Citation: Jie Jiao, Qiang Wang, Hua Wei Zhu, Hao Fang, Wen Fang Xu. Synthesis and biological evaluation of a new series of histone deacetylases inhibitors[J]. Chinese Chemical Letters, ;2008, 19(6): 673-675. doi: 10.1016/j.cclet.2008.04.010 shu

Synthesis and biological evaluation of a new series of histone deacetylases inhibitors

School of Pharmaceutical Science, Shandong University, Jinan 250012, China

Received Date: 7 January 2008

Fund Project: This work was supported by the National "863" Foundation (No. 2007AA02Z314).

Histone deacetylases (HDACs) play an important role in tumorigenesis. Inhibition of HDACs is considered as a potent strategy for cancer therapy. Two lead compounds (ja and jb) were found to have activities against HDACs with IC₅₀ at about 15 μmol/L. Then a new series of hydroximic acid derivatives were designed and synthesized based on them. The HDACs activity assay in vitro found that compounds J04 and J09 are nearly as potent as the positive control drug Zolinza.
- HDACs,
- Tumorigenesis,
- Cancer therapy,
- Hydroximic acid
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