Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364346 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Joseph E. Payne, Céline 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. Malecha, Stewart A. Noble, Jeffrey H. Hager, Nicholas D. Smith,