期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 23, 页码 6093-6096出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.029
关键词
Histone deacetylase inhibitor; HDAC; Mercaptoketone; Prodrug; HCT-116; KD5170; Sulfonamide
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. (C) 2008 Elsevier Ltd. All rights reserved.
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