1688677-89-5Relevant academic research and scientific papers
Containing thiazolinone structure of hydroxamic acid small molecular organic compound and its derivatives, their preparation and their use
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Paragraph 0059; 0061; 0062; 0065; 0068; 0102; 0103, (2017/06/15)
The invention discloses a novel hydroxamic acid micromolecule organic compound with a thaizolidinone structure represented by a formula (1) or (II), hydroximic acid derivatives, pharmaceutically acceptable salts and a preparation method of the hydroxamic
A hybrid of thiazolidinone with the hydroxamate scaffold for developing novel histone deacetylase inhibitors with antitumor activities
Yang, Feifei,Peng, Shihong,Li, Yunqi,Su, Liqiang,Peng, Yangrui,Wu, Jing,Chen, Huang,Liu, Mingyao,Yi, Zhengfang,Chen, Yihua
, p. 1727 - 1735 (2016/02/10)
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.
