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Literature summary for 1.5.1.3 extracted from

  • Gangjee, A.; Li, W.; Yang, J.; Kisliuk, R.L.
    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 (2008), J. Med. Chem., 51, 68-76.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.5.1.3

Inhibitors

Inhibitors Comment Organism Structure
2-amino-5-(4-bromobenzyl)-6-methyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
 Toxoplasma gondii
2-amino-5-(4-chlorobenzyl)-6-methyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
 Toxoplasma gondii
2-amino-5-(4-methoxybenzyl)-6-methyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
 Toxoplasma gondii
2-amino-6-methyl-5-(4-nitrobenzyl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
 Toxoplasma gondii
2-amino-6-methyl-5-[4-(trifluoromethoxy)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
-
 Toxoplasma gondii
methotrexate
-
 Homo sapiens
methotrexate
-
 Toxoplasma gondii
N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl)-L-glutamic acid dual inhibitor of both dihydrofolate reductase and thymidylate synthase. Inhibitory to Toxoplasma gondii dihydrofolate reductase, little inhibition of Escherichia coli enzyme Homo sapiens
N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl)-L-glutamic acid inhibitory to human dihydrofolate reductase, little inhibition of Escherichia coli enzyme Toxoplasma gondii

Organism

Organism UniProt Comment Textmining
Homo sapiens P00374
-
-
Toxoplasma gondii
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00002
-
 37°C Homo sapiens methotrexate
0.000023
-
 37°C Toxoplasma gondii N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl)-L-glutamic acid
0.000033
-
 37°C Toxoplasma gondii methotrexate
0.00012
-
 37°C Homo sapiens N-(4-[(2-amino-6-methyl-4-oxo-3,4-dihydro-5H-pyrrolo[3,2-d]pyrimidin-5-yl)methyl]benzoyl)-L-glutamic acid
0.00027
-
-
 Toxoplasma gondii 2-amino-5-(4-bromobenzyl)-6-methyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.0003
-
-
 Toxoplasma gondii 2-amino-6-methyl-5-[4-(trifluoromethoxy)benzyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00033
-
-
 Toxoplasma gondii 2-amino-6-methyl-5-(4-nitrobenzyl)-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.00035
-
-
 Toxoplasma gondii 2-amino-5-(4-chlorobenzyl)-6-methyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
0.0035
-
-
 Toxoplasma gondii 2-amino-5-(4-methoxybenzyl)-6-methyl-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one