Cap-Modified Hydroxamate Analogues as Histone Deacetylases Inhibitors and Antitumor Agents

Bulletin of the Korean chemical society

Juan Feng¹  Qing-Wei Zhang¹  Jian-Qi Li¹ 

关键词: Histone deacetylases;    SAHA;    Molecular docking;    Antitumor activity;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

Two series of SAHA-liked hydroxamate analogues were designed, synthesized and evaluated for their biological activities against nuclear HDACs. Compounds of Series I were found to be very effective inhibitors of cancer cell growth in the PC-3, Hut78, K562 and Jurkat E6-1 cancer cell lines with mean IC50 values from 0.54 M (Ic, Jurkat E6-1) to 7.73 M (Ib, K562), indicating that they are cell permeable and the benzimidazolyl-based ligands are flexible enough to occupy the binding site of HDAC.

【 授权许可】

Unknown