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Synthesis and Biological Evaluation of 3-(4-Substituted-phenyl)-N-hydroxy-2-propenamides, a New Class of Histone Deacetylase Inhibitors

Cited 39 time in Web of Science Cited 44 time in Scopus
Authors
Kim, Dae-Kee; Lee, Ju Young; Kim, Jae-Sun; Ryu, Je-Ho; Choi, Jin-Young; Lee, Jun Won; Im, Guang-Jin; Kim, Tae-Kon; Seo, Jung Woo; Park, Hyun-Ju; Yoo, Jakyung; Park, Jung-Hyun; Kim, Tae-You; Bang, Yung-Jue
Issue Date
2003-12
Citation
Journal of Medicinal Chemistry, Vol.46 No.26, pp.5745-5751
Abstract
Inhibitors of histone deacetylases (HDACs) have been shown to induce differentiation and/or apoptosis of human tumor cells. Novel 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides have been prepared as a new class of HDAC inhibitors and evaluated for their antiproliferative activity and HDAC inhibitory activity. Incorporation of a 1,4-phenylene carboxamide linker, shown by 5, and a 4-(dimethylamino)phenyl or 4-(pyrrolidin-1-yl)phenyl group as a cap substructure generated highly potent hydroxamic acid-based HDAC inhibitors 5a and 5b.
ISSN
0022-2623
URI
https://hdl.handle.net/10371/173160
DOI
https://doi.org/10.1021/jm030377q
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College of Medicine/School of Medicine (의과대학/대학원)Internal Medicine (내과학전공)Journal Papers (저널논문_내과학전공)
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