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Literature summary for 2.1.2.2 extracted from

  • Wang, Y.; Cherian, C.; Orr, S.; Mitchell-Ryan, S.; Hou, Z.; Raghavan, S.; Matherly, L.H.; Gangjee, A.
    Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor alpha and inhibition of de novo purine nucleotide biosynthesis (2013), J. Med. Chem., 56, 8684-8695.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-[[4-[(1RS)-1-[(2,4-diaminopteridin-6-yl)methyl]but-3-ynyl]benzoyl]amino]pentanedioic acid
-
 Homo sapiens
lometrexol i.e. 5,10-dideaza-5,6,7,8-tetrahydrofolate Homo sapiens
additional information design and synthesis of series of 6-substituted straight side chain pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 5-8), non-benzoyl 6-carbon chain pyrrolo[2,3-d]pyrimidine antifolates are inhibitors of cell proliferation, correlating with expression of folate receptors. The compounds show selective cellular uptake via folate receptor-alpha and -beta, associated with high affinity binding and inhibition of de novo purine nucleotide biosynthesis via the enzyme, resulting in potent inhibition against folate receptor-expressing Chinese hamster cells and human KB tumor cells in culture Homo sapiens
N-(4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl)-L-glutamic acid
-
 Homo sapiens
N-(5-[N-(3,4-dihydro-2-methyl-4-oxyquinazolin-6-ylmethyl)-N-methyl-amino]-2-thienoyl)-L-glutamic acid
-
 Homo sapiens
N-[4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
N-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexanoyl]-L-glutamic acid
-
 Homo sapiens
N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-L-glutamic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P22102
-
-

Source Tissue

Source Tissue Comment Organism Textmining
KB cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
GARFTase
-
 Homo sapiens