterns of the folic acid-enhanced synergies for combinations of trimetrexate plus a polyglutamylatable inhibitor of purine or thymidylate synthesis against human ileocecal HCT-8 cells.
Topics: Adenocarcinoma; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cecal Neoplasms; Cell Division; Drug Resistance, Multiple; Drug Synergism; Enzyme Inhibitors; Folic Acid; Glutamates; Hematinics; Humans; Hydroxymethyl and Formyl Transferases; Hypoxanthine; Ileal Neoplasms; Peptide Synthases; Phosphoribosylglycinamide Formyltransferase; Pyrimidines; Quinazolines; Thiophenes; Thymidine; Thymidylate Synthase; Trimetrexate; Tumor Cells, Cultured | 2003 |
The role of alpha-folate receptor-mediated transport in the antitumor activity of antifolate drugs.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Agents; Biological Transport; Carrier Proteins; Cell Line, Tumor; Cytosol; Dose-Response Relationship, Drug; Folate Receptors, GPI-Anchored; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Inhibitory Concentration 50; Models, Chemical; Neoplasms; Pemetrexed; Quinazolines; Receptors, Cell Surface; Thiophenes; Time Factors | 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 |
Low folate conditions may enhance the interaction of trifluorothymidine with antifolates in colon cancer cells.
Topics: Antimetabolites; Colonic Neoplasms; DNA Damage; Drug Interactions; Folic Acid; Folic Acid Antagonists; Homeostasis; Humans; Indoles; Isoindoles; Quinazolines; Thiophenes; Trifluridine; Tumor Cells, Cultured | 2006 |
The apo and ternary complex structures of a chemotherapeutic target: human glycinamide ribonucleotide transformylase.
Topics: Apoproteins; Binding Sites; Catalysis; Crystallography, X-Ray; Drug Design; Enzyme Inhibitors; Escherichia coli Proteins; Folic Acid; Humans; Hydrogen-Ion Concentration; Hydroxymethyl and Formyl Transferases; Models, Molecular; Phosphoribosylglycinamide Formyltransferase; Protein Binding; Protein Structure, Tertiary; Quinazolines; Substrate Specificity | 2005 |
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 |
BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors.
Topics: Animals; Apoptosis; Biological Transport; Carrier Proteins; Cell Proliferation; Choriocarcinoma; Enzyme Inhibitors; Female; Folate Receptors, GPI-Anchored; Folic Acid; Humans; Idoxuridine; Iodine Radioisotopes; Leukemia L1210; Lung Neoplasms; Membrane Transport Proteins; Mice; Mice, Nude; Ovarian Neoplasms; Quinazolines; Receptors, Cell Surface; Reduced Folate Carrier Protein; Thymidylate Synthase; Tissue Distribution; Transplantation, Heterologous; Tumor Cells, Cultured | 2005 |
Nuclear and membrane receptor-mediated signalling pathways modulate polyamine biosynthesis and interconversion.
Topics: Adenosylmethionine Decarboxylase; Animals; Folic Acid; Folic Acid Antagonists; Hepatocyte Growth Factor; Hypertrophy; Kidney; Mice; Ornithine Decarboxylase; Polyamines; Quinazolines; Receptors, Cytoplasmic and Nuclear; RNA, Messenger; Signal Transduction; Testosterone | 2007 |
Androgen receptor and c-Myc transcription factors as putative partners in the in vivo cross-talk between androgen receptor-mediated and c-Met-mediated signalling pathways.
Topics: Animals; Down-Regulation; Female; Folic Acid; Folic Acid Antagonists; Hepatocyte Growth Factor; Kidney; Mice; Ornithine Decarboxylase; Proto-Oncogene Proteins c-met; Proto-Oncogene Proteins c-myc; Quinazolines; Receptors, Androgen; RNA, Messenger; Signal Transduction; Testosterone; Transcriptional Activation; Up-Regulation | 2007 |
Nonconserved residues Ala287 and Ser290 of the Cryptosporidium hominis thymidylate synthase domain facilitate its rapid rate of catalysis.
Topics: Alanine; Amino Acid Sequence; Animals; Binding Sites; Catalysis; Chromatography, High Pressure Liquid; Cryptosporidium; Crystallography, X-Ray; Folic Acid; Kinetics; Models, Molecular; Molecular Sequence Data; Multienzyme Complexes; Mutagenesis, Site-Directed; Protein Structure, Tertiary; Protozoan Proteins; Quinazolines; Serine; Tetrahydrofolate Dehydrogenase; Tetrahydrofolates; Thymidine Monophosphate; Thymidylate Synthase | 2007 |
DNA damage and homologous recombination signaling induced by thymidylate deprivation.
