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Volumn 6, Issue 9, 1995, Pages 871-881

Folate-based thymidylate synthase inhibitors as anticancer drugs

Author keywords

Antifolates; Thymidylate synthase

Indexed keywords

10 PROPARGYL 5,8 DIDEAZAFOLIC ACID; 2 [5 [[(1,2 DIHYDRO 3 METHYL 1 OXOBENZO[F]QUINAZOLIN 9 YL)METHYL]AMINO] 1 OXO 2 ISOINDOLINYL]GLUTARIC ACID; ENZYME INHIBITOR; METESIND GLUCURONATE; N [4 [2 (2 AMINO 4,7 DIHYDRO 4 OXOPYRROLO[2,3 D]PYRIDIN 5 YL)ETHYL]BENZOYL]GLUTAMIC ACID; NOLATREXED; PLEVITREXED; RALTITREXED; THYMIDYLATE SYNTHASE; THYMIDYLATE SYNTHASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 0028853821     PISSN: 09237534     EISSN: None     Source Type: Journal    
DOI: 10.1093/oxfordjournals.annonc.a059353     Document Type: Review
Times cited : (161)

References (84)
  • 1
    • 85113068442 scopus 로고
    • The basis for antifolate cytotoxicity, selectivity and metabolic transformations: Effects on utilisation of endogenous and exogenous folate cofactors
    • Matherly L.H. Seither R.L. Goldman I.D. The basis for antifolate cytotoxicity, selectivity and metabolic transformations: Effects on utilisation of endogenous and exogenous folate cofactors Powis G. Anticancer Drugs: Antimetabolite Metabolism and Natural Anticancer Agents 1994 Pergamon Press Ltd Oxford UK
    • (1994)
    • Matherly, L.H.1    Seither, R.L.2    Goldman, I.D.3
  • 2
    • 0019383730 scopus 로고
    • Fluorinated pyrimidines as tight-binding inhibitors of thymidylate synthetase
    • Danenberg P.V. Lockshin A. Fluorinated pyrimidines as tight-binding inhibitors of thymidylate synthetase Pharmacol Ther 13 1981 69 90
    • (1981) Pharmacol Ther , vol.13 , pp. 69-90
    • Danenberg, P.V.1    Lockshin, A.2
  • 3
    • 0018926163 scopus 로고
    • Assessment of growth-limiting events caused by 5-fluorouracil in mouse and in human cells
    • Evans R.M. Laskin J.D. Hakala M.T. Assessment of growth-limiting events caused by 5-fluorouracil in mouse and in human cells Cancer Res 40 1980 4113 4122
    • (1980) Cancer Res , vol.40 , pp. 4113-4122
    • Evans, R.M.1    Laskin, J.D.2    Hakala, M.T.3
  • 4
    • 0026637845 scopus 로고
    • Novel mechanism(s) of resistance to 5-fluorouracil in human colon cancer (HCT-8) sublines following exposure to two different clinically relevant dose schedules
    • Aschele C. Sobero A. Faderan M.A. Bertino J.R. Novel mechanism(s) of resistance to 5-fluorouracil in human colon cancer (HCT-8) sublines following exposure to two different clinically relevant dose schedules Cancer Res 52 1992 1855 1864
    • (1992) Cancer Res , vol.52 , pp. 1855-1864
    • Aschele, C.1    Sobero, A.2    Faderan, M.A.3    Bertino, J.R.4
  • 5
    • 0002021562 scopus 로고
    • Gynecologic tumours
    • Hoskins W.J. Perez C.A. Young R.C. Gynecologic tumours DeVita V.T. Jr. Hellman S. Rosenberg S.A. Cancer, Principles and Practice of Oncology 1993 Lippincott Co. J.B. Philadelphia 1152 1225
    • (1993) , pp. 1152-1225
    • Hoskins, W.J.1    Perez, C.A.2    Young, R.C.3
  • 6
    • 85113043326 scopus 로고
    • Poplack D.G. Magrath I.T. Kun L.E. Pizzo P.A. DeVita V.T. Jr. Hellman S. Rosenberg S.A. Leukemias and lymphomas of childhood 1993 J.B. Lippincott Co. Philadelphia 1792 1818
    • (1993) , pp. 1792-1818
    • Poplack, D.G.1    Magrath, I.T.2    Kun, L.E.3    Pizzo, P.A.4
  • 7
    • 85113081102 scopus 로고
    • Harris J.R. Morrow M. Bonadonna G. DeVita V.T. Jr. Hellman S. Rosenberg S.A. Cancer of the breast 1993 J.B. Lippincott Co. Philadelphia 1264 1332
    • (1993) , pp. 1264-1332
    • Harris, J.R.1    Morrow, M.2    Bonadonna, G.3
  • 8
    • 0026597027 scopus 로고
    • Chemotherapeutic strategies in metastatic colorectal cancer An overview of current clinical trials
    • Kohne-Wompner C-H Schmoll H-J Harstrick A. Rustum Y.M. Chemotherapeutic strategies in metastatic colorectal cancer An overview of current clinical trials Semin Oncol 19 Suppl 3 1992 105 125
    • (1992) Semin Oncol , vol.19 , Issue.Suppl 3 , pp. 105-125
    • Kohne-Wompner, C-H1    Schmoll, H-J2    Harstrick, A.3    Rustum, Y.M.4
  • 9
    • 0027980010 scopus 로고
    • Preclinical and clinical aspects of biomodulation of 5-fluorouracil
    • Sotos G.A. Grogan L. Allegra C.J. Preclinical and clinical aspects of biomodulation of 5-fluorouracil Cancer Treat Rev 20 1994 11 49
    • (1994) Cancer Treat Rev , vol.20 , pp. 11-49
    • Sotos, G.A.1    Grogan, L.2    Allegra, C.J.3
  • 10
    • 0028956045 scopus 로고
    • Fluorouracil plus Levamisole as effective adjuvant therapy after resection of stage III colon carcinoma: A final report
    • Moertel C.G. Fleming T.R. Macdonald J.S. Fluorouracil plus Levamisole as effective adjuvant therapy after resection of stage III colon carcinoma: A final report Ann Intern Med 122 1995 321 326
    • (1995) Ann Intern Med , vol.122 , pp. 321-326
