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J Med Chem. 2003 Dec 18;46(26):5745-51.

Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors.

Author information

1
In2Gen Co. Ltd., 28 Yongon-dong, Chongno-gu, Seoul 110-799, Korea. dkkim@ewha.ac.kr

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.

PMID:
14667227
DOI:
10.1021/jm030377q
[Indexed for MEDLINE]

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