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Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency |
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| Authors: | 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 |
| Institution: | Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. stephen.gwaltney@syrrx.com |
| 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. |
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