    • Moertel, C.G.1    Fleming, T.R.2    Macdonald, J.S.3
  • 11
    • 0016242550 scopus 로고
    • Adjuvant methotrexate and citrovorum-factor treatment of osteogenic sarcoma
    • Jaffe N. Frei E. III Traggis F. Bishop Y. Adjuvant methotrexate and citrovorum-factor treatment of osteogenic sarcoma N Engl J Med 291 1974 994 997
    • (1974) N Engl J Med , vol.291 , pp. 994-997
    • Jaffe, N.1    Frei, E.2    Traggis, F.3    Bishop, Y.4
  • 12
    • 0019368721 scopus 로고
    • A potent antitumour quinazoline inhibitor of thymidylate synthetase: Synthesis, biological properties and therapeutic results in mice
    • Jones T.R. Calvert A.H. Jackman A.L. A potent antitumour quinazoline inhibitor of thymidylate synthetase: Synthesis, biological properties and therapeutic results in mice Eur J Cancer 17 1981 11 19
    • (1981) Eur J Cancer , vol.17 , pp. 11-19
    • Jones, T.R.1    Calvert, A.H.2    Jackman, A.L.3
  • 13
    • 0022894985 scopus 로고
    • A phase I evaluation of the quinazoline antifolate thymidylate synthase inhibitor, N10-propargyl-5,8-dideazafolic acid, CB3717
    • Calvert A.H. Alison D.L. Harland S.J. A phase I evaluation of the quinazoline antifolate thymidylate synthase inhibitor, N10-propargyl-5,8-dideazafolic acid, CB3717 J Clin Oncol 4 1986 1245 1252
    • (1986) J Clin Oncol , vol.4 , pp. 1245-1252
    • Calvert, A.H.1    Alison, D.L.2    Harland, S.J.3
  • 14
    • 0021988146 scopus 로고
    • The clinical pharmacokinetics of the novel antifolate N10-propargyl-5,8-dideazafolic caid (CB3717)
    • Alison D.L. Newell D.R. Sessa C. The clinical pharmacokinetics of the novel antifolate N10-propargyl-5,8-dideazafolic caid (CB3717) Cancer Chemother Pharmacol 14 1985 265 271
    • (1985) Cancer Chemother Pharmacol , vol.14 , pp. 265-271
    • Alison, D.L.1    Newell, D.R.2    Sessa, C.3
  • 15
    • 0023491912 scopus 로고
    • Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB3717)
    • Calvert A.H. Newell D.R. Jackman A.L. Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB3717) NCI Monograph 5 1987 213 218
    • (1987) NCI Monograph , vol.5 , pp. 213-218
    • Calvert, A.H.1    Newell, D.R.2    Jackman, A.L.3
  • 16
    • 0002169639 scopus 로고
    • Thymidylate synthase inhibitors: experimental and clinical aspects
    • Jackman A.L. Jones T.R. Calvert A.H. Thymidylate synthase inhibitors: experimental and clinical aspects Muggia F.M. Experimental and Clinical Progress in Cancer Chemotherapy 1985 Martinus Nijhoff Boston 155 210
    • (1985) , pp. 155-210
    • Jackman, A.L.1    Jones, T.R.2    Calvert, A.H.3
  • 17
    • 0027889184 scopus 로고
    • The history of the development and clinical use of CB3717 and ICI D1694
    • Clarke S.J. Jackman A.L. Judson I.R. The history of the development and clinical use of CB3717 and ICI D1694 Rustum Y. Proc of the International Symposium on Novel Approaches to Selective Treatments of Human Solid Tumors: Laboratory and Clinical Correlation 1993 Plenum Press New York 277 287
    • (1993) , pp. 277-287
    • Clarke, S.J.1    Jackman, A.L.2    Judson, I.R.3
  • 18
    • 0027403420 scopus 로고
    • Design of thymidylate synthase inhibitors using protein crystal structures: The synthesis and biological evaluation of a novel class of 5-substituted quinazolinones
    • Webber S.E. Bleckman T.M. Attard J. Design of thymidylate synthase inhibitors using protein crystal structures: The synthesis and biological evaluation of a novel class of 5-substituted quinazolinones J Med Chem 36 1993 733 746
    • (1993) J Med Chem , vol.36 , pp. 733-746
    • Webber, S.E.1    Bleckman, T.M.2    Attard, J.3
  • 19
    • 0021015054 scopus 로고
    • Biochemical effects of a quinazoline inhibitor of thymidylate synthetase, CB3717, on human lymphoblastoid cells
    • Jackson R.C. Jackman A.L. Calvert A.H. Biochemical effects of a quinazoline inhibitor of thymidylate synthetase, CB3717, on human lymphoblastoid cells Biochem Pharmacol 32 1983 3783 3790
    • (1983) Biochem Pharmacol , vol.32 , pp. 3783-3790
    • Jackson, R.C.1    Jackman, A.L.2    Calvert, A.H.3
  • 20
    • 0024997423 scopus 로고
    • Activity of the thymidylate synthase inhibitor 2-desamino-N10-propargyl-5,8-dideazafolic acid and related compounds in murine (L1210) and human (W1L2) systems in vitro and in L1210 in vivo
    • Jackman A.L. Taylor G.A. O'Connor B.M. Activity of the thymidylate synthase inhibitor 2-desamino-N10-propargyl-5,8-dideazafolic acid and related compounds in murine (L1210) and human (W1L2) systems in vitro and in L1210 in vivo Cancer Res 50 1990 5212 5218
    • (1990) Cancer Res , vol.50 , pp. 5212-5218
    • Jackman, A.L.1    Taylor, G.A.2    O'Connor, B.M.3
  • 21
    • 0021996160 scopus 로고
    • Structural features of 4-amino folates required for substrate activity with mammalian folylpolyglutamate synthetase
