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

Title
Synthesis and Biological Evaluation of 3-(4-Substituted-phenyl)-N-hydroxy-2-propenamides, a New Class of Histone Deacetylase Inhibitors
Authors
Kim D.-K.Lee J.Y.Kim J.-S.Ryu J.-H.Choi J.-Y.Lee J.W.Im G.-J.Kim T.-K.Seo J.W.Park H.-J.Yoo J.Park J.-H.Kim T.-Y.Bang Y.-J.
Ewha Authors
김대기
SCOPUS Author ID
김대기scopus
Issue Date
2003
Journal Title
Journal of Medicinal Chemistry
ISSN
0022-2623JCR Link
Citation
vol. 46, no. 26, pp. 5745 - 5751
Indexed
SCI; SCIE; SCOPUS WOS scopus
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.
DOI
10.1021/jm030377q
Appears in Collections:
약학대학 > 약학과 > Journal papers
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