New pathways from pteridines. Design and synthesis of a new class of potent and selective antitumor agents

Temporary Remissions in Acute Leukemia in Children Produced by Folic Acid Antagonist, 4-Aminopteroyl-Glutamic Acid (Aminopterin)

1948 • 1,702 citations

Chemistry and biology of pteridines

1956 • 1,263 citations

Chemistry and biology of pteridines 1986

1987 • 335 citations

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

1981 • 242 citations

A new folate antimetabolite, 5,10-dideaza-5,6,7,8-tetrahydrofolate is a potent inhibitor of de novo purine synthesis

1989 • 234 citations

Relative frequency and kinetic properties of transport-defective phenotypes among methotrexate-resistant L1210 clonal cell lines derived in vivo.

1981 • 191 citations

Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin

1985 • 150 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

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

1986 • 103 citations

Modulation of anti-metabolite effects

1984 • 96 citations

Acquired methotrexate resistance in lymphoblasts resulting from altered kinetic properties of dihydrofoltate reductase

1977 • 95 citations

Kinetics and mechanism of interaction of 10-propargyl-5,8-dideazafolate with thymidylate synthase

1986 • 89 citations

The Role of Dihydrofolic Reductase in the Metabolism of One-Carbon Units^*

1963 • 81 citations

Synthesis and biological activity of L-5-deazafolic acid and L-deazaaminopterin: synthetic strategies to 5-deazapteridines

1983 • 73 citations

Similar differential for total polyglutamylation and cytotoxicity among various folate analogues in human and murine tumor cells in vitro.

1985 • 72 citations

Convergent and efficient palladium-effected synthesis of 5, 10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF)

1989 • 68 citations

Preparation of 6-(bromomethyl)-2,4-pteridinediamine hydrobromide and its use in improved syntheses of methotrexate and related compounds

1977 • 64 citations

A methotrexate insensitive variant of folate reductase present in two lines of methotrexate-resistant L5178Y cells

1980 • 61 citations

Methotrexate resistance in al L1210 cell line resulting from increased dihydrofolate reductase, decreased thymidylate synthetase activity, and normal membrane transport. Computer simulations based on network thermodynamics.

1981 • 49 citations

Synthesis and antitumor activity of 5-deaza-5,6,7,8-tetrahydrofolic acid and its N10-substituted analogs

1989 • 44 citations

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

1985 • 44 citations

Membrane transport of methotrexate (NSC 740) and other folate compounds: relevance to rescue protocols

1975 • 43 citations

Pyrido[2,3-d]pyrimidines. The synthesis of the 5-deaza analogs of aminopterin, methotrexate, folic acid, and N10-methylfolic acid

1982 • 42 citations

5-Methyltetrahydrofolate transport by hepatoma cells and methotrexate-resistant sublines in culture.

1981 • 38 citations

Biological and biochemical properties of new anticancer folate antagonists

1987 • 38 citations

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.

1985 • 36 citations

A convenient synthesis of aminopterin and homologs via 6‐(bromomethyl)‐2,4‐diaminopteridine hydrobromide

1974 • 31 citations

Novel cycloaddition routes to fused heterocycles

1988 • 31 citations

Isolation and characterization of dihydrofolic acid reductase from methotrexate-sensitive and -resistant human cell lines.

1981 • 29 citations

Establishment of dihydrofolate reductase-increased human cell lines and relationship between dihydrofolate reductase levels and gene copy.

1983 • 26 citations

Über Pterinchemie. 44. Mitteilung. Eine eindeutige Synthese isomerenfreier Folsäure

1973 • 24 citations

A Convenant Synthesis of 6-Formyl-5-Deazapterin

1988 • 24 citations

Synthesis of 5-H-thieno[2,3-c]pyrrole

1986 • 23 citations

A retro-malonate addition reaction: synthesis of 3,4-condensed heteroaromatic pyrroles

1988 • 23 citations

A Facile Route to "Open Chain" Analogues of DDATHF

1989 • 21 citations

Antimetabolites in the chemotherapy of leukemia*1

1963 • 20 citations

Synthesis of 5,10‐dideazaminopterin

1986 • 20 citations

Diels-Alder Reactions of 6-Azapterins. An Alternative Strategy for the Synthesis of 5,10-Dideaza-5,6,7,8-tetrahydrofolic Acid (DDATHF)

1988 • 17 citations

A mechanism for the addition of multiple moles of glutamate by folylpolyglutamate synthetase

1984 • 13 citations

THE REACTION OF N-BROMOSUCCINIMIDE WITH SOME ALKYL PYRIDINES

1964 • 13 citations

Methotrexate-resistant human promyelocytic leukemia (HL-60) cells express a dihydrofolate reductase with altered properties associated with increased enzyme activity

1985 • 9 citations

Personal View

1977 • 3 citations