Výsledky vyhledávání - "Ronald A. Forsch"

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

Autor: Joel E. Wright, Ronald A. Forsch, Andre Rosowsky

Publikováno v: Journal of Medicinal Chemistry. 47:6958-6963

Heretofore unknown analogues of aminopterin (AMT) and methotrexate (MTX) in which free rotation of the amide bond between the phenyl ring and amino acid side chain is prevented by a CH(2) bridge were synthesized and tested for in vitro antifolate act

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12d504c1d4b4da60f3a8545a352b6b26
https://doi.org/10.1021/jm040122s

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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

Autor: Sherry F. Queener, Andre Rosowsky, Ronald A. Forsch

Publikováno v: Journal of Medicinal Chemistry. 46:1726-1736

As part of an ongoing effort to discover novel small-molecule antifolates combining the enzyme-binding species selectivity of trimethoprim (TMP) with the potency of piritrexim (PTX), 10 previously unreported 2,4-diamino-5-(2'-methoxy-5'-substituted)b

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https://doi.org/10.1021/jm020466n

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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

Autor: Ronald A. Forsch, Sherry F. Queener, Andre Rosowsky

Publikováno v: Journal of Medicinal Chemistry. 45:233-241

A series of previously undescribed 2,4-diamino-5-[2-methoxy-5-alkoxybenzyl]pyrimidines (3a-e) and 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines (3f-k) with up to eight CH2 groups in the alkoxy or omega-carboxyalkyloxy side chai

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4b351c54dba1c0708545040d06a9c704
https://doi.org/10.1021/jm010407u

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

Autor: Chitra M. Vaidya, Andre Rosowsky, Joel E. Wright, Ronald A. Forsch, Henry Bader

Publikováno v: Journal of Medicinal Chemistry. 43:1620-1634

Seven Nα-(4-amino-4-deoxypteroyl)-Nδ-hemiphthaloyl-l-ornithine (2, PT523) analogues were synthesized by modifications of the literature synthesis of the corresponding AMT (1) analogues and were tested as inhibitors of tumor cell growth. In growth a

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https://doi.org/10.1021/jm990630f

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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 Nα-(4-amino-4-deoxypteroyl)-Nδ-hemiphthaloyl-l-ornithine

Autor: Chitra M. Vaidya, Andre Rosowsky, Joel E. Wright, Ronald A. Forsch

Publikováno v: Pharmacology & Therapeutics. 85:191-205

N a -(4-Amino-4-deoxypteroyl)- N d -hemiphthaloyl- L -ornithine (PT523) is an unusually tight-binding dihydrofolate reductase (DHFR) inhibitor and is efficiently taken up into cells via the reduced folate carrier (RFC). Unlike classical DHFR inhibito

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https://doi.org/10.1016/s0163-7258(99)00055-8

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

Autor: Ronald A. Forsch, Andre Rosowsky

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 42:1103-1117

A synthesis of the mono-, di-, and tri[ 15 N]glutamate forms of the potent de novo purine synthesis inhibitor and anticancer agent (6R,6S)-5,10-dideaza-5,6,7,8-tetrahydrofolate (6R,6S-DDATHF) from (6R,6S)-5,10-dideaza-5,6,7,8-tetrahydropteroic acid i

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https://doi.org/10.1002/(sici)1099-1344(199911)42:11<1103::aid-jlcr269>3.0.co

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

Autor: Ronald A. Forsch, Andrew T. Papoulis, Andre Rosowsky, Sherry F. Queener

Publikováno v: Journal of Medicinal Chemistry. 42:1007-1017

Nineteen previously undescribed 2,4-diamino-6-(arylmethyl)-5,6,7, 8-tetrahydroquinazolines (5a-m, 10-12) were synthesized as part of a larger effort to assess the therapeutic potential of lipophilic dihydrofolate reductase (DHFR) inhibitors against o

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https://doi.org/10.1021/jm980572i

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Synthesis of L-2-(N-Pteroylamino )-3-(N -phosphonoacetyl)aminopropanoic Acid as an Analogue of the Putative Phosphorylated Intermediate in the γ-Glutamation of Folic Acid by Folylpolyglutamate Synthetase

Autor: Henry Bader, Andre Rosowsky, Ronald A. Forsch

Publikováno v: Pteridines, Vol 10, Iss 1, Pp 39-46 (1999)

L-2-(N-Pteroyl)amino-3-(N-phosphonoacetyl)aminopropanoic acid was synthesized as an analogue of the putative y-phosphorylated intermediate in the enzyme-catalyzed γ-glutamation of folic acid by folylpolyglutamate synthetase (FPGS). N-(Benzyloxycarbo

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https://doi.org/10.1515/pteridines.1999.10.1.39

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

Autor: Chitra M. Vaidya, Ronald A. Forsch, Andre Rosowsky, Clara E. Mota, Henry Bader, Joel E. Wright, Cindy S. Chen, Jorge Pardo, Ying-Nan Chen

Publikováno v: Journal of Medicinal Chemistry. 41:5310-5319

Six new B-ring analogues of the nonpolyglutamatable antifolate Nα-(4-amino-4-deoxypteroyl)-Nδ-hemiphthaloyl-l-ornithine (PT523, 3) were synthesized with a view to determining the effect of modifications at the 5- and/or 8-position on dihydrofolate

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https://doi.org/10.1021/jm980477+

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Synthesis of 2,4-Diaminopteridines with Bulky Lipophilic Groups at the 6-Position as Inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mammalian Dihydrofolate Reductase

Autor: Andre Rosowsky, Ronald A. Forsch, Joseph R. Bertino, Sherry F. Queener

Publikováno v: Pteridines, Vol 8, Iss 3, Pp 173-187 (1997)

SummaryTen previously undescribed 2,4-diamino-6-(2-naphthylamino )methylpteridines with lipophilic chlorine or long-chain alkyl groups on the naphthyl moiety and either hydrogen or a methyl group on N 10 were synthesized from the appropriate 2-naphth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::516f84ec33675ad0797ae68f7e3f3d65
https://doi.org/10.1515/pteridines.1997.8.3.173

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