A hybrid of thiazolidinone with the hydroxamate scaffold for developing novel histone deacetylase inhibitors with antitumor activities†,10.1039/C5OB02250A

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

A hybrid of thiazolidinone with the hydroxamate scaffold for developing novel histone deacetylase inhibitors with antitumor activities†

Shihong Peng,Yunqi Li,Liqiang Su,Yangrui Peng,Jing Wu,Huang Chen,Mingyao Liu,Zhengfang Yi,Yihua Chen

Organic & Biomolecular Chemistry Pub Date : 12/21/2015 00:00:00 , DOI:10.1039/C5OB02250A

Abstract

A series of novel histone deacetylase (HDAC) inhibitors were designed, synthesized and evaluated based on the strategies of a hybrid of the classic pharmacophore of HDAC inhibitors with the thiazolidinone scaffold. Some of the compounds showed potent HDAC1 inhibition with nM IC₅₀ values, more importantly, compound 12i displayed much better anti-metastatic effects than vorinostat (SAHA) against migration of the A549 cell line. Further mechanism exploration implied that compound 12i may inhibit tumor metastasis via modulating the epithelial–mesenchymal transition (EMT) and upregulating the acetylation of α-tubulin.