Proteins > Bifunctional dihydrofolate reductase-thymidylate synthase
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Bifunctional dihydrofolate reductase-thymidylate synthase
[no definition available]
Synonyms
DHFR-TS
Research
Bioassay Publications (59)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 27 (45.76) | 18.2507 |
| 2000's | 25 (42.37) | 29.6817 |
| 2010's | 7 (11.86) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| trimethoprim | Toxoplasma gondii | Activity | 2.8000 | 1 | 1 |
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
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
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
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
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
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
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
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
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
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
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
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 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
Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis.Journal of medicinal chemistry, , Mar-08, Volume: 50, Issue:5, 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
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 of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
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, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 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 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
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
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
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
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
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
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
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 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
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
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
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
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
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
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
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
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
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 of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
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
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, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 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
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-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
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
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
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
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 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
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-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
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-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
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
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
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
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
Recent advances in the chemistry and biology of pyridopyrimidines.European journal of medicinal chemistry, , May-05, Volume: 95, 2015
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
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
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
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
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 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
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
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
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
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 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
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-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 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
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-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-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
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
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
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
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
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
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 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
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
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
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
CoMFA and CoMSIA analyses of Pneumocystis carinii dihydrofolate reductase, Toxoplasma gondii dihydrofolate reductase, and rat liver dihydrofolate reductase.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
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
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
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
CoMFA and CoMSIA analyses of Pneumocystis carinii dihydrofolate reductase, Toxoplasma gondii dihydrofolate reductase, and rat liver dihydrofolate reductase.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
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
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
Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
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
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
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
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 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
Highly efficient ligands for dihydrofolate reductase from Cryptosporidium hominis and Toxoplasma gondii inspired by structural analysis.Journal of medicinal chemistry, , Mar-08, Volume: 50, Issue:5, 2007
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Synthesis of classical and nonclassical, partially restricted, linear, tricyclic 5-deaza antifolates.Journal of medicinal chemistry, , Nov-07, Volume: 45, Issue:23, 2002
Synthesis of N-[4-[1-ethyl-2-(2,4-diaminofuro[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Effect of C9-methyl substitution and C8-C9 conformational restriction on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
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
Effect of N9-methylation and bridge atom variation on the activity of 5-substituted 2,4-diaminopyrrolo[2,3-d]pyrimidines against dihydrofolate reductases from Pneumocystis carinii and Toxoplasma gondii.Journal of medicinal chemistry, , Mar-28, Volume: 40, Issue:7, 1997
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
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
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
Classical and nonclassical furo[2,3-d]pyrimidines as novel antifolates: synthesis and biological activities.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
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
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
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
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
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
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Synthesis, antifolate, and antitumor activities of classical and nonclassical 2-amino-4-oxo-5-substituted-pyrrolo[2,3-d]pyrimidines.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Design, synthesis, biological evaluation and X-ray crystal structure of novel classical 6,5,6-tricyclic benzo[4,5]thieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents.Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors.Journal of medicinal chemistry, , Jan-10, Volume: 51, Issue:1, 2008
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolJournal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005