Synthesis and biological evaluation of 1-arylsulfonyl-5-(N-hydroxyacrylamide) indoles as potent histone deacetylase inhibitors with antitumor activity in vivo

…, TK Yeh, PH Huang, CM Teng, CS Chen…

Index: Lai, Mei-Jung; Huang, Han-Li; Pan, Shiow-Lin; Liu, Yi-Min; Peng, Chieh-Yu; Lee, Hsueh-Yun; Yeh, Teng-Kuang; Huang, Po-Hsien; Teng, Che-Ming; Chen, Ching-Shih; Chuang, Hsun-Yueh; Liou, Jing-Ping Journal of Medicinal Chemistry, 2012 , vol. 55, # 8 p. 3777 - 3791

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Citation Number: 28

Abstract

A series of 1-arylsulfonyl-5-(N-hydroxyacrylamide) indoles has been identified as a new class of histone deacetylase inhibitors. Compounds 8, 11, 12, 13, and 14 demonstrated stronger antiproliferative activities than 1 (SAHA) with GI50 values ranging from 0.36 to 1.21 μM against Hep3B, MDA-MB-231, PC-3, and A549 human cancer cell lines. Lead compound 8 showed remarkable HDAC 1, 2, and 6 isoenzymes inhibitory activities with ...