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Dihydrofolate reductase
A dihydrofolate reductase that is encoded in the genome of rat. [PRO:DAN]
Synonyms
EC 1.5.1.3
Research
Bioassay Publications (67)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 14 (20.90) | 18.7374 |
| 1990's | 30 (44.78) | 18.2507 |
| 2000's | 19 (28.36) | 29.6817 |
| 2010's | 4 (5.97) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (27)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| trimethoprim | Rattus norvegicus (Norway rat) | Activity | 180.0000 | 1 | 1 |
Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Structural studies on bioactive compounds. 34. Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-03, Volume: 38, Issue:5, 1995
2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity.Journal of medicinal chemistry, , Dec-23, Volume: 37, Issue:26, 1994
Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cJournal of medicinal chemistry, , Volume: 32, Issue:11, 1989
Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Design, synthesis, biological evaluation and computational investigation of novel inhibitors of dihydrofolate reductase of opportunistic pathogens.Bioorganic & medicinal chemistry, , May-01, Volume: 18, Issue:9, 2010
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
The effect of 5-alkyl modification on the biological activity of pyrrolo[2,3-d]pyrimidine containing classical and nonclassical antifolates as inhibitors of dihydrofolate reductase and as antitumor and/or antiopportunistic infection agents.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Folate-synthesizing enzyme system as target for development of inhibitors and inhibitor combinations against Candida albicans-synthesis and biological activity of new 2,4-diaminopyrimidines and 4'-substituted 4-aminodiphenyl sulfones.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
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, , Mar-11, Volume: 47, Issue:6, 2004
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
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, , Apr-24, Volume: 46, Issue:9, 2003
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines: marked improvement in potency relative to trimethoprim and species selectivityJournal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jul-01, Volume: 42, Issue:13, 1999
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Selective Pneumocystis carinii dihydrofolate reductase inhibitors: design, synthesis, and biological evaluation of new 2,4-diamino-5-substituted-furo[2,3-d]pyrimidines.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
2,4-Diaminothieno[2,3-d]pyrimidine lipophilic antifolates as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and dihydrofolate reductase inhibitory activities of 2,4-diamino-5-deaza and 2,4-diamino-5,10-dideaza lipophilic antifolates.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Synthesis and biological evaluation of nonclassical 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines with novel side chain substituents as potential inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolate reductases from rat liver, Pneumocystis carinii, and Toxoplasma gondii.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Mar-29, Volume: 39, Issue:7, 1996
Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-03, Volume: 38, Issue:5, 1995
Novel 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolate inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
6-substituted 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
2,4-Diaminopyrido[3,2-d]pyrimidine inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity.Journal of medicinal chemistry, , Dec-23, Volume: 37, Issue:26, 1994
Synthesis of 5-methyl-5-deaza nonclassical antifolates as inhibitors of dihydrofolate reductases and as potential antipneumocystis, antitoxoplasma, and antitumor agents.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 14. 2,3-Dihydro-1-(2,4-diamino-5-pyrimidyl)-1H-indenes as conformationally restricted analogues of trimethoprim.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Receptor-based design of novel dihydrofolate reductase inhibitors: benzimidazole and indole derivatives.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 10. 2,4-Diamino-5-(6-quinolylmethyl)- and -[(tetrahydro-6-quinolyl)methyl]pyrimidine derivatives. Further specificity studies.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 13. Some alkenyl derivatives with high in vitro activity against anaerobic organisms.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 9. Lipophilic trimethoprim analogues as antigonococcal agents.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 8. The 3,4,5-triethyl isostere of trimethoprim. A study of specificity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 7. Analysis of the effect of 3,5-dialkyl substituent size and shape on binding to four different dihydrofolate reductase enzymes.Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogues.Journal of medicinal chemistry, , Volume: 28, Issue:3, 1985
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 5. 3',5'-Dimethoxy-4'-substituted-benzyl analogues of trimethoprim.Journal of medicinal chemistry, , Volume: 24, Issue:8, 1981
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogues.Journal of medicinal chemistry, , Volume: 23, Issue:4, 1980
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 4. 6-Substituted trimethoprim derivatives from phenolic Mannich intermediates. Application to the synthesis of trimethoprim and 3,5-dialkylbenzyl analogues.Journal of medicinal chemistry, , Volume: 23, Issue:5, 1980
Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 18, Issue:2, 2010
The effect of 5-alkyl modification on the biological activity of pyrrolo[2,3-d]pyrimidine containing classical and nonclassical antifolates as inhibitors of dihydrofolate reductase and as antitumor and/or antiopportunistic infection agents.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Design and synthesis of classical and nonclassical 6-arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as antifolates.Journal of medicinal chemistry, , Jun-28, Volume: 50, Issue:13, 2007
Design, synthesis, and biological evaluation of 2,4-diamino-5-methyl-6-substituted-pyrrolo[2,3-d]pyrimidines as dihydrofolate reductase inhibitors.Journal of medicinal chemistry, , Jul-01, Volume: 47, Issue:14, 2004
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
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, , Apr-05, Volume: 14, Issue:7, 2004
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
Structural studies on bioactive compounds. 34. Design, synthesis, and biological evaluation of triazenyl-substituted pyrimethamine inhibitors of Pneumocystis carinii dihydrofolate reductase.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Structure-based design of selective inhibitors of dihydrofolate reductase: synthesis and antiparasitic activity of 2, 4-diaminopteridine analogues with a bridged diarylamine side chain.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jul-01, Volume: 42, Issue:13, 1999
