[KSCI] Korea Science Citation Index Service

http://dx.doi.org/10.5012/bkcs.2014.35.1.129

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

Zhang, Qing-Wei (Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry)
Feng, Juan (College of Chemical & Pharmaceutical Engineering, Hebei University of Science and Technology)
Li, Jian-Qi (Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry)

Publication Information

Bