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Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity.
The transport properties and growth-inhibitory potential of 37 classic and novel antifolate compounds have been tested in vitro against human and murine cell lines expressing different levels of theExpand
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Endocytosis of GPI-linked membrane folate receptor-alpha
GPI-linked membrane folate receptors (MFRs) have been implicated in the receptor-mediated uptake of reduced folate cofactors and folate-based chemotherapeutic drugs. We have studied the biosyntheticExpand
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Hydroxylamine derivatives as potential antimalarial agents. 1. Hydroxamic acids.
  • J. Hynes
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 1 November 1970
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Improved synthesis and antitumor evaluation of 5,8-dideazaisofolic acid and closely related analogues.
A new synthetic route to 5,8-dideazaisofolic acid (IAHQ) is described which precludes the possibility of contamination due to its 4-amino counterpart 5,8-dideazaisoaminopterin. Substitution ofExpand
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Quinazolines as inhibitors of dihydrofolate reductase. 3. Analogs of pteroic and isopteroic acids.
A series of 19 quinazoline analogs of pteroic and isopteroic acid was prepared with particular emphasis being placed upon carboxylic acid esters. Each compound was evaluated as an inhibitor of theExpand
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Synthesis and biological evaluation of a fluorescent analogue of folic acid.
A fluorescein derivative of the lysine analogue of folic acid, N alpha-pteroyl-N epilson-(4'-fluoresceinthiocarbamoyl)-L-lysine (PLF), was synthesized as a probe for dihydrofolate reductase (DHFR)Expand
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Purification of mammalian tumor (L1210) thymidylate synthetase by affinity chromatography on stable biospecific adsorbent. Stabilization of the enzyme with neutral detergents.
Thymidylate synthetase from mouse leukemic L1210 cells was purified to electrophoretic homogeneity with 70% yield as a result of an affinity chromatography procedure based on reversibleExpand
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Quinazolines as inhibitors of dihydrofolate reductase. 4. Classical analogues of folic and isofolic acids.
A series of classical quinazoline analogues of folic and isofolic acids was evaluated for inhibitory activity against the dihydrofolate reductases from rat liver and from Streptococcus faecium.Expand
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Biochemical and antitumor effects of 5,8-dideazaisopteroylglutamate, a unique quinazoline inhibitor of thymidylate synthase.
Abstract The effects of 5,8-dideazaisopteroylglutamate ( N -[ p -{[(2-amino-4-hydroxy-6-quinazolinyl)amino]methyl}benzoyl]-l-glutamic acid) (IAHQ) on thymidylate synthase and dihydrofolate reductaseExpand
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