Page last updated: 2024-08-07 15:30:36
Dihydrofolate reductase
[no definition available]
Synonyms
EC 1.5.1.3
Research
Bioassay Publications (41)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 26 (63.41) | 18.7374 |
| 1990's | 8 (19.51) | 18.2507 |
| 2000's | 6 (14.63) | 29.6817 |
| 2010's | 1 (2.44) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
Drugs with Other Measurements
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
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
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
On the structure selectivity problem in drug design. A comparative study of benzylpyrimidine inhibition of vertebrate and bacterial dihydrofolate reductase via molecular graphics and quantitative structure-activity relationships.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
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
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
Quantitative structure-activity relationships of 2, 4-diamino-5-(2-X-benzyl)pyrimidines versus bacterial and avian dihydrofolate reductase.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
On the structure selectivity problem in drug design. A comparative study of benzylpyrimidine inhibition of vertebrate and bacterial dihydrofolate reductase via molecular graphics and quantitative structure-activity relationships.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
Pteridine-sulfonamide conjugates as dual inhibitors of carbonic anhydrases and dihydrofolate reductase with potential antitumor activity.Bioorganic & medicinal chemistry, , Jul-15, Volume: 18, Issue:14, 2010
Novel boron-containing, nonclassical antifolates: synthesis and preliminary biological and structural evaluation.Journal of medicinal chemistry, , Jul-12, Volume: 50, Issue:14, 2007
Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
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
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
Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 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
Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[omega-(2-amino-4-substituted-6,7-dihydrocyclopenta [d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
Synthesis and biological evaluation of 8-deazahomofolic acid and its tetrahydro derivative.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogues of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase.Journal of medicinal chemistry, , Volume: 31, Issue:11, 1988
Folate analogues. 25. Synthesis and biological evaluation of N10-propargylfolic acid and its reduced derivatives.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
Synthesis and antifolate properties of 5,10-methylenetetrahydro-8,10-dideazaminopterin.Journal of medicinal chemistry, , Volume: 29, Issue:9, 1986
Folate analogues. 26. Syntheses and antifolate activity of 10-substituted derivatives of 5,8-dideazafolic acid and of the poly-gamma-glutamyl metabolites of N10-propargyl-5,8-dideazafolic acid (PDDF).Journal of medicinal chemistry, , Volume: 29, Issue:9, 1986
Synthesis and biological activity of resolved C-10 diastereomers of 10-methyl- and 10-ethyl-10-deazaminopterin.Journal of medicinal chemistry, , Volume: 29, Issue:6, 1986
A 1H NMR study of the interactions and conformations of rationally designed brodimoprim analogues in complexes with Lactobacillus casei dihydrofolate reductase.Journal of medicinal chemistry, , Volume: 27, Issue:12, 1984
Folate analogues. 21. Synthesis and antifolate and antitumor activities of N10-(cyanomethyl)-5,8-dideazafolic acid.Journal of medicinal chemistry, , Volume: 26, Issue:4, 1983
Methotrexate analogues. 20. Replacement of glutamate by longer-chain amino diacids: effects on dihydrofolate reductase inhibition, cytotoxicity, and in vivo antitumor activity.Journal of medicinal chemistry, , Volume: 26, Issue:12, 1983
10-Propargylaminopterin and alkyl homologues of methotrexate as inhibitors of folate metabolism.Journal of medicinal chemistry, , Volume: 25, Issue:7, 1982
Methotrexate analogues. 15. A methotrexate analogue designed for active-site-directed irreversible inactivation of dihydrofolate reductase.Journal of medicinal chemistry, , Volume: 25, Issue:8, 1982
Methotrexate analogues. 13. Chemical and pharmacological studies on amide, hydrazide, and hydroxamic acid derivatives of the glutamate side chain.Journal of medicinal chemistry, , Volume: 24, Issue:5, 1981
Folate analogues altered in the C9-N10 bridge region. 16. Synthesis and antifolate activity of 11-thiohomoaminopterin.Journal of medicinal chemistry, , Volume: 23, Issue:8, 1980
Methotrexate analogues. 12. Synthesis and biological properties of some aza homologues.Journal of medicinal chemistry, , Volume: 22, Issue:7, 1979
Methotrexate analogues. 9. Synthesis and biological properties of some 8-alkyl-7,8-dihydro analogues.Journal of medicinal chemistry, , Volume: 20, Issue:10, 1977
Folate analogues altered in the C9-N10 bridge region. 10-Oxafolic acid and 10-oxaaminopterin.Journal of medicinal chemistry, , Volume: 19, Issue:6, 1976
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
Effect of bridge region variation on antifolate and antitumor activity of classical 5-substituted 2,4-diaminofuro[2,3-d]pyrimidines.Journal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[omega-(2-amino-4-substituted-6,7-dihydrocyclopenta [d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
Synthesis and biological evaluation of poly-gamma-glutamyl metabolites of 10-deazaaminopterin and 10-ethyl-10-deazaaminopterin.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
Folate analogues. 32. Synthesis and biological evaluation of 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid and related compounds.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Folate analogues. 30. Synthesis and biological evaluation of N10-propargyl-5,8-dideaza-5,6,7,8-tetrahydrofolic acid and related compounds.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Folate analogues. 25. Synthesis and biological evaluation of N10-propargylfolic acid and its reduced derivatives.Journal of medicinal chemistry, , Volume: 29, Issue:7, 1986
Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis of classical, three-carbon-bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.Journal of medicinal chemistry, , Dec-30, Volume: 47, Issue:27, 2004
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and Journal of medicinal chemistry, , Feb-13, Volume: 46, Issue:4, 2003
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