Topics: Cell Line, Tumor; Cell Survival; Colonic Neoplasms; DNA Damage; DNA, Neoplasm; Flow Cytometry; Folic Acid; Folic Acid Antagonists; HeLa Cells; Humans; Nucleotides; Phosphorylation; Quinazolines; Rad51 Recombinase; Recombination, Genetic; Replication Protein A; Thiophenes; Thymidine Monophosphate; Thymidylate Synthase | 2008 |
Antifolate/folate-activated HGF/c-Met signalling pathways in mouse kidneys-the putative role of their downstream effectors in cross-talk with androgen receptor.
Topics: Androstadienes; Animals; Cyclin D2; Cyclins; Female; Folic Acid; Folic Acid Antagonists; Glycogen Synthase Kinase 3; Glycogen Synthase Kinase 3 beta; Hepatocyte Growth Factor; Kidney; Mice; Mitogen-Activated Protein Kinases; Models, Biological; Ornithine Decarboxylase; Proliferating Cell Nuclear Antigen; Proto-Oncogene Proteins c-akt; Proto-Oncogene Proteins c-met; PTEN Phosphohydrolase; Quinazolines; Receptor Cross-Talk; Receptors, Androgen; Signal Transduction; Testosterone; Wortmannin | 2009 |
Impact of cellular folate status and epidermal growth factor receptor expression on BCRP/ABCG2-mediated resistance to gefitinib and erlotinib.
Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Caco-2 Cells; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Folic Acid; Gefitinib; Genotype; Humans; Neoplasm Proteins; Phosphorylation; Proto-Oncogene Proteins c-akt; Quinazolines | 2009 |
Functional identity of the active sites of crustacean and viral thymidylate synthases.
Topics: Amino Acid Sequence; Animals; Base Sequence; Catalytic Domain; Cloning, Molecular; Deoxyuracil Nucleotides; Folic Acid; Folic Acid Antagonists; Isoindoles; Kinetics; Models, Molecular; Molecular Sequence Data; Penaeidae; Phylogeny; Quinazolines; Sequence Alignment; Thymidylate Synthase; White spot syndrome virus 1 | 2009 |
Effects of the antifolates pemetrexed and CB3717 on the tissue distribution of (99m)Tc-EC20 in xenografted and syngeneic tumor-bearing mice.
Topics: Animals; Cell Line, Tumor; Female; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; Humans; Kidney; Mice; Mice, Nude; Oligopeptides; Organotechnetium Compounds; Pemetrexed; Quinazolines; Technetium; Xenograft Model Antitumor Assays | 2010 |
Folic acid activity of N-(4-(4-quinazoline)-benzoyl)glutamic acid.
Topics: Folic Acid; Glutamic Acid; Humans; Quinazolines; Vitamin B Complex; Vitamins | 1947 |
EGFR activity is required for renal tubular cell dedifferentiation and proliferation in a murine model of folic acid-induced acute kidney injury.
Topics: Acute Kidney Injury; Animals; Apoptosis; Cell Dedifferentiation; Cell Proliferation; Creatinine; ErbB Receptors; Folic Acid; Gefitinib; Kidney Tubules; Mice; Mice, Inbred C57BL; PAX2 Transcription Factor; Phosphatidylinositol 3-Kinases; Phosphorylation; Proliferating Cell Nuclear Antigen; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-akt; Quinazolines; Signal Transduction | 2013 |
Intestinal absorption of raltitrexed and evaluation of the effects of absorption enhancers.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Acrylic Resins; Algorithms; Animals; Antimetabolites, Antineoplastic; ATP-Binding Cassette Transporters; Biological Availability; Caco-2 Cells; Decanoic Acids; Deoxycholic Acid; Excipients; Folic Acid; Humans; Intestinal Absorption; Male; Pantoprazole; Probenecid; Quinazolines; Rats; Rats, Wistar; Thiophenes; Verapamil | 2013 |
Molecular modeling studies and synthesis of novel methyl 2-(2-(4-oxo-3-aryl-3,4-dihydroquinazolin-2-ylthio)acetamido)alkanoates with potential anti-cancer activity as inhibitors for methionine synthase.
Topics: 5-Methyltetrahydrofolate-Homocysteine S-Methyltransferase; Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Databases, Protein; Enzyme Inhibitors; Folic Acid; Humans; Kinetics; Liver; Molecular Docking Simulation; Protein Structure, Tertiary; Quinazolines; Thermodynamics | 2014 |
Gefitinib loaded folate decorated bovine serum albumin conjugated carboxymethyl-beta-cyclodextrin nanoparticles enhance drug delivery and attenuate autophagy in folate receptor-positive cancer cells.
