Pyrrolo[2,3- d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I

Pyrrolo[2,3- d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of lck in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (19), p.2167-2170
Hauptverfasser:	Arnold, Lee D, Calderwood, David J, Dixon, Richard W, Johnston, David N, Kamens, Joanne S, Munschauer, Rainer, Rafferty, Paul, Ratnofsky, Sheldon E
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Immunomodulators Jurkat Cells Lymphocyte Specific Protein Tyrosine Kinase p56(lck) - antagonists & inhibitors Lymphocyte Specific Protein Tyrosine Kinase p56(lck) - chemistry Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments Proto-Oncogene Proteins pp60(c-src) - antagonists & inhibitors Proto-Oncogene Proteins pp60(c-src) - metabolism Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Receptor Protein-Tyrosine Kinases - antagonists & inhibitors Receptor Protein-Tyrosine Kinases - metabolism Receptor, TIE-2 Receptors, Growth Factor - antagonists & inhibitors Receptors, Growth Factor - metabolism Receptors, Vascular Endothelial Growth Factor Substrate Specificity
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Beschreibung
Zusammenfassung:	Pyrrolo[2,3- d]pyrimidines containing a 5-(4-phenoxyphenyl) substituent are potent and selective inhibitors of lck in vitro; some compounds are selective for lck over src. Data are shown for two compounds demonstrating that they are potent and selective inhibitors of IL2 production in cells.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00441-8