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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 1
BKCSDE 35(1)
January 20, 2014 

Cap-Modified Hydroxamate Analogues as Histone Deacetylases Inhibitors and Antitumor Agents
Qing-Wei Zhang, Juan Feng, Jian-Qi Li*
Histone deacetylases, SAHA, Molecular docking, Antitumor activity
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.
129 - 134
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