Literature summary for 1.5.1.3 extracted from

Gangjee, A.; Jain, H.D.; Queener, S.F.; Kisliuk, R.L.
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 (2008), J. Med. Chem., 51, 4589-4600.

Search for more literature for 1.5.1.3

Inhibitors

Inhibitors	Comment	Organism	Structure
2,4-diamino-5-isopropyl-6-(phenylsulfanyl)-7H-pyrrolo[2,3-d]pyrimidine	-	Toxoplasma gondii
2,4-diamino-5-isopropyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine	evaluation of cytotoxicity against 17 different tumor cell lines	Homo sapiens
2,4-diamino-5-isopropyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine	-	Pneumocystis carinii
2,4-diamino-5-isopropyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine	-	Rattus norvegicus
2,4-diamino-5-propyl-6-(1'-naphthylsulfanyl)-7H-pyrrolo[2,3-d]pyrimidine	-	Toxoplasma gondii
2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine	evaluation of cytotoxicity against 17 different tumor cell lines. GI values are below 100 nM	Homo sapiens
2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine	-	Pneumocystis carinii
2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine	-	Rattus norvegicus
methotrexate	-	Toxoplasma gondii
pemetrexed	-	Toxoplasma gondii
pyrimethamine	-	Toxoplasma gondii
trimetrexate	-	Pneumocystis carinii
trimetrexate	-	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P00374	-	-
Pneumocystis carinii	-	-	-
Rattus norvegicus	-	-	-
Toxoplasma gondii	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
cell culture	evaluation of cytotoxicity of compounds 2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine and 2,4-diamino-5-isopropyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine against 17 different tumor cell lines. GI values of compound 2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine are below 100 nM	Homo sapiens	-
liver	-	Rattus norvegicus	-
liver	-	Toxoplasma gondii	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000003	-	37°C	Rattus norvegicus	trimetrexate
0.00000311	-	37°C	Pneumocystis carinii	2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine
0.0000048	-	37°C	Pneumocystis carinii	2,4-diamino-5-isopropyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine
0.000011	-	37°C	Toxoplasma gondii	methotrexate
0.000042	-	37°C	Pneumocystis carinii	trimetrexate
0.000058	-	37°C	Toxoplasma gondii	2,4-diamino-5-propyl-6-(1'-naphthylsulfanyl)-7H-pyrrolo[2,3-d]pyrimidine
0.00006	-	37°C	Rattus norvegicus	2,4-diamino-5-propyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine
0.000064	-	37°C	Toxoplasma gondii	2,4-diamino-5-isopropyl-6-(phenylsulfanyl)-7H-pyrrolo[2,3-d]pyrimidine
0.00008	-	37°C	Toxoplasma gondii	pyrimethamine
0.000186	-	37°C	Rattus norvegicus	2,4-diamino-5-isopropyl-6-arylthio-7H-pyrrolo[2,3-d]pyrimidine
0.00046	-	37°C	Toxoplasma gondii	pemetrexed

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Release 2023.1 (January 2023)