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

DK Kim, JY Lee, JS Kim, JH Ryu, JY Choi…

Index: 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 Journal of Medicinal Chemistry, 2003 , vol. 46, # 26 p. 5745 - 5751

Full Text: HTML

Citation Number: 49

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) ...