期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 23, 页码 7084-7086出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.09.093
关键词
Histone deacetylase; HDAC inhibitor; Isoform selectivity; Vorinostat
资金
- National Institute of Health [GM067657]
- Wayne State University
Suberoylanilide hydroxamic acid (SAHA, Vorinostat), the first FDA-approved histone deacetylase (HDAC) inhibitor drug, was modified at the C6 position to study the structural requirements for high potency and selectivity. Substituents on the C6 position only modestly influenced inhibitor potency, with poorer activity observed as substituent size increased. Interestingly, C6 substituents also modestly influenced selectivity compared to the parent compound, SAHA. This systematic study documenting the influence of substituents on the SAHA linker region will aid development of anti-cancer drugs targeting HDAC proteins. (C) 2012 Elsevier Ltd. All rights reserved.
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