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

Dae Kee Kim, Ju Young Lee, Jae Sun Kim, Je Ho Ryu, Jin Young Choi, Jun Won Lee, Guang Jin Im, Tae Kon Kim, Jung Woo Seo, Hyun Ju Park, Jakyung Yoo, Jung Hyun Park, Tae You Kim, Yung Jue Bang

Research output: Contribution to journalArticlepeer-review

46 Scopus citations

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.

Original languageEnglish
Pages (from-to)5745-5751
Number of pages7
JournalJournal of Medicinal Chemistry
Volume46
Issue number26
DOIs
StatePublished - 18 Dec 2003

Fingerprint

Dive into the research topics of 'Synthesis and Biological Evaluation of 3-(4-Substituted-phenyl)-N-hydroxy-2-propenamides, a New Class of Histone Deacetylase Inhibitors'. Together they form a unique fingerprint.

Cite this