Optimization of 2-(3-(arylalkyl amino carbonyl) phenyl)-3-(2-methoxyphenyl)-4-thiazolidinone derivatives as potent antitumor growth and metastasis agents

Eur J Med Chem. 2014 Jun 10:80:340-51. doi: 10.1016/j.ejmech.2014.04.068.

Jing Wu ¹, Linxi Yu ¹, Feifei Yang ¹, Jingjie Li ¹, Peng Wang ¹, Wenbo Zhou ¹, Liwen Qin ¹, Yunqi Li ¹, Jian Luo ¹, Zhengfang Yi ², Mingyao Liu ³, Yihua Chen ⁴

Affiliations

1 Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, 500 Dongchuan Rd, Shanghai 200241, China.
2 Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, 500 Dongchuan Rd, Shanghai 200241, China. Electronic address: zfyi@bio.ecnu.edu.cn.
3 Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, 500 Dongchuan Rd, Shanghai 200241, China; Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology, Texas A&M University Health Science Center, Houston 77030, USA.
4 Shanghai Key Laboratory of Regulatory Biology, The Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, 500 Dongchuan Rd, Shanghai 200241, China. Electronic address: yhchen@bio.ecnu.edu.cn.

PMID: 24794770 DOI: 10.1016/j.ejmech.2014.04.068

Abstract

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.

Keywords

Antitumor growth and metastasis; Structure–activity relationships; Thiazolidinone derivatives.

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