N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: Design,synthesis, SAR studies,and in vivo antitumor activity |
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Authors: | Haishan Wang Niefang Yu Hongyan Song Dizhong Chen Yong Zou Weiping Deng Pek Ling Lye Joyce Chang Melvin Ng Stéphanie Blanchard Eric T. Sun Kanda Sangthongpitag Xukun Wang Kee Chuan Goh Xiaofeng Wu Hwee Hoon Khng Lijuan Fang Siok Kun Goh Wai Chung Ong Zahid Bonday Michael Entzeroth |
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Affiliation: | S1BIO Pte Ltd, 1 Science Park Road, #05-09 The Capricorn, Singapore Science Park II, Singapore 117528, Singapore |
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Abstract: | A series of N-hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides were designed and synthesized as novel HDAC inhibitors. General SAR has been established for the substituents at positions 1 and 2, as well as the importance of the ethylene group and its attachment to position 5. Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays. A representative compound, 23 (SB639), has demonstrated antitumor activity in a colon cancer xenograft model. |
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