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Synthesis and Antiparasitic and Antitumor Activity of 2,4-Diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline Analogues of Piritrexim

Journal of medicinal chemistry, 1999-03, Vol.42 (6), p.1007-1017

1999

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2,4-Diaminopyrido[3,2-d]pyrimidine Inhibitors of Dihydrofolate Reductase from Pneumocystis carinii and Toxoplasma gondii

Journal of medicinal chemistry, 1995-07, Vol.38 (14), p.2615-2620

1995

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5-Deazafolate Analogues with a Rotationally Restricted Glutamate or Ornithine Side Chain: Synthesis and Binding Interaction with Folylpolyglutamate Synthetase

Journal of medicinal chemistry, 1999-09, Vol.42 (18), p.3510-3519

1999

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Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity

Molecular pharmacology, 1995-09, Vol.48 (3), p.459

1995

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Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium Dihydrofolate Reductases by 2,4-Diamino-5-[2-methoxy-5-(ω-carboxyalkyloxy)benzyl]pyrimidines: Marked Improvement in Potency Relative to Trimethoprim and Species Selectivity Relative to Piritrexim

Journal of medicinal chemistry, 2002-01, Vol.45 (1), p.233-241

2002

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

Molecular pharmacology, 1985-01, Vol.27 (1), p.156-166

1985

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N-[4-[[(3,4-dihydro-4-oxo-1,2,3-benzotriazin-6-yl)methyl]amino]benzoyl]-L-glutamic acid, a novel A-ring analogue of 2-desamino-5,8-dideazafolic acid

Journal of medicinal chemistry, 1992-07, Vol.35 (14), p.2626-2630

1992

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Regiospecific gamma-conjugation of methotrexate to poly(L-lysine). Chemical and biological studies

Molecular pharmacology, 1985-01, Vol.27 (1), p.141-147

1985

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Analogues of the Potent Nonpolyglutamatable Antifolate N α-(4-Amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine (PT523) with Modifications in the Side Chain, p-Aminobenzoyl Moiety, or 9,10-Bridge: Synthesis and in Vitro Antitumor Activity

Journal of medicinal chemistry, 2000-04, Vol.43 (8), p.1620-1634

2000

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Folic acid analogs lacking the 2-carbon are substrates for folylpolyglutamate synthetase and inhibit cell growth

Journal of medicinal chemistry, 1991-01, Vol.34 (1), p.461-463

1991

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Synthesis and Potent Antifolate Activity and Cytotoxicity of B-Ring Deaza Analogues of the Nonpolyglutamatable Dihydrofolate Reductase Inhibitor N α-(4-Amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine (PT523)

Journal of medicinal chemistry, 1998-12, Vol.41 (26), p.5310-5319

1998

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Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium

Bioorganic & medicinal chemistry letters, 2004-04, Vol.14 (7), p.1811-1815

2004

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

Journal of medicinal chemistry, 1984-10, Vol.27 (10), p.1263-1267

1984

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Synthesis of γ-[15N]-L-glutamyl derivatives of 5,10-dideazatetrahydrofolate

Journal of labelled compounds & radiopharmaceuticals, 1999-11, Vol.42 (11), p.1103-1117

1999

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Design, Synthesis, and Antifolate Activity of New Analogues of Piritrexim and Other Diaminopyrimidine Dihydrofolate Reductase Inhibitors with ω-Carboxyalkoxy or ω-Carboxy-1-alkynyl Substitution in the Side Chain

Journal of medicinal chemistry, 2005-06, Vol.48 (13), p.4420-4431

2005

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Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogs of aminopterin and methotrexate

Journal of medicinal chemistry, 1991-01, Vol.34 (1), p.227-234

1991

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Further Studies on 2,4-Diamino-5-(2‘,5‘-disubstituted benzyl)pyrimidines as Potent and Selective Inhibitors of Dihydrofolate Reductases from Three Major Opportunistic Pathogens of AIDS

Journal of medicinal chemistry, 2003-04, Vol.46 (9), p.1726-1736

2003

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Synthesis and in vitro biological activity of new deaza analogs of folic acid, aminopterin, and methotrexate with an L-ornithine side chain

Journal of medicinal chemistry, 1991-04, Vol.34 (4), p.1447-1454

1991

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The 2-desamino and 2-desamino-2-methyl analogs of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture

Journal of medicinal chemistry, 1989-03, Vol.32 (3), p.517-520

1989

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Methotrexate analogues. 32. Chain extension, alpha-carboxyl deletion, and gamma-carboxyl replacement by sulfonate and phosphonate: effect on enzyme binding and cell-growth inhibition

Journal of medicinal chemistry, 1988-07, Vol.31 (7), p.1326-1331

1988

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The effect of side-chain, para-aminobenzoyl region, and B-ring modifications on dihydrofolate reductase binding, influx via the reduced folate carrier, and cytotoxicity of the potent nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L- ornithine

