Synthesis and Biological Evaluation of 3-(4-Substituted-phenyl)-N-hydroxy-2-propenamides, a New Class of Histone Deacetylase Inhibitors
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.
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
p. 5745 - 5751
(2007/10/03)
α,β-UNSATURATED HYDROXAMIC ACID DERIVATIVES AND THEIR USE AS HISTONE DEACETYLASE INHIBITORS
Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacetylase inhibitory activity.
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Page/Page column 17
(2008/06/13)
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