Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine,phenylalanine and histidine derivatives |
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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 |
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Institution: | Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. stephen.gwaltney@syrrx.com |
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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 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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