Pharmacology & therapeutics (Oxford), 2000-03, Vol.85 (3), p.191-205

2000

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New 2,4-Diamino-5-(2‘,5‘-substituted benzyl)pyrimidines as Potential Drugs against Opportunistic Infections of AIDS and Other Immune Disorders. Synthesis and Species-Dependent Antifolate Activity

Journal of medicinal chemistry, 2004-03, Vol.47 (6), p.1475-1486

2004

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Analogues of the potent nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523) with modifications in the side chain, p-aminobenzoyl moiety, or 9,10-bridge: synthesis and in vitro antitumor activity

Journal of medicinal chemistry, 2000-04, Vol.43 (8), p.1620

2000

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Synthesis and in Vitro Antifolate Activity of Rotationally Restricted Aminopterin and Methotrexate Analogues

Journal of medicinal chemistry, 2004-12, Vol.47 (27), p.6958-6963

2004

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A new one-step synthesis of leucovorin from folic acid and of 5-formyl-5,6,7,8-tetrahydrohomofolic acid from homofolic acid using dimethylamine-borane in formic acid

Journal of organic chemistry, 1985-07, Vol.50 (14), p.2582-2583

1985

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Synthesis and Antiparasitic and Antitumor Activity of 2,4-Diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline Analogues of Piritrexim

2,4-Diaminopyrido[3,2-d]pyrimidine Inhibitors of Dihydrofolate Reductase from Pneumocystis carinii and Toxoplasma gondii

5-Deazafolate Analogues with a Rotationally Restricted Glutamate or Ornithine Side Chain: Synthesis and Binding Interaction with Folylpolyglutamate Synthetase

Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity

Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium Dihydrofolate Reductases by 2,4-Diamino-5-[2-methoxy-5-(ω-carboxyalkyloxy)benzyl]pyrimidines: Marked Improvement in Potency Relative to Trimethoprim and Species Selectivity Relative to Piritrexim

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

N-[4-[[(3,4-dihydro-4-oxo-1,2,3-benzotriazin-6-yl)methyl]amino]benzoyl]-L-glutamic acid, a novel A-ring analogue of 2-desamino-5,8-dideazafolic acid

Regiospecific gamma-conjugation of methotrexate to poly(L-lysine). Chemical and biological studies

Analogues of the Potent Nonpolyglutamatable Antifolate N α-(4-Amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine (PT523) with Modifications in the Side Chain, p-Aminobenzoyl Moiety, or 9,10-Bridge: Synthesis and in Vitro Antitumor Activity

Folic acid analogs lacking the 2-carbon are substrates for folylpolyglutamate synthetase and inhibit cell growth

Synthesis and Potent Antifolate Activity and Cytotoxicity of B-Ring Deaza Analogues of the Nonpolyglutamatable Dihydrofolate Reductase Inhibitor N α-(4-Amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine (PT523)

Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium

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

Synthesis of γ-[15N]-L-glutamyl derivatives of 5,10-dideazatetrahydrofolate

Design, Synthesis, and Antifolate Activity of New Analogues of Piritrexim and Other Diaminopyrimidine Dihydrofolate Reductase Inhibitors with ω-Carboxyalkoxy or ω-Carboxy-1-alkynyl Substitution in the Side Chain

Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogs of aminopterin and methotrexate

Further Studies on 2,4-Diamino-5-(2‘,5‘-disubstituted benzyl)pyrimidines as Potent and Selective Inhibitors of Dihydrofolate Reductases from Three Major Opportunistic Pathogens of AIDS

Synthesis and in vitro biological activity of new deaza analogs of folic acid, aminopterin, and methotrexate with an L-ornithine side chain

The 2-desamino and 2-desamino-2-methyl analogs of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture

Methotrexate analogues. 32. Chain extension, alpha-carboxyl deletion, and gamma-carboxyl replacement by sulfonate and phosphonate: effect on enzyme binding and cell-growth inhibition

The effect of side-chain, para-aminobenzoyl region, and B-ring modifications on dihydrofolate reductase binding, influx via the reduced folate carrier, and cytotoxicity of the potent nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L- ornithine

New 2,4-Diamino-5-(2‘,5‘-substituted benzyl)pyrimidines as Potential Drugs against Opportunistic Infections of AIDS and Other Immune Disorders. Synthesis and Species-Dependent Antifolate Activity

Analogues of the potent nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523) with modifications in the side chain, p-aminobenzoyl moiety, or 9,10-bridge: synthesis and in vitro antitumor activity

Synthesis and in Vitro Antifolate Activity of Rotationally Restricted Aminopterin and Methotrexate Analogues

A new one-step synthesis of leucovorin from folic acid and of 5-formyl-5,6,7,8-tetrahydrohomofolic acid from homofolic acid using dimethylamine-borane in formic acid

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