Identification of KD5170: A novel mercaptoketone-based histone deacetylase inhibitor

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• 作者：Joseph E. Payne ; Cé ; line Bonnefous ; Christian A. Hassig ; Kent T. Symons ; Xin Guo ; Phan-Manh Nguyen ; Tami Annable ; Paul L. Wash ; Timothy Z. Hoffman ; Tadimeti S. Rao ; Andrew K. Shiau ; James W. Malec
• 关键词：Histone deacetylase inhibitor ; HDAC ; Mercaptoketone ; Prodrug ; HCT-116 ; KD5170 ; Sulfonamide
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 December 2008
• 年：2008
• 卷：18
• 期：23
• 页码：6093-6096
• 全文大小：351 K

文摘

We report the identification of KD5170, a potent mercaptoketone-based Class I and II-histone deacetylase inhibitor that demonstrates broad spectrum cytotoxic activity against a range of human tumor-derived cell lines. KD5170 exhibits robust and sustained histone H3 hyperacetylation in HCT-116 xenograft tumors following single oral or iv dose and inhibition of tumor growth following chronic dosing.