1395434-53-3Relevant articles and documents
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)
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.
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; 0063, (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
Optimization of 2-(3-(arylalkyl amino carbonyl) phenyl)-3-(2-methoxyphenyl) -4-thiazolidinone derivatives as potent antitumor growth and metastasis agents
Wu, Jing,Yu, Linxi,Yang, Feifei,Li, Jingjie,Wang, Peng,Zhou, Wenbo,Qin, Liwen,Li, Yunqi,Luo, Jian,Yi, Zhengfang,Liu, Mingyao,Chen, Yihua
, p. 340 - 351 (2014/05/20)
A series of 2,3-diaryl-4-thiazolidinone derivatives were synthesized and evaluated for their antiproliferative properties against two well-known cancer cell lines (A549 as human lung cancer and MDA-MB-231 as human breast cancer). Structure activity relationship (SAR) analysis resulted in the discovery of 2-(3-(arylalkyl amino carbonyl)phenyl)-3-(2-methoxy-phenyl)-4-thiazolidinone derivatives with high potent inhibitory effects on the proliferation of both cancer cell lines. Furthermore, several compounds with potent antiproliferative activities displayed excellent inhibitory activities on migration with an IC50 of about 0.05 μM on MDA-MB-231 cells in two different migration assays. In particular, compound 39 was indicated to suppress tumor growth and metastasis as well as promote survival rate. Intriguingly, this series of analogs have been indicated to inhibit tumor cell proliferation through inducing cell cycle arrest. These results suggested that the new series of 2-(3-(arylalkyl amino carbonyl)phenyl)-3-(2-methoxyphenyl)-4-thiazolidinone derivatives could be regarded and developed as novel highly potential anticancer agents in the future.
