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- 作者：Haishan Wang ; Niefang Yu ; Hongyan Song ; Dizhong Chen ; Yong Zou ; Weiping Deng ; Pek Ling Lye ; Joyce Chang ; Melvin Ng ; Sté ; phanie Blanchard ; Eric T. Sun ; K ; a Sangthongpitag ; Xukun Wang ; Kee Chuan Goh
- 关键词：HDAC inhibitor ; Benzimidazole ; Hydroxamic acid ; SAR ; Anticancer
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 March 2009
- 年：2009
- 卷：19
- 期：5
- 页码：1403-1408
- 全文大小：367 K
文摘
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.