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.
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container_end_page 1574
container_issue 9
container_start_page 1571
container_title Bioorganic & medicinal chemistry letters
container_volume 13
creator 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.
description 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.
doi_str_mv 10.1016/S0960-894X(03)00195-1
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ispartof Bioorganic & medicinal chemistry letters, 2003-05, Vol.13 (9), p.1571-1574
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source MEDLINE; ScienceDirect Journals (5 years ago - present)
subjects 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
title Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability
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