    • Moran R.G. Colman P.D. Rosowsky A. Structural features of 4-amino folates required for substrate activity with mammalian folylpolyglutamate synthetase Mol Pharmacol 27 1985 156 166
    • (1985) Mol Pharmacol , vol.27 , pp. 156-166
    • Moran, R.G.1    Colman, P.D.2    Rosowsky, A.3
  • 22
    • 0023699993 scopus 로고
    • Formation and retention and biological activity of N10-propargyl-5,8-dideazafolic acid (CB3717) polyglutamates in L1210 cells in vitro
    • Sikora E. Jackman A.L. Newell D.R. Calvert A.H. Formation and retention and biological activity of N10-propargyl-5,8-dideazafolic acid (CB3717) polyglutamates in L1210 cells in vitro Biochem Pharmacol 37 1988 4047 4054
    • (1988) Biochem Pharmacol , vol.37 , pp. 4047-4054
    • Sikora, E.1    Jackman, A.L.2    Newell, D.R.3    Calvert, A.H.4
  • 23
    • 0024585682 scopus 로고
    • Quinazoline antifolates inhibiting thymidylate synthase: Synthesis of four oligo (L-γ-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition
    • Pawelczak K. Jones T.R. Kempney M. Quinazoline antifolates inhibiting thymidylate synthase: Synthesis of four oligo (L-γ-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition J Med Chem 32 1989 160 165
    • (1989) J Med Chem , vol.32 , pp. 160-165
    • Pawelczak, K.1    Jones, T.R.2    Kempney, M.3
  • 24
    • 0027811090 scopus 로고
    • The role of the reduced-folate carrier and metabolism to intracellular polyglutamates for the activity of ICI D1694. Proc of the International Symposium on Novel Approaches to Selective Treatments of Human Solid Tumors: Laboratory and Clinical Correlation
    • Jackman A.L. Gibson W. Brown M. The role of the reduced-folate carrier and metabolism to intracellular polyglutamates for the activity of ICI D1694. Proc of the International Symposium on Novel Approaches to Selective Treatments of Human Solid Tumors: Laboratory and Clinical Correlation Rustum Y. Adv Exptl Med 1993 Plenum Press New York 265 276
    • (1993) , pp. 265-276
    • Jackman, A.L.1    Gibson, W.2    Brown, M.3
  • 25
    • 85113049580 scopus 로고    scopus 로고
    • Jackman AL, Kimbell R, Brown M et al. Quinazoline thymidylate synthase inhibitors: Methods for assessing the contribution of polyglutamation to their in vitro activity. Anticancer Drug Des; in press.
  • 26
    • 0023920753 scopus 로고
    • Phase II study of the antifolate N10-propargyl-5,8-dideazafolic acid (CB3717) in advanced breast cancer
    • Cantwell B.M.J. MacCaulay V. Harris A.L. Phase II study of the antifolate N10-propargyl-5,8-dideazafolic acid (CB3717) in advanced breast cancer Eur J Cancer 24 1988 733 736
    • (1988) Eur J Cancer , vol.24 , pp. 733-736
    • Cantwell, B.M.J.1    MacCaulay, V.2    Harris, A.L.3
  • 27
    • 0023276902 scopus 로고
    • Induction of remission to hepatocellular carcinoma with a new thymidylate synthase inhibitor, CB3717: A phase II study
    • Bassendine M.F. Curtin N.J. Loose H. Induction of remission to hepatocellular carcinoma with a new thymidylate synthase inhibitor, CB3717: A phase II study J Hepatol 4 1987 349 356
    • (1987) J Hepatol , vol.4 , pp. 349-356
    • Bassendine, M.F.1    Curtin, N.J.2    Loose, H.3
  • 28
    • 0023894086 scopus 로고
    • Phase II study of the thymidylate synthase inhibitor CB3717 (N10-propargyl-5,8-dideazafolic acid) in colorectal cancer
    • Harding M.J. Cantwell B.M.J. Milstead R.A.V. Phase II study of the thymidylate synthase inhibitor CB3717 (N10-propargyl-5,8-dideazafolic acid) in colorectal cancer Br J Cancer 57 1988 628 629
    • (1988) Br J Cancer , vol.57 , pp. 628-629
    • Harding, M.J.1    Cantwell, B.M.J.2    Milstead, R.A.V.3
  • 29
    • 0024521754 scopus 로고
    • Quinazoline antifolates inhibiting thymidylate synthase: 2-Desamino derivatives with enhanced solubility and potency
    • Jones T.R. Thornton T.J. Flinn A. Quinazoline antifolates inhibiting thymidylate synthase: 2-Desamino derivatives with enhanced solubility and potency J Med Chem 32 1989 847 852
    • (1989) J Med Chem , vol.32 , pp. 847-852
    • Jones, T.R.1    Thornton, T.J.2    Flinn, A.3
  • 30
    • 0024993953 scopus 로고
    • Quinazoline antifolate thymidylate synthase inhibitors: Alkyl, substituted alkyl, and aryl substituents in the C2 position
    • Hughes L.R. Jackman A.L. Oldfield J. Quinazoline antifolate thymidylate synthase inhibitors: Alkyl, substituted alkyl, and aryl substituents in the C2 position J Med Chem 33 1990 3060 3067
    • (1990) J Med Chem , vol.33 , pp. 3060-3067
    • Hughes, L.R.1    Jackman, A.L.2    Oldfield, J.3
  • 31
    • 0025933916 scopus 로고
    • The biochemical pharmacology of the thymidylate synthase inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)
    • Jackman A.L. Newell D.R. Gibson W. The biochemical pharmacology of the thymidylate synthase inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583) Biochem Pharmacol 42 1991 1885 1895
