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Literature summary for 2.7.10.1 extracted from

  • Gangjee, A.; Namjoshi, O.; Ihnat, M.; Buchanan, A.
    The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines (2010), Bioorg. Med. Chem. Lett., 20, 3177-3181.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.10.1

Inhibitors

Inhibitors Comment Organism Structure
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
 Homo sapiens
6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
 Homo sapiens
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
 Homo sapiens
6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
 Homo sapiens
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
-
 Homo sapiens
6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
-
 Homo sapiens
additional information the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds; the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds; the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds; the inclusion of a 2-amino group in pyrrolo[2,3-d]pyrimidines improves multiple receptor tyrosine kinase inhibition and antiangiogenic activity. The 2-amino analogs are better against epidermal growth factor receptor EGFR and platelet derived growth factor PDGFR-beta in whole cell inhibition assays and in the A-431 cytotoxicity assay compared to the 2-deamino analogs. The 2-deamino analogs are more potent inhibitors against vascular endothelial growth factor VEGFR-2 than the corresponding 2-amino compounds Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00533 EGFR
-
Homo sapiens P09619 PDGFR-beta
-
Homo sapiens P17948 VEGFR-1
-
Homo sapiens P35968 VEGFR-2
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0003
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.0085
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.0118
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.025
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.031
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.0451
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.05
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.056
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.057
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.077
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.09
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.104
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.112
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.122
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.129
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.164
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.2
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(3-bromobenzyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.2
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.2
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.2
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidin-2-amine
0.223
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-(1H-indol-5-ylmethyl)-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine
0.5
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 6-[4-fluoro-3-(trifluoromethyl)benzyl]-4-phenyl-7H-pyrrolo[2,3-d]pyrimidine