2-Arylindole-3-acetamides: FPP-Competitive inhibitors of farnesyl protein transferase

A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative m...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-04, Vol.11 (7), p.865-869
Hauptverfasser:	Trotter, B.Wesley, Quigley, Amy G., Lumma, William C., Sisko, John T., Walsh, Eileen S., Hamann, Christian S., Robinson, Ronald G., Bhimnathwala, Hema, Kolodin, D.Garrett, Zheng, Wei, Buser, Carolyn A., Huber, Hans E., Lobell, Robert B., Kohl, Nancy E., Williams, Theresa M., Graham, Samuel L., Dinsmore, Christopher J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkyl and Aryl Transferases - antagonists & inhibitors Alkyl and Aryl Transferases - metabolism Antineoplastic agents Biological and medical sciences Carrier Proteins - metabolism Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology General aspects Heat-Shock Proteins - metabolism HSP40 Heat-Shock Proteins Humans Indoleacetic Acids - chemical synthesis Indoleacetic Acids - metabolism Indoleacetic Acids - pharmacology Medical sciences Pharmacology. Drug treatments Protein Prenylation - drug effects Protein Prenylation - physiology ras Proteins - metabolism Structure-Activity Relationship Tumor Cells, Cultured
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