    • (1991) Biochem Pharmacol , vol.42 , pp. 1885-1895
    • Jackman, A.L.1    Newell, D.R.2    Gibson, W.3
  • 32
    • 0020686617 scopus 로고
    • Analysis of the role of membrane transport and polyglutamation of methotrexate in gut and Ehrlich tumour in vivo as factors of drug sensitivity and selectivity
    • Fry D.W. Anderson L.A. Borst M. Goldman I.D. Analysis of the role of membrane transport and polyglutamation of methotrexate in gut and Ehrlich tumour in vivo as factors of drug sensitivity and selectivity Cancer Res 43 1983 1087 1092
    • (1983) Cancer Res , vol.43 , pp. 1087-1092
    • Fry, D.W.1    Anderson, L.A.2    Borst, M.3    Goldman, I.D.4
  • 33
    • 0019800796 scopus 로고
    • Differential synthesis of methotrexate polyglutamates in normal proliferative and neoplastic mouse tissues in vivo
    • Poser R.G. Sirotnak F.M. Chello P.L. Differential synthesis of methotrexate polyglutamates in normal proliferative and neoplastic mouse tissues in vivo Cancer Res 41 1981 4441 4446
    • (1981) Cancer Res , vol.41 , pp. 4441-4446
    • Poser, R.G.1    Sirotnak, F.M.2    Chello, P.L.3
  • 34
    • 0025329072 scopus 로고
    • Differing specificities for 4-aminofolate analogs, of folylpolyglutamyl synthetase from tumours and proliferative intestinal epithelium of the mouse with significance for selective antitumour action
    • Rumberger B.G. Barrueco J.R. Sirotnak F.M. Differing specificities for 4-aminofolate analogs, of folylpolyglutamyl synthetase from tumours and proliferative intestinal epithelium of the mouse with significance for selective antitumour action Cancer Res 50 1990 4639 4643
    • (1990) Cancer Res , vol.50 , pp. 4639-4643
    • Rumberger, B.G.1    Barrueco, J.R.2    Sirotnak, F.M.3
  • 35
    • 85113074904 scopus 로고    scopus 로고
    • Jackman AL, Kimbell R, Brown M et al. Quinazoline-based thymidylate synthase inhibitors: Relationship between structural modifications and polyglutamation. Anticancer Drug Des; in press.
  • 36
    • 0021222361 scopus 로고
    • Modulation of antimetabolite effects: Effects of thymidine on the efficacy of the quinazoline-based thymidylate synthetase inhibitor, CB 3717
    • Jackman A.L. Taylor G.A. Calvert A.H. Harrap K.R. Modulation of antimetabolite effects: Effects of thymidine on the efficacy of the quinazoline-based thymidylate synthetase inhibitor, CB 3717 Biochem Pharmacol 33 1984 3269 3275
    • (1984) Biochem Pharmacol , vol.33 , pp. 3269-3275
    • Jackman, A.L.1    Taylor, G.A.2    Calvert, A.H.3    Harrap, K.R.4
  • 37
    • 0025997350 scopus 로고
    • 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
    • Jackman A.L. Taylor G.A. Gibson W. 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 Cancer Res 51 1991 5579 5586
    • (1991) Cancer Res , vol.51 , pp. 5579-5586
    • Jackman, A.L.1    Taylor, G.A.2    Gibson, W.3
  • 38
    • 0027438847 scopus 로고
    • Use of murine L5178Y lymphoma thymidine kinase mutants for in vitro and in vivo antitumour efficacy evaluation of novel thymidine synthase inhibitors. Chemistry and Biology of Pteridines and Folates
    • Stephens T.C. Smith M.N. Waterman S.E. Use of murine L5178Y lymphoma thymidine kinase mutants for in vitro and in vivo antitumour efficacy evaluation of novel thymidine synthase inhibitors. Chemistry and Biology of Pteridines and Folates Ayling J.E. Nair M.G. Baugh C.M. Advances in Experimental Medicine and Biology 1993 Plenum Press New York 589 592
    • (1993) , pp. 589-592
    • Stephens, T.C.1    Smith, M.N.2    Waterman, S.E.3
  • 39
    • 0026326240 scopus 로고
    • ICI D1694, an inhibitor of thymidylate synthase for clinical study
    • Jackman A.L. Jodrell Dl Gibson W. Stephens T.C. ICI D1694, an inhibitor of thymidylate synthase for clinical study Harkness R.A. Elion G.B. Zollner N. Purine and Pyrimidine Metabolism in Man VII, Part A, pp 19–23 1991 Plenum Press New York 19 23
    • (1991) , pp. 19-23
    • Jackman, A.L.1    Jodrell, Dl2    Gibson, W.3    Stephens, T.C.4
  • 40
    • 0009688297 scopus 로고
    • The thymidylate synthase inhibitor ICI D1694 is superior to CB3717, 5-fluorouracil and methotrexate against a panel of human tumour xenografts
    • Stephens T.C. Valaccia B.E. Sheader M.L. The thymidylate synthase inhibitor ICI D1694 is superior to CB3717, 5-fluorouracil and methotrexate against a panel of human tumour xenografts Proc Am Assoc Cancer Res 32 1991 328
    • (1991) Proc Am Assoc Cancer Res , vol.32 , pp. 328
    • Stephens, T.C.1    Valaccia, B.E.2    Sheader, M.L.3
  • 41
    • 0026519367 scopus 로고
    • Kinetic characteristics of ICI D1694: A quinazoline antifolate which inhibits thymidyate synthase
    • Ward W.H.J. Kimbell R. Jackman A.L. Kinetic characteristics of ICI D1694: A quinazoline antifolate which inhibits thymidyate synthase Biochem Pharmacol 43 1992 2029 2031
