Folate-based thymidylate synthase inhibitors as anticancer drugs

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1994 • 1,825 citations

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1962 • 940 citations

Fluorouracil plus Levamisole as Effective Adjuvant Therapy after Resection of Stage III Colon Carcinoma: A Final Report

1995 • 907 citations

Adjuvant Methotrexate and Citrovorum-Factor Treatment of Osteogenic Sarcoma

1974 • 484 citations

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.

1991 • 360 citations

A dideazatetrahydrofolate analog lacking a chiral center at C-6: N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5yl)ethyl[benzoyl]-L-glutamic acid is an inhibitor of thymidylate synthase

1992 • 254 citations

A potent antitumour quinazoline inhibitor of thymidylate synthetase: Synthesis, biological properties and therapeutic results in mice

1981 • 242 citations

Novel mechanism(s) of resistance to 5-fluorouracil in human colon cancer (HCT-8) sublines following exposure to two different clinically relevant dose schedules.

1992 • 195 citations

Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones

1993 • 162 citations

New folate analogs of the 10-deaza-aminopterin series Basis for structural design and biochemical and pharmacologic properties

1984 • 143 citations

Crystal-structure-based design and synthesis of benz[cd]indole-containing inhibitors of thymidylate synthase

1992 • 114 citations

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

1983 • 113 citations

Biochemical and cellular pharmacology of 1843U89, a novel benzoquinazoline inhibitor of thymidylate synthase.

1993 • 112 citations

Assessment of growth-limiting events caused by 5-fluorouracil in mouse cells and in human cells.

1980 • 110 citations

Mechanisms of acquired resistance to the quinazoline thymidylate synthase inhibitor ZD1694 (Tomudex) in one mouse and three human cell lines

1995 • 105 citations

A phase I evaluation of the quinazoline antifolate thymidylate synthase inhibitor, N10-propargyl-5,8-dideazafolic acid, CB3717.

1986 • 103 citations

Chemotherapeutic strategies in metastatic colorectal cancer: an overview of current clinical trials.

1992 • 102 citations

ZD1694 (Tomudex): A new thymidylate synthase inhibitor with activity in colorectal cancer

1995 • 102 citations

Preclinical and clinical aspects of biomodulation of 5-fluorouracil

1994 • 99 citations

Modulation of anti-metabolite effects

1984 • 96 citations

Differential synthesis of methotrexate polyglutamates in normal proliferative and neoplastic mouse tissues in vivo.

1981 • 84 citations

Analysis of the role of membrane transport and polyglutamation of methotrexate in gut and the Ehrlich tumor in vivo as factors in drug sensitivity and selectivity.

1983 • 84 citations

Structural features of 4-amino antifolates required for substrate activity with mammalian folylpolyglutamate synthetase.

1985 • 78 citations

Quinazoline antifolate thymidylate synthase inhibitors: alkyl, substituted alkyl, and aryl substituents in the C-2 position

1990 • 74 citations

Experimental and Clinical Progress in Cancer Chemotherapy

1985 • 69 citations

Fluorinated pyrimidines as tight-binding inhibitors of thymidylate synthetase

1981 • 64 citations

Quinazoline antifolates inhibiting thymidylate synthase: 2-desamino derivatives with enhanced solubility and potency

1989 • 63 citations

Formation and retention and biological activity of N10-propargyl-5, 8-dideazafolic acid (CB3717) polyglutamates in L1210 cells in vitro

1988 • 63 citations

‘Tomudex’ (ZD1694) : A novel thymidylate synthase inhibitor with clinical antitumour activity in a range of solid tumours

1996 • 61 citations

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.

1990 • 61 citations

The biochemical pharmacology of the thymidylate synthase inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)

1991 • 59 citations

Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones

1993 • 52 citations

Mode of binding of folate analogs to thymidylate synthase. Evidence for two asymmetric but interactive substrate binding sites.

1994 • 50 citations

Phase II study of the antifolate N10-propargyl-5,8-dideazafolic acid (CB 3717) in advanced breast cancer

1988 • 47 citations

The clinical pharmacokinetics of the novel antifolate N10-propargyl-5,8-dideazafolic acid (CB 3717)

1985 • 44 citations

Kinetic characteristics of ICI D1694: a quinazoline antifolate which inhibits thymidylate synthase

1992 • 42 citations

Thymidylate synthase inhibitors: The in vitro activity of a series of heterocyclic benzoyl ring modified 2-desamino-2-methyl-N10-substituted-5,8-dideazafolates

1991 • 42 citations

The Role of the Reduced-Folate Carrier and Metabolism to Intracellular Polyglutamates for the Activity of ICI D1694

1993 • 42 citations

The renal effects of N10-propargyl-5,8-dideazafolic acid (CB3717) and a non-nephrotoxic analogue ICI D1694, in mice

1991 • 41 citations

The measurement of polyglutamate metabolites of the thymidylate synthase inhibitoR, ICI D1694, in mouse and human cultured cells

1993 • 36 citations

Differing specificities for 4-aminofolate analogues of folylpolyglutamyl synthetase from tumors and proliferative intestinal epithelium of the mouse with significance for selective antitumor action.

1990 • 34 citations

Induction of remission in hepatocellular carcinoma with a new thymidylate synthase inhibitor, CB3717

1987 • 32 citations

Recent preclinical and clinical studies with the thymidylate synthase inhibitor N10-propargyl-5,8-dideazafolic acid (CB 3717).

1987 • 29 citations

The pharmacokinetics of the quinazoline antifolate ICID 1694 in mice and rats

1991 • 28 citations

The Antitumour Activity of ZD9331, a Non-Polyglutamatable Quinazoline Thymidylate Synthase Inhibitor

1995 • 26 citations

Quinazoline antifolates inhibiting thymidylate synthase: synthesis of four oligo(L-.gamma.-glutamyl) conjugates of N10-propargyl-5,8-dideazafolic acid and their enzyme inhibition

1989 • 26 citations

ICI D1694, An Inhibitor of Thymidylate Synthase for Clinical Study

1991 • 25 citations

Phase II study of the thymidylate synthetase inhibitor CB3717 (N10-propargyl-5,8-dideazafolic acid) in colorectal cancer

1988 • 19 citations

Biological activity of a novel rationally designed lipophilic thymidylate synthase inhibitor

1994 • 17 citations

Quinazoline thymidylate synthase inhibitors: methods for assessing the contribution of polyglutamation to their in vitro activity.

1995 • 16 citations

Anticancer Drugs: Antimetabolite Metabolism and Natural Anticancer Agents

1994 • 15 citations

Use of Murine L5178Y Lymphoma Thymidine Kinase Mutants for in Vitro and in Vivo Antitumour Efficacy Evaluation of Novel Thymidylate Synthase Inhibitors

1993 • 13 citations

Comparison of basic fibroblast growth factor levels in clone A human colon cancer cells in vitro with levels in xenografted tumours

1995 • 11 citations

The Measurement of Deoxynucleotide (dNTP) Pools by Radioimmunoassay (RIA)

1995 • 11 citations

Quinazoline-based thymidylate synthase inhibitors: relationship between structural modifications and polyglutamation.

1995 • 9 citations

The Toxicity of ICI D1694 in Man and Mouse

1993 • 7 citations

Influence of intracellular polyglutamation on the cytotoxicity of the thymidylate synthase inhibitor 1843U89

1993 • 5 citations

Studies on the Cross-Resistance of Folylpolyglutamate Synthetase-Deficient, Methotrexate-Resistant CCRF-CEM Human Leukemia Sublines

1993 • 4 citations