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Literature summary for 1.5.1.3 extracted from

  • Gangjee, A.; Jain, H.D.; Phan, J.; Lin, X.; Song, X.; McGuire, J.J.; Kisliuk, R.L.
    Dual inhibitors of thymidylate synthase and dihydrofolate reductase as antitumor agents: design, synthesis, and biological evaluation of classical and nonclassical pyrrolo[2,3-d]pyrimidine antifolates(1) (2006), J. Med. Chem., 49, 1055-1065.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-((4-[(2-amino-6-ethyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)thio]benzoyl)amino)pentanedioic acid 50% inhibition at 0.00042 mM, additionally inhibitory on thymidylate synthase Homo sapiens
(2S)-2-((4-[(2-amino-6-methyl-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)thio]benzoyl)amino)pentanedioic acid 50% inhibition at 0.0021 mM, additionally inhibitory on thymidylate synthase Homo sapiens
methotrexate 50% inhibition at 0.000022 mM Homo sapiens
pemetrexed i.e. LY231514, 50% inhibition at 0.0066 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00374
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