Search Results - "Forsch, Ronald A"

Preliminary in vitro studies on two potent, water-soluble trimethoprim analogues with exceptional species selectivity against dihydrofolate reductase from Pneumocystis carinii and Mycobacterium avium by Forsch, Ronald A., Queener, Sherry F., Rosowsky, Andre

“…2,4-Diamino-5-[3′,4′-dimethoxy-5′-(5-carboxy-1-pentynyl)]benzylpyrimidine ( 6) and 2,4-diamino-5-[3′,4′-dimethoxy-5′-(4-carboxyphenylethynyl)benzylpyrimidine (…”
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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 by Chan, David C. M, Fu, Hongning, Forsch, Ronald A, Queener, Sherry F, Rosowsky, Andre

“…As part of a search for dihydrofolate reductase (DHFR) inhibitors combining the high potency of piritrexim (PTX) with the high antiparasitic vs mammalian…”
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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 by Rosowsky, Andre, Forsch, Ronald A, Queener, Sherry F

“…As part of an ongoing effort to discover novel small-molecule antifolates combining the enzyme-binding species selectivity of trimethoprim (TMP) with the…”
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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 by Rosowsky, Andre, Forsch, Ronald A, Sibley, Carol Hopkins, Inderlied, Clark B, Queener, Sherry F

“…In a continuing effort to design small-molecule inhibitors of dihydrofolate reductase (DHFR) that combine the enzyme-binding selectivity of…”
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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 by Rosowsky, Andre, Forsch, Ronald A, Queener, Sherry F

“…A series of previously undescribed 2,4-diamino-5-[2-methoxy-5-alkoxybenzyl]pyrimidines (3a−e) and…”
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Synthesis and in Vitro Antifolate Activity of Rotationally Restricted Aminopterin and Methotrexate Analogues by Rosowsky, Andre, Forsch, Ronald A, Wright, Joel E

“…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…”
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Synthesis and In Vitro Antitumor Activity of Thiophene Analogues of 5-Chloro-5,8-dideazafolic Acid and 2-Methyl-2-desamino-5-chloro-5,8-dideazafolic Acid by Forsch, Ronald A., Wright, Joel E., Rosowsky, Andre

“…N-[5-[ N-(2-Amino-5-chloro-3,4-dihydro-4-oxoquinazolin-6-yl)methylamino]-2-thenoyl]- l-glutamic acid ( 6 ) and N-[5-[…”
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Synthesis and Antiparasitic and Antitumor Activity of 2,4-Diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline Analogues of Piritrexim by Rosowsky, Andre, Papoulis, Andrew T, Forsch, Ronald A, Queener, Sherry F

“…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…”
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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 by Rosowsky, Andre, Forsch, Ronald A, Sibley, Carol Hopkins, Inderlied, Clark B, Queener, Sherry F

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Synthesis and Antiparasitic and Antitumor Activity of 2,4-Diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline Analogues of Piritrexim by Rosowsky, Andre, Papoulis, Andrew, Forsch, Ronald A, Queener, Sherry F

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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 by Rosowsky, Andre, Wright, Joel E, Vaidya, Chitra M, Forsch, Ronald A, Bader, Henry

“…Seven N α-(4-amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine (2, PT523) analogues were synthesized by modifications of the literature synthesis of the…”
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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) by Rosowsky, Andre, Wright, Joel E, Vaidya, Chitra M, Bader, Henry, Forsch, Ronald A, Mota, Clara E, Pardo, Jorge, Chen, Cindy S, Chen, Ying-Nan

“…Six new B-ring analogues of the nonpolyglutamatable antifolate N α-(4-amino-4-deoxypteroyl)-N δ-hemiphthaloyl-l-ornithine (PT523, 3) were synthesized with a…”
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2,4-Diaminopyrido[3,2-d]pyrimidine Inhibitors of Dihydrofolate Reductase from Pneumocystis carinii and Toxoplasma gondii by Rosowsky, Andre, Forsch, Ronald A, Queener, Sherry F

“…Six previously unknown 2,4-diamino-6-(anilinomethyl)- and 2,4-diamino-6-[(N-methylanilino)-methyl]pyrido[3,2-d]pyrimidines (5-10) were synthesized from…”
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5-Deazafolate Analogues with a Rotationally Restricted Glutamate or Ornithine Side Chain:  Synthesis and Binding Interaction with Folylpolyglutamate Synthetase by Rosowsky, Andre, Forsch, Ronald A, Null, Allison, Moran, Richard G

“…Rotationally restricted analogues of 5-deazapteroyl-l-glutamate and (6R,6S)-5-deaza-5,6,7,8-tetrahydropteroyl-l-glutamate with a one-carbon bridge between the…”
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Side chain modified 5-deazatolate and 5-deazatetrahydrotolate analogs as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyltransferase inhibitors: synthesis and in vitro biological evaluation. 47. N-[4-[[(3,4-Dihydro-4-oxo-1,2,3-benzotriazin-6-yl)methyl]amino]benzoyl-L-glutamic acid, a novel a-ring analog of 2-desamino-5,8-dideazafolic acid by Rosowsky, Andre, Forsch, Ronald A, Moran, Richard G

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(6R,6S)-5,8,10-Trideaza-5,6,7,8-tetrahydrofolate and (6R,6S)-5,8,10-trideaza-5,6,7,8-tetrahydropteroyl-L-ornithine as potential antifolates and antitumor agents. 35 by Rosowsky, Andre, Forsch, Ronald A, Moran, Richard G

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

“…Ten previously undescribed 2,4-diamino-6-(2-naphthylamino )methylpteridines with lipophilic chlorine or long-chain alkyl groups on the naphthyl moiety and…”
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First use of the Taylor pteridine synthesis as a route to polyglutamate derivatives of antifolates. 46. Side chain modified 5-deazafolate and 5-deazatetrahydrofolate analogs as mammalian folylpolyglutamate synthetase and glycinamide ribonucleotide formyl transferase inhibitors: synthesis and in vitro biological evaluation by Rosowsky, Andre, Forsch, Ronald A, Reich, Valerie E, Freisheim, James H, Moran, Richard G

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Methotrexate analogs. 21. Selective cleavage of 2-(trimethylsilyl)ethyl esters in the presence of N-tert-butyloxycarbonyl groups during the synthesis of protected dilysine and trilysine derivatives of methotrexate by Forsch, Ronald A, Rosowsky, Andre

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Synthesis and biological activity of the 2-desamino and 2-desamino-2-methyl analogs of aminopterin and methotrexate by Rosowsky, Andre, Forsch, Ronald A, Moran, Richard G, Freisheim, James H

“…The previously undescribed 2-desamino and 2-desamino-2-methyl analogues of aminopterin (AMT) and methotrexate (MTX) were synthesized from…”
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