Syntheses and Biological Evaluation of Novel Hydroxamic Acid Derivatives Containing Purine Moiety as Histone Deacetylase Inhibitors

The novel hydroxamates containing purine scaffold were designed, synthesized and screened for their biological activities as histone deacetylase (HDAC) inhibitors. Some of them exhibited excellent acti-HDACs activities and antiproliferative activities, the most promising compound was 7m′. Western bl...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2018/04/01, Vol.66(4), pp.439-451
Hauptverfasser:	Xu, Zhaoxing, Yang, Yongchao, Mai, Xi, Liu, Bin, Xiong, Yuanzhen, Feng, Lihuang, Liao, Yijing, Zhang, Yu, Wang, Huanlu, Ouyang, Leiting, Liu, Shuhao
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylation antiproliferative Catalysis Cell lines Chromatin Conformation Dose-Response Relationship, Drug HCT116 Cells HDAC2 protein Histone deacetylase Histone Deacetylase Inhibitors - chemical synthesis Histone Deacetylase Inhibitors - chemistry Histone Deacetylase Inhibitors - pharmacology Histone Deacetylases - metabolism Histone H3 Humans Hydroxamic acid Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Inhibitors K562 Cells Molecular docking Molecular Docking Simulation Molecular Structure purine Purines - chemistry Purines - pharmacology Structure-Activity Relationship Western blot analysis Zinc
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