Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives.
作者信息
Gwaltney Stephen L, O'Connor Stephen J, Nelson Lissa T J, Sullivan Gerard M, Imade Hovis, Wang Weibo, Hasvold Lisa, Li Qun, Cohen Jerome, Gu Wen-Zhen, Tahir Stephen K, Bauch Joy, Marsh Kennan, Ng Shi-Chung, Frost David J, Zhang Haiying, Muchmore Steve, Jakob Clarissa G, Stoll Vincent, Hutchins Charles, Rosenberg Saul H, Sham Hing L
机构信息
Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA.
出版信息
Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62. doi: 10.1016/s0960-894x(03)00095-7.
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
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