Design, synthesis and evaluation of belinostat analogs as histone deacetylase inhibitors

贝利司他类似物作为组蛋白去乙酰化酶抑制剂的设计、合成及评价

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作者:Jie-Huan Zhang, Madhusoodanan Mottamal, Hai-Shan Jin, Shanchun Guo, Yan Gu, Guangdi Wang, Li-Ming Zhao

Aim

Histone deacetylase (HDAC) is an attractive target for antitumor therapy. Therefore, the development of novel HDAC inhibitors is warranted. Materials &

Conclusion

Among them, compound 7e showed an IC50 value of 11.5 nM in inhibiting the HDAC in a pan-HDAC assay, being the most active compound of the series.

Methods

A series of HDAC inhibitors based on N-hydroxycinnamamide fragment was designed as the clinically used belinostat analog using amide as the connecting unit. All target compounds were evaluated for their in vitro HDAC inhibitory activities and some selected compounds were tested for their antiproliferative activities.

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