Histone deacetylase (HDAC) inhibitors with a novel connecting unit linker region reveal a selectivity profile for HDAC4 and HDAC5 with improved activity against …

L Marek, A Hamacher, FK Hansen, K Kuna…

文献索引：Marek, Linda; Hamacher, Alexandra; Hansen, Finn K.; Kuna, Krystina; Gohlke, Holger; Kassack, Matthias U.; Kurz, Thomas Journal of Medicinal Chemistry, 2013 , vol. 56, # 2 p. 427 - 436

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被引用次数: 39

摘要

The synthesis and biological evaluation of new potent hydroxamate-based HDAC inhibitors with a novel alkoxyamide connecting unit linker region are described. Biological evaluation includes MTT and cellular HDAC assays on sensitive and chemoresistant cancer cell lines as well as HDAC profiling of selected compounds. Compound 19i (LMK235)(N-((6- (hydroxyamino)-6-oxohexyl) oxy)-3, 5-dimethylbenzamide) showed similar effects ...