Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src

5,7-Diphenyl-pyrrolo[2,3d]pyrimidines represent a new class of highly potent inhibitors of the tyrosine kinase c-Src (IC50 < 50 nM) with specificity against a panel of different tyrosine kinases. The substitution pattern on the two phenyl rings determines potency and specificity and provides a me...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (9), p.945-949
Hauptverfasser:	Missbach, M, Altmann, E, Widler, L, Susa, M, Buchdunger, E, Mett, H, Meyer, T, Green, J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Blotting, Western Chickens Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Models, Molecular Phosphorylation Protein-Tyrosine Kinases - antagonists & inhibitors Pyrimidines - chemical synthesis Pyrimidines - pharmacology Pyrroles - chemical synthesis Pyrroles - pharmacology src-Family Kinases Structure-Activity Relationship Substrate Specificity
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Beschreibung
Zusammenfassung:	5,7-Diphenyl-pyrrolo[2,3d]pyrimidines represent a new class of highly potent inhibitors of the tyrosine kinase c-Src (IC50 < 50 nM) with specificity against a panel of different tyrosine kinases. The substitution pattern on the two phenyl rings determines potency and specificity and provides a means to modulate cellular activity.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(00)00131-1