title: A hybrid of thiazolidinone with the hydroxamate scaffold for developing novel histone deacetylase inhibitors with antitumor activities.
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.
authors.affiliation: 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.
authors.forename: Feifei
authors.initials: F
authors.lastname: Yang
authors.affiliation: 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.
authors.forename: Shihong
authors.initials: S
authors.lastname: Peng
authors.affiliation: 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.
authors.forename: Yunqi
authors.initials: Y
authors.lastname: Li
authors.affiliation: 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.
authors.forename: Liqiang
authors.initials: L
authors.lastname: Su
authors.affiliation: 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.
authors.forename: Yangrui
authors.initials: Y
authors.lastname: Peng
authors.affiliation: 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.
authors.forename: Jing
authors.initials: J
authors.lastname: Wu
authors.affiliation: 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.
authors.forename: Huang
authors.initials: H
authors.lastname: Chen
authors.affiliation: 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.
authors.forename: Mingyao
authors.initials: M
authors.lastname: Liu
authors.affiliation: 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.
authors.forename: Zhengfang
authors.initials: Z
authors.lastname: Yi
authors.affiliation: 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.
authors.forename: Yihua
authors.initials: Y
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006877:Hydroxamic Acids / Q000737:chemistry* / Q000494:pharmacology*; D061986:MCF-7 Cells; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D053778:Thiazolidines