Non-thiol farnesyltransferase inhibitors: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides

We have designed the nitrophenylfurylacryl-substituted benzophenone 4f as a non-thiol farnesyltransferase inhibitor utilizing a novel aryl binding site of farnesyltransferase. Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2003-04, Vol.11 (7), p.1521-1530
Hauptverfasser:	KETTLER, Katja, SAKOWSKI, Jacek, SILBER, Katrin, SATTLER, Isabel, KLEBE, Gerhard, SCHLITZER, Martin
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkyl and Aryl Transferases - antagonists & inhibitors Amides - chemical synthesis Amides - pharmacology Antineoplastic agents Biological and medical sciences Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Farnesyltranstransferase Furans - chemical synthesis Furans - pharmacology General aspects Indicators and Reagents Magnetic Resonance Spectroscopy Medical sciences Models, Molecular Nitro Compounds - chemical synthesis Nitro Compounds - pharmacology Pharmacology. Drug treatments Protein Conformation Saccharomyces cerevisiae - enzymology Structure-Activity Relationship
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Zusammenfassung:	We have designed the nitrophenylfurylacryl-substituted benzophenone 4f as a non-thiol farnesyltransferase inhibitor utilizing a novel aryl binding site of farnesyltransferase. Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol farnesyltransferase inhibitors with improved activity. These compounds display activity in the low nanomolar range.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/S0968-0896(03)00064-6