Synthesis and biological activities of tricyclic conformationally restricted tetrahydropyrido annulated furo[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Selective Pneumocystis carinii dihydrofolate reductase inhibitors: design, synthesis, and biological evaluation of new 2,4-diamino-5-substituted-furo[2,3-d]pyrimidines.Journal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Structural studies on bioactive compounds. 28. Selective activity of triazenyl-substituted pyrimethamine derivatives against Pneumocystis carinii dihydrofolate reductase.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Synthesis and biological activities of conformationally restricted, tricyclic nonclassical antifolates as inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Synthesis and dihydrofolate reductase inhibitory activities of 2,4-diamino-5-deaza and 2,4-diamino-5,10-dideaza lipophilic antifolates.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Conformationally restricted analogues of trimethoprim: 2,6-diamino-8-substituted purines as potential dihydrofolate reductase inhibitors from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolate reductases from rat liver, Pneumocystis carinii, and Toxoplasma gondii.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
2,4-diamino-5-deaza-6-substituted pyrido[2,3-d]pyrimidine antifolates as potent and selective nonclassical inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Mar-29, Volume: 39, Issue:7, 1996
Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-03, Volume: 38, Issue:5, 1995
Novel 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolate inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
6-substituted 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines as inhibitors of dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
2,4-Diaminopyrido[3,2-d]pyrimidine inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
Nonclassical 2,4-diamino-6-(aminomethyl)-5,6,7,8-tetrahydroquinazoline antifolates: synthesis and biological activities.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity.Journal of medicinal chemistry, , Dec-23, Volume: 37, Issue:26, 1994
Synthesis of 5-methyl-5-deaza nonclassical antifolates as inhibitors of dihydrofolate reductases and as potential antipneumocystis, antitoxoplasma, and antitumor agents.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
2,4-Diaminothieno[2,3-d]pyrimidine analogues of trimetrexate and piritrexim as potential inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 14. 2,3-Dihydro-1-(2,4-diamino-5-pyrimidyl)-1H-indenes as conformationally restricted analogues of trimethoprim.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 8. The 3,4,5-triethyl isostere of trimethoprim. A study of specificity.Journal of medicinal chemistry, , Volume: 30, Issue:11, 1987
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 7. Analysis of the effect of 3,5-dialkyl substituent size and shape on binding to four different dihydrofolate reductase enzymes.Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
N9-substituted 2,4-diaminoquinazolines: synthesis and biological evaluation of lipophilic inhibitors of pneumocystis carinii and toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.Journal of medicinal chemistry, , Jun-30, Volume: 48, Issue:13, 2005
Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase.Journal of medicinal chemistry, , May-06, Volume: 47, Issue:10, 2004
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, , Mar-11, Volume: 47, Issue:6, 2004
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, , Apr-05, Volume: 14, Issue:7, 2004
Synthesis and biological evaluation of 2,4-diamino-6-(arylaminomethyl)pyrido[2,3-d]pyrimidines as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase and as antiopportunistic infection and antitumor agents.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
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, , Apr-24, Volume: 46, Issue:9, 2003
Inhibition of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductases by 2,4-diamino-5-[2-methoxy-5-(omega-carboxyalkyloxy)benzyl]pyrimidines: marked improvement in potency relative to trimethoprim and species selectivityJournal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.Journal of medicinal chemistry, , Jul-19, Volume: 44, Issue:15, 2001
Synthesis and antiparasitic and antitumor activity of 2, 4-diamino-6-(arylmethyl)-5,6,7,8-tetrahydroquinazoline analogues of piritrexim.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jul-01, Volume: 42, Issue:13, 1999
6-Substituted 2,4-diaminopyrido[3,2-d]pyrimidine analogues of piritrexim as inhibitors of dihydrofolate reductase from rat liver, Pneumocystis carinii, and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Nonclassical 2,4-diamino-5-aryl-6-ethylpyrimidine antifolates: activity as inhibitors of dihydrofolate reductase from Pneumocystis carinii and Toxoplasma gondii and as antitumor agents.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Synthesis and biological activities of conformationally restricted, tricyclic nonclassical antifolates as inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Synthesis and dihydrofolate reductase inhibitory activities of 2,4-diamino-5-deaza and 2,4-diamino-5,10-dideaza lipophilic antifolates.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Conformationally restricted analogues of trimethoprim: 2,6-diamino-8-substituted purines as potential dihydrofolate reductase inhibitors from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Sep-12, Volume: 40, Issue:19, 1997
Synthesis and biological evaluation of nonclassical 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines with novel side chain substituents as potential inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
Nonclassical 2,4-diamino-8-deazafolate analogues as inhibitors of dihydrofolate reductases from rat liver, Pneumocystis carinii, and Toxoplasma gondii.Journal of medicinal chemistry, , Apr-26, Volume: 39, Issue:9, 1996
Lipophilic antifolates as agents against opportunistic infections. 1. Agents superior to trimetrexate and piritrexim against Toxoplasma gondii and Pneumocystis carinii in in vitro evaluations.Journal of medicinal chemistry, , Mar-15, Volume: 39, Issue:6, 1996
2,4-Diamino-5-substituted-quinazolines as inhibitors of a human dihydrofolate reductase with a site-directed mutation at position 22 and of the dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-03, Volume: 38, Issue:5, 1995
Novel 2,4-diamino-5-substituted-pyrrolo[2,3-d]pyrimidines as classical and nonclassical antifolate inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
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