    • (1992) Biochem Pharmacol , vol.43 , pp. 2029-2031
    • Ward, W.H.J.1    Kimbell, R.2    Jackman, A.L.3
  • 42
    • 0029164564 scopus 로고
    • ZD1694 (Tomudex): A new thymidylate synthase inhibitor with activity in colorectal cancer
    • Jackman A.L. Farrugia D.C. Gibson ZD1694 (Tomudex): A new thymidylate synthase inhibitor with activity in colorectal cancer Eur J Cancer 31A 1995 1277 1282
    • (1995) Eur J Cancer , vol.31A , pp. 1277-1282
    • Jackman, A.L.1    Farrugia, D.C.2    Gibson3
  • 43
    • 0026054878 scopus 로고
    • Thymidylate synthase inhibitors: The in vitro activity of a series of heterocyclic benzoyl ring modified 2-desanuno-2-methyl-N10-substituted-5,8-dideazafolates
    • Jackman A.L. Marsham P.R. Moran R.G. Thymidylate synthase inhibitors: The in vitro activity of a series of heterocyclic benzoyl ring modified 2-desanuno-2-methyl-N10-substituted-5,8-dideazafolates Adv Enzyme Regul 31 1991 13 27
    • (1991) Adv Enzyme Regul , vol.31 , pp. 13-27
    • Jackman, A.L.1    Marsham, P.R.2    Moran, R.G.3
  • 44
    • 0027502819 scopus 로고
    • The measurement of polyglutamate metabolites of the thymidylate synthase inhibitor, ICI D1694, in mouse and human cultured cells
    • Gibson W. Bisset G.M.F. Marsham P.R. The measurement of polyglutamate metabolites of the thymidylate synthase inhibitor, ICI D1694, in mouse and human cultured cells Biochem Pharmacol 45 1993 863 869
    • (1993) Biochem Pharmacol , vol.45 , pp. 863-869
    • Gibson, W.1    Bisset, G.M.F.2    Marsham, P.R.3
  • 45
    • 0029031286 scopus 로고
    • Mechanisms of acquired resistance to the quinazoline thymidylate synthase inhibitor, ZD1694 (Tomudex) in one mouse and three human cell lines
    • Jackman A.L. Kelland L.R. Kimbell Mechanisms of acquired resistance to the quinazoline thymidylate synthase inhibitor, ZD1694 (Tomudex) in one mouse and three human cell lines Br J Cancer 71 1995 914 924
    • (1995) Br J Cancer , vol.71 , pp. 914-924
    • Jackman, A.L.1    Kelland, L.R.2    Kimbell3
  • 46
    • 0029017702 scopus 로고
    • The measurement of deoxynucleotide (dNTP) pools by radioimmunoassay. Purine and Pyrimidine Metabolism in Man
    • Aherne W. Hardcastle A. Kelland L. Jackman A. The measurement of deoxynucleotide (dNTP) pools by radioimmunoassay. Purine and Pyrimidine Metabolism in Man Sahota A. Taylor M. Advances in Experimental Medicine and Biology 1995 Plenum Press New York 801 804
    • (1995) , pp. 801-804
    • Aherne, W.1    Hardcastle, A.2    Kelland, L.3    Jackman, A.4
  • 47
    • 0025744809 scopus 로고
    • The pharmacokinetics of the quinazoline antifolate ICI D1694 in mice and rats
    • Jodrell D.I. Newell D.R. Gibson W. The pharmacokinetics of the quinazoline antifolate ICI D1694 in mice and rats Cancer Chemother Pharmacol 28 1991 331 338
    • (1991) Cancer Chemother Pharmacol , vol.28 , pp. 331-338
    • Jodrell, D.I.1    Newell, D.R.2    Gibson, W.3
  • 48
    • 0025925284 scopus 로고
    • The renal effects of N10-propargyl-5,8-dideazafolic acid (CB3717) and a non-nephrotoxic analogue ICI D1694, in mice
    • Jodrell D.I. Newell D.R. Morgan S.E. The renal effects of N10-propargyl-5,8-dideazafolic acid (CB3717) and a non-nephrotoxic analogue ICI D1694, in mice Br J Cancer 64 1991 833 838
    • (1991) Br J Cancer , vol.64 , pp. 833-838
    • Jodrell, D.I.1    Newell, D.R.2    Morgan, S.E.3
  • 49
    • 0027494408 scopus 로고
    • The toxicity of ICI D1694 in man and mouse. Chemistry and Biology of Pteridines and Folates
    • Clarke S.J. Jackman A.L. Judson I.R. The toxicity of ICI D1694 in man and mouse. Chemistry and Biology of Pteridines and Folates Ayling J.E. Nair M.G. Baugh C.M. Advances in Experimental Medicine and Biology 1993 Plenum Press New York 601 604
    • (1993) , pp. 601-604
    • Clarke, S.J.1    Jackman, A.L.2    Judson, I.R.3
  • 50
    • 0343303553 scopus 로고
    • Antitumour activity of a new thymidylate synthase inhibitor, D1694
    • Stephens T.C. Calvete J.A. Janes D. Antitumour activity of a new thymidylate synthase inhibitor, D1694 Proc Am Assoc Cancer Res 31 1990 342
    • (1990) Proc Am Assoc Cancer Res , vol.31 , pp. 342
    • Stephens, T.C.1    Calvete, J.A.2    Janes, D.3
  • 51
    • 0000154770 scopus 로고
    • Phase I study of the new thymidylate synthase inhibitor Tomudex (ZD1694) in patients with advanced malignancy
    • Clarke S.J. Ward J. de Boer M. Phase I study of the new thymidylate synthase inhibitor Tomudex (ZD1694) in patients with advanced malignancy Ann Oncol 5 Suppl 5 1994 132
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 5 , pp. 132
    • Clarke, S.J.1    Ward, J.2    de Boer, M.3
  • 52
    • 0000154770 scopus 로고
    • Phase I trial of ZD1694 (Tomudex), a direct inhibitor of thymidylate synthase
