期刊论文详细信息
Bulletin of the Korean chemical society | |
Cap-Modified Hydroxamate Analogues as Histone Deacetylases Inhibitors and Antitumor Agents | |
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
【 预 览 】
Files | Size | Format | View |
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RO201912010244789ZK.pdf | 1839KB | download |