Synthesis and biological evaluation of 3-(4-substituted-phenyl)-N-hydroxy-2-propenamides, a new class of histone deacetylase inhibitors |
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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 |
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Affiliation: | In2Gen Co. Ltd., 28 Yongon-dong, Chongno-gu, Seoul 110-799, Korea. dkkim@ewha.ac.kr |
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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. |
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