Topics: Adenosine Triphosphate; Antineoplastic Agents; Autophagy; beta-Cyclodextrins; Cell Survival; Drug Delivery Systems; Folate Receptors, GPI-Anchored; Folic Acid; Gefitinib; HeLa Cells; Humans; Molecular Targeted Therapy; Nanoparticles; Quinazolines; Serum Albumin, Bovine; Spectroscopy, Fourier Transform Infrared | 2014 |
Determinants of the activities of antifolates delivered into cells by folate-receptor-mediated endocytosis.
Topics: Cell Line, Tumor; Endocytosis; Folate Receptor 1; Folic Acid; Folic Acid Antagonists; Glutamates; Guanine; HeLa Cells; Humans; Pemetrexed; Proton-Coupled Folate Transporter; Quinazolines; Reduced Folate Carrier Protein; Thiophenes | 2015 |
A Single Mutation Traps a Half-Sites Reactive Enzyme in Midstream, Explaining Asymmetry in Hydride Transfer.
Topics: Binding Sites; Catalytic Domain; Crystallography, X-Ray; Escherichia coli; Folic Acid; Hydrogen; Models, Molecular; Mutation; Protein Conformation; Quinazolines; Substrate Specificity; Tetrahydrofolates; Thymidylate Synthase | 2018 |
Nucleoside Analogue-Based Supramolecular Nanodrugs Driven by Molecular Recognition for Synergistic Cancer Therapy.
Topics: Animals; Antineoplastic Agents; Clofarabine; Folic Acid; Folic Acid Antagonists; HeLa Cells; Humans; Hydrophobic and Hydrophilic Interactions; Mice, Inbred BALB C; Mice, Nude; Molecular Dynamics Simulation; Nanoparticles; Neoplasms; Quinazolines; Rats; Thiophenes | 2018 |
Persistent accumulation of unrepaired DNA damage in rat cortical neurons: nuclear organization and ChIP-seq analysis of damaged DNA.
Topics: Animals; Antineoplastic Agents; Calcium-Binding Proteins; Cell Nucleus; Cerebral Cortex; Chromatin Immunoprecipitation; DNA Damage; DNA Repair; Folic Acid; Gene Expression Regulation; Glial Fibrillary Acidic Protein; Histones; Male; Microfilament Proteins; Microscopy, Electron; Neurons; Quinazolines; Rats; Rats, Sprague-Dawley; RNA, Messenger; Time Factors; X-Rays | 2018 |
Design and synthesis of leucine-linked quinazoline-4(3H)-one-sulphonamide molecules distorting malarial reductase activity in the folate pathway.
Topics: Animals; Antimalarials; Cell Survival; Chlorocebus aethiops; Drug Design; Folic Acid; Folic Acid Antagonists; Inhibitory Concentration 50; Leucine; Molecular Docking Simulation; Molecular Structure; Plasmodium falciparum; Quantitative Structure-Activity Relationship; Quinazolines; Sulfonamides; Vero Cells | 2019 |
A Dual-Mechanism Antibiotic Kills Gram-Negative Bacteria and Avoids Drug Resistance.
Topics: Animals; Anti-Bacterial Agents; Cell Membrane; Drug Resistance, Bacterial; Female; Folic Acid; Gram-Negative Bacteria; Gram-Positive Bacteria; HEK293 Cells; Humans; Male; Methicillin-Resistant Staphylococcus aureus; Mice; Mice, Inbred BALB C; Microbial Sensitivity Tests; Ovariectomy; Proteomics; Pseudomonas aeruginosa; Pyrroles; Quinazolines | 2020 |
Passive Diffusion vs Active pH-Dependent Encapsulation of Tyrosine Kinase Inhibitors Vandetanib and Lenvatinib into Folate-Targeted Ferritin Delivery System.
Topics: Animals; Antineoplastic Agents; Biocompatible Materials; Cell Death; Cell Line; Cell Movement; Clone Cells; Diffusion; Drug Carriers; Drug Delivery Systems; Ferritins; Folic Acid; Horses; Humans; Hydrogen-Ion Concentration; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Quinazolines; Quinolines; Surface Properties | 2021 |
Folic acid alleviates age-related cognitive decline and inhibits apoptosis of neurocytes in senescence-accelerated mouse prone 8: deoxythymidine triphosphate biosynthesis as a potential mechanism.
Topics: Aging; Animals; Apoptosis; Brain; Cognitive Dysfunction; Dietary Supplements; Folic Acid; Male; Memory; Mice; Morris Water Maze Test; Neurons; Quinazolines; Telomere Shortening; Thiophenes; Thymidylate Synthase; Thymine Nucleotides; Uracil | 2021 |
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 |