title: Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors.
abstract: Novel indeno[1,2-d]thiazole hydroxamic acids were designed, synthesized, and evaluated for histone deacetylases (HDACs) inhibition and antiproliferative activities on tumor cell lines. Most of the tested compounds exhibited HDAC inhibition and antiproliferative activity against both MCF7 and HCT116 cells with GI50 values in the sub-micromolar range. Among them, compound 6o showed good inhibitory activity against pan-HDAC with IC50 value of 0.14 μM and significant growth inhibition on MCF7 and HCT116 cells with GI50 values of 0.869 and 0.535 μM, respectively.
authors: School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
authors: Ming
authors: M
authors: Zhou
authors: Chengqing
authors: C
authors: Ning
authors: Ruihuan
authors: R
authors: Liu
authors: Yujun
authors: Y
authors: He
authors: Niefang
authors: N
authors: Yu
mesh_terms: D001665:Binding Sites; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006575:Heterocyclic Compounds, 3-Ring / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D006655:Histone Deacetylases / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D061986:MCF-7 Cells; D062105:Molecular Docking Simulation; D017434:Protein Structure, Tertiary; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D006575:Heterocyclic Compounds, 3-Ring; D056572:Histone Deacetylase Inhibitors; D006877:Hydroxamic Acids; D013844:Thiazoles; D006655:Histone Deacetylases