2. Academic Validation
  3. Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives

Search for novel histone deacetylase inhibitors. Part II: design and synthesis of novel isoferulic acid derivatives

  • Bioorg Med Chem. 2014 May 1;22(9):2707-13. doi: 10.1016/j.bmc.2014.03.019.
Wen Lu 1,  Fang Wang 1,  Tao Zhang 1,  Jinyun Dong 1,  Hongping Gao 1,  Ping Su 1,  Yaling Shi 1,  Jie Zhang 2
Affiliations

Affiliations

  • 1 School of Pharmacy, Health Science Center, Xi'an Jiaotong University, No. 76, Yanta West Road, Xi'an, Shaanxi Province 710061, PR China.
  • 2 School of Pharmacy, Health Science Center, Xi'an Jiaotong University, No. 76, Yanta West Road, Xi'an, Shaanxi Province 710061, PR China. Electronic address: zhj8623@mail.xjtu.edu.cn.
PMID: 24702857 DOI: 10.1016/j.bmc.2014.03.019
Abstract

Previously, we described the discovery of potent ferulic acid-based histone deacetylase inhibitors (HDACIs) with halogeno-acetanilide as novel surface recognition moiety (SRM). In order to improve the affinity and activity of these HDACIs, twenty seven isoferulic acid derivatives were described herein. The majority of title compounds displayed potent HDAC inhibitory activity. In particular, IF5 and IF6 exhibited significant enzymatic inhibitory activities, with IC50 values of 0.73 ± 0.08 and 0.57 ± 0.16 μM, respectively. Furthermore, these compounds showed moderate antiproliferative activity against human Cancer cells. Especially, IF6 displayed promising profile as an antitumor candidate with IC50 value of 3.91 ± 0.97 μM against HeLa cells. The results indicated that these isoferulic acid derivatives could serve as promising lead compounds for further optimization.

Keywords

Anticancer; HDAC inhibitor; Histone deacetylase; Isoferulic acid.

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