期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 14, 期 5, 页码 1727-1735出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5ob02250a
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资金
- National Basic Research Program of China [2012CB910404]
- National Major Scientific and Technological Special Project for Significant New Drugs Development [2013ZX09507001]
- National Natural Science Foundation of China [81202407, 81272463]
- Science and Technology Commission of Shanghai Municipality [15431902200]
- Research Fund for the Doctoral Program of Higher Education of China [20120076120029]
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 alpha-tubulin.
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