Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability

A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics. A pyridyl moiety was introduced into a previously developed series of farnesyltransfer...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-05, Vol.13 (9), p.1571-1574
Hauptverfasser:	Tong, Yunsong, Lin, Nan-Horng, Wang, Le, Hasvold, Lisa, Wang, Weibo, Leonard, Nicholas, Li, Tongmei, Li, Qun, Cohen, Jerry, Gu, Wen-Zhen, Zhang, Haiying, Stoll, Vincent, Bauch, Joy, Marsh, Kennan, Rosenberg, Saul H., Sham, Hing L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Alkyl and Aryl Transferases - antagonists & inhibitors Animals Antineoplastic agents Biological and medical sciences Biological Availability Crystallography, X-Ray Dogs Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Farnesyltranstransferase General aspects Haplorhini Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Medical sciences Models, Molecular Nitriles - chemical synthesis Nitriles - chemistry Nitriles - pharmacology Pharmacology. Drug treatments Stereoisomerism Structure-Activity Relationship
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Zusammenfassung:	A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics. A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl, resulting in potent inhibitors with improved pharmacokinetics.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00195-1