    • Sorenson J.M. Jordan E. Grem J.L. Phase I trial of ZD1694 (Tomudex), a direct inhibitor of thymidylate synthase Ann Oncol 5 Suppl 5 1994 132
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 5 , pp. 132
    • Sorenson, J.M.1    Jordan, E.2    Grem, J.L.3
  • 53
    • 0000267893 scopus 로고
    • Tomudex: A novel thymidylate synthase inhibitor with clinical antitumour activity in a range of solid rumours
    • Cunningham D. Zalcberg J. Smith I.E. Tomudex: A novel thymidylate synthase inhibitor with clinical antitumour activity in a range of solid rumours Ann Oncol 5 Suppl 8 1994 179
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 8 , pp. 179
    • Cunningham, D.1    Zalcberg, J.2    Smith, I.E.3
  • 54
    • 0342489558 scopus 로고
    • The final results of a large phase II study of the potent thymidylate synthase inhibitor Tomudex (ZD1694) in advanced colorectal cancer
    • Zalcberg J. Cunningham D. Green M. The final results of a large phase II study of the potent thymidylate synthase inhibitor Tomudex (ZD1694) in advanced colorectal cancer Proc ASCO 14 1995 204
    • (1995) Proc ASCO , vol.14 , pp. 204
    • Zalcberg, J.1    Cunningham, D.2    Green, M.3
  • 55
    • 0002783456 scopus 로고
    • Tomudex (ZD1694) has superior response and toxicity profiles compared to 5-fluorouracil and LV in advanced colorectal cancer: First results of a large international phase III study
    • Kerr D. Cunningham D. Zalcberg J. Tomudex (ZD1694) has superior response and toxicity profiles compared to 5-fluorouracil and LV in advanced colorectal cancer: First results of a large international phase III study Br J Cancer 72 Suppl XV 1995 10
    • (1995) Br J Cancer , vol.72 , Issue.Suppl XV , pp. 10
    • Kerr, D.1    Cunningham, D.2    Zalcberg, J.3
  • 56
    • 0026494947 scopus 로고
    • A dideazatetrahydrofolate analogue lacking a chiral center at C-6, N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, is an inhibitor of thymidylate synthase
    • Taylor E.C. Kuhnt D. A dideazatetrahydrofolate analogue lacking a chiral center at C-6, N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid, is an inhibitor of thymidylate synthase J Med Chem 35 1992 4450 4454
    • (1992) J Med Chem , vol.35 , pp. 4450-4454
    • Taylor, E.C.1    Kuhnt, D.2
  • 57
    • 0000730899 scopus 로고
    • LY231514, a novel pyrrolo-pyrimidine antifolate that inhibits thymidylate synthase
    • Grindey G.B. Shih C. Barnett LY231514, a novel pyrrolo-pyrimidine antifolate that inhibits thymidylate synthase Proc Am Assoc Cancer Res 33 1992 411
    • (1992) Proc Am Assoc Cancer Res , vol.33 , pp. 411
    • Grindey, G.B.1    Shih, C.2    Barnett3
  • 58
    • 2642641659 scopus 로고
    • A phase I evaluation of the novel thymidylate synthase inhibitor, LY231514, in patients with advanced solid tumours
    • Rinaldi D.A. Burris H.A. Dorr F.A. A phase I evaluation of the novel thymidylate synthase inhibitor, LY231514, in patients with advanced solid tumours Proc ASCO 13 1994 159
    • (1994) Proc ASCO , vol.13 , pp. 159
    • Rinaldi, D.A.1    Burris, H.A.2    Dorr, F.A.3
  • 59
    • 2642618936 scopus 로고
    • Clinical phase I study of LY231514 (an inhibitor of thymidylate synthase) using a daily × 5 q 21 schedule
    • Vasey P.A. Calvert A.H. Kaye S.B. Cassidy J. Clinical phase I study of LY231514 (an inhibitor of thymidylate synthase) using a daily × 5 q 21 schedule Ann Oncol 5 Suppl 5 1994 131
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 5 , pp. 131
    • Vasey, P.A.1    Calvert, A.H.2    Kaye, S.B.3    Cassidy, J.4
  • 60
    • 0344138767 scopus 로고
    • A phase I evaluation of LY231514 administered every 21 days, utilising the modified continual reassessment method for dose escalation
    • Rinaldi D. Burris H. Dorr F. A phase I evaluation of LY231514 administered every 21 days, utilising the modified continual reassessment method for dose escalation Proc ASCO 14 1995 474
    • (1995) Proc ASCO , vol.14 , pp. 474
    • Rinaldi, D.1    Burris, H.2    Dorr, F.3
  • 61
    • 0004829272 scopus 로고
    • Preclinical studies on AG-337, a novel lipophilic thymidylate synthase inhibitor
    • Webber S. Johnston A. Shetty B. Preclinical studies on AG-337, a novel lipophilic thymidylate synthase inhibitor Proc Am Assoc Cancer Res 34 1993 273
    • (1993) Proc Am Assoc Cancer Res , vol.34 , pp. 273
    • Webber, S.1    Johnston, A.2    Shetty, B.3
  • 62
    • 0026554077 scopus 로고
    • Crystal-structure-based design and synthesis of benz[cd]indole-containing inhibitors of thymidylate synthase
    • Varney M.D. Marzoni G.P. Palmer C.L. Crystal-structure-based design and synthesis of benz[cd]indole-containing inhibitors of thymidylate synthase J Med Chem 35 1992 663 676
    • (1992) J Med Chem , vol.35 , pp. 663-676
    • Varney, M.D.1    Marzoni, G.P.2    Palmer, C.L.3
  • 63
    • 0028237440 scopus 로고
