| Literature DB >> 19181524 |
Haishan Wang1, Niefang Yu, Hongyan Song, Dizhong Chen, Yong Zou, Weiping Deng, Pek Ling Lye, Joyce Chang, Melvin Ng, Eric T Sun, Kanda Sangthongpitag, Xukun Wang, Xiaofeng Wu, Hwee Hoon Khng, Lijuan Fang, Siok Kun Goh, Wai Chung Ong, Zahid Bonday, Walter Stünkel, Anders Poulsen, Michael Entzeroth.
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.Entities:
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Year: 2009 PMID： 19181524 DOI： 10.1016/j.bmcl.2009.01.041
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823