Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency.

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):1363-6. doi: 10.1016/s0960-894x(03)00094-5.

DOI:10.1016/s0960-894x(03)00094-5

PMID:12657283

Abstract

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 bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.

摘要

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