    • Biological activity of a novel rationally designed lipophilic thymidylate synthase inhibitor
    • O'Connor B.M. Webber S. Jackson R.C. Biological activity of a novel rationally designed lipophilic thymidylate synthase inhibitor Cancer Chemother Pharmacol 34 1994 225 229
    • (1994) Cancer Chemother Pharmacol , vol.34 , pp. 225-229
    • O'Connor, B.M.1    Webber, S.2    Jackson, R.C.3
  • 64
    • 0013472183 scopus 로고
    • In vitro properties and antitumour activity of AG-331, a novel lipophilic thymidylate synthase inhibitor
    • Webber S. Shetty B. Johnston A. In vitro properties and antitumour activity of AG-331, a novel lipophilic thymidylate synthase inhibitor Proc Am Assoc Cancer Res 33 1992 413
    • (1992) Proc Am Assoc Cancer Res , vol.33 , pp. 413
    • Webber, S.1    Shetty, B.2    Johnston, A.3
  • 65
    • 0008797213 scopus 로고
    • A phase I study of the novel antifolate 3,4-dihydro-2-amino-6-methyl-4-oxo-5-(4-pyridylthio)-quinazolone dihydrochloride (AG337) given by a 24 intravenous continuous infusion
    • Rafi I. Taylor G.A. Balmanno K. A phase I study of the novel antifolate 3,4-dihydro-2-amino-6-methyl-4-oxo-5-(4-pyridylthio)-quinazolone dihydrochloride (AG337) given by a 24 intravenous continuous infusion Ann Oncol 5 Suppl 5 1994 131
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 5 , pp. 131
    • Rafi, I.1    Taylor, G.A.2    Balmanno, K.3
  • 66
    • 0008742276 scopus 로고
    • Pre-clinical and clinical studies of prolonged administration of the novel thymidylate synthase inhibitor. AG337
    • Calvete J.A. Balmanno K. Taylor G.A. Pre-clinical and clinical studies of prolonged administration of the novel thymidylate synthase inhibitor. AG337 Proc Am Assoc Cancer Res 35 1994 306
    • (1994) Proc Am Assoc Cancer Res , vol.35 , pp. 306
    • Calvete, J.A.1    Balmanno, K.2    Taylor, G.A.3
  • 67
    • 25144442774 scopus 로고
    • A phase I clinical study of the novel antifolate AG337 given by 5 day continuous infusion
    • Rafi I. Taylor G.A. Calvete J.A. A phase I clinical study of the novel antifolate AG337 given by 5 day continuous infusion Br J Cancer 71 Suppl XXIV 1995 10
    • (1995) Br J Cancer , vol.71 , Issue.Suppl XXIV , pp. 10
    • Rafi, I.1    Taylor, G.A.2    Calvete, J.A.3
  • 68
    • 0008758702 scopus 로고
    • AG331, a 'non-classical', lipophilic thymidylate synthase inhibitor for the treatment of solid tumours
    • Clendennin N.J. Peterkin J.J. Webber S. AG331, a 'non-classical', lipophilic thymidylate synthase inhibitor for the treatment of solid tumours Ann Oncol 5 Suppl 5 1994 133
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 5 , pp. 133
    • Clendennin, N.J.1    Peterkin, J.J.2    Webber, S.3
  • 69
    • 0342868519 scopus 로고
    • Phase I trial of AG331 as a 5-day continuous infusion
    • Giantonio B. Qian M. Gallo J. Phase I trial of AG331 as a 5-day continuous infusion Proc ASCO 14 1995 480
    • (1995) Proc ASCO , vol.14 , pp. 480
    • Giantonio, B.1    Qian, M.2    Gallo, J.3
  • 70
    • 0027186327 scopus 로고
    • Benzoquinazoline inhibitors of thymidylate synthase: Enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones
    • Pendagast W. Johnson J.V. Dickerson S.H. Benzoquinazoline inhibitors of thymidylate synthase: Enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones J Med Chem 36 1993 2279 2291
    • (1993) J Med Chem , vol.36 , pp. 2279-2291
    • Pendagast, W.1    Johnson, J.V.2    Dickerson, S.H.3
  • 71
    • 0027477992 scopus 로고
    • Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase
    • Duch D.S. Banks S. Dev I.K. Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase Cancer Res 53 1993 810 818
    • (1993) Cancer Res , vol.53 , pp. 810-818
    • Duch, D.S.1    Banks, S.2    Dev, I.K.3
  • 72
    • 0028014283 scopus 로고
    • Mode of binding of folate analogs to thymidylate synthase
    • Dev I.K. Dallas W.S. Ferone R. Mode of binding of folate analogs to thymidylate synthase J Biol Chem 269 1994 1873 1882
    • (1994) J Biol Chem , vol.269 , pp. 1873-1882
    • Dev, I.K.1    Dallas, W.S.2    Ferone, R.3
  • 73
    • 0002997779 scopus 로고
    • Influence of intracellular polyglutamation on the cytotoxicity of the thymidylate synthase inhibitor 1843U89
    • Ferone R. Hanlon M.H. Waters K.A. Dev I.K. Influence of intracellular polyglutamation on the cytotoxicity of the thymidylate synthase inhibitor 1843U89 Proc Am Assoc Cancer Res 34 1993 274
    • (1993) Proc Am Assoc Cancer Res , vol.34 , pp. 274
    • Ferone, R.1    Hanlon, M.H.2    Waters, K.A.3    Dev, I.K.4
  • 74
    • 0027369455 scopus 로고
    • Studies on the cross-resistance of folylpolyglutamate synthetase-deficient, methotrexate-resistant CCRF-CEM human leukemia sublines. Chemistry and Biology of Pteridines and Folates
    • McGuire J.J. Heitzman K.J. Haile W.H. Studies on the cross-resistance of folylpolyglutamate synthetase-deficient, methotrexate-resistant CCRF-CEM human leukemia sublines. Chemistry and Biology of Pteridines and Folates Ayling J.E. Nair M.G. Baugh C.M. Advances in Experimental Medicine and Biology 1993 Plenum Press New York 667 670
    • (1993) , pp. 667-670
    • McGuire, J.J.1    Heitzman, K.J.2    Haile, W.H.3
  • 75
    • 0002995796 scopus 로고
    • Antitumour activity of the novel thymidylate synthase inhibitor 1843U89 in cells resistant to antifolates by multiple mechanisms
    • Humphreys J. Smith G. Waters K. Duch D. Antitumour activity of the novel thymidylate synthase inhibitor 1843U89 in cells resistant to antifolates by multiple mechanisms Proc Am Assoc Cancer Res 34 1993 273
    • (1993) Proc Am Assoc Cancer Res , vol.34 , pp. 273
    • Humphreys, J.1    Smith, G.2    Waters, K.3    Duch, D.4
  • 76
    • 0003061366 scopus 로고
    • In vivo antitumour activity of 1843U89, a new antifolate thymidylate synthase inhibitor
    • Wilson H.R. Heath L.S. Knick V.C. In vivo antitumour activity of 1843U89, a new antifolate thymidylate synthase inhibitor Proc Am Assoc Cancer Res 33 1992 407
    • (1992) Proc Am Assoc Cancer Res , vol.33 , pp. 407
    • Wilson, H.R.1    Heath, L.S.2    Knick, V.C.3
  • 77
    • 0000494096 scopus 로고
    • ZD9331, The design and synthesis of a novel non-polyglutamatable TS inhibitor
    • Wardleworth J.M. Boyle F.T. Barker R.J. ZD9331, The design and synthesis of a novel non-polyglutamatable TS inhibitor Ann Oncol 5 Suppl 5 1994 247
    • (1994) Ann Oncol , vol.5 , Issue.Suppl 5 , pp. 247
    • Wardleworth, J.M.1    Boyle, F.T.2    Barker, R.J.3
  • 78
    • 0345582800 scopus 로고
    • ZD9331 — Design of a novel non-polyglutamatable quinazoline-based inhibitor of thymidylate synthase
    • Boyle F.T. Wardleworth J.M. Hennequin L.F. ZD9331 — Design of a novel non-polyglutamatable quinazoline-based inhibitor of thymidylate synthase Proc Am Assoc Cancer Res 35 1994 302
    • (1994) Proc Am Assoc Cancer Res , vol.35 , pp. 302
    • Boyle, F.T.1    Wardleworth, J.M.2    Hennequin, L.F.3
  • 79
    • 0029044677 scopus 로고
    • The antitumour activity of ZD9331, a non-polyglutamatable quinazoline thymidylate synthase inhibitor. Purine and Pyrimidine Metabolism in Man
    • Jackman A.L. Kimbell R. Brown M. The antitumour activity of ZD9331, a non-polyglutamatable quinazoline thymidylate synthase inhibitor. Purine and Pyrimidine Metabolism in Man Sahota A. Taylor M. Advances in Experimental Medicine and Biology 1995 Plenum Press New York 185 188
    • (1995) , pp. 185-188
    • Jackman, A.L.1    Kimbell, R.2    Brown, M.3
  • 80
    • 0007357121 scopus 로고
    • ZD9331, A non-polyglutamatable quinazoline thymidylate synthase inhibitor
    • Jackman A.L. Aherne G.W. Kimbell R. ZD9331, A non-polyglutamatable quinazoline thymidylate synthase inhibitor Proc Am Assoc Cancer Res 35 1994 301
    • (1994) Proc Am Assoc Cancer Res , vol.35 , pp. 301
    • Jackman, A.L.1    Aherne, G.W.2    Kimbell, R.3
  • 81
    • 0001104819 scopus 로고
    • ZD9331, a novel non-polyglutamated thymidylate synthase inhibitor In vivo antitumour efficacy and toxicity to normal murine tissues
    • Stephens T.C. Smith M.N. McCloskey M.L. ZD9331, a novel non-polyglutamated thymidylate synthase inhibitor In vivo antitumour efficacy and toxicity to normal murine tissues Proc Am Assoc Cancer Res 35 1994 305
    • (1994) Proc Am Assoc Cancer Res , vol.35 , pp. 305
    • Stephens, T.C.1    Smith, M.N.2    McCloskey, M.L.3
  • 82
    • 0021328814 scopus 로고
    • New folate analogues of the 10-deaza-aminopterin series. Basis for structural design and biochemical and pharmacologic properties
    • Sirotnak F.M. DeGraw J.I. Moccio D.M. New folate analogues of the 10-deaza-aminopterin series. Basis for structural design and biochemical and pharmacologic properties Cancer Chemother Pharmacol 12 1984 18 25
    • (1984) Cancer Chemother Pharmacol , vol.12 , pp. 18-25
    • Sirotnak, F.M.1    DeGraw, J.I.2    Moccio, D.M.3
  • 83
    • 0013684729 scopus 로고
    • Delayed rescue of ZD1694 toxicity in Balb.c mice with thymidine or Leucovorin
    • Jackman A.L. Farrugia D.C. Clarke S.J. Delayed rescue of ZD1694 toxicity in Balb.c mice with thymidine or Leucovorin Proc Am Assoc Cancer Res 36 1995 377
    • (1995) Proc Am Assoc Cancer Res , vol.36 , pp. 377
    • Jackman, A.L.1    Farrugia, D.C.2    Clarke, S.J.3
  • 84
    • 85113059515 scopus 로고
    • Enhanced antitumour selectivity for 1843U89 through decreased host toxicity with oral folic acid
    • Smith G.K. Duch D.S. Ferone R. Enhanced antitumour selectivity for 1843U89 through decreased host toxicity with oral folic acid Proc Am Assoc Cancer Res 36 1995 376
    • (1995) Proc Am Assoc Cancer Res , vol.36 , pp. 376
    • Smith, G.K.1    Duch, D.S.2    Ferone, R.3


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