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Org Biomol Chem. 2016 Feb 7;14(5):1727-35. doi: 10.1039/c5ob02250a.

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

Author information

1
Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China. yhchen@bio.ecnu.edu.cn zfyi@bio.ecnu.edu.cn and School of biological science and technology, University of Jinan, Jinan, Shandong Province 250022, China.
2
Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China. yhchen@bio.ecnu.edu.cn zfyi@bio.ecnu.edu.cn.

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 12i showed potent HDAC1 inhibition with nM IC50 values, more importantly, compound 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.

PMID:
26732459
DOI:
10.1039/c5ob02250a
[Indexed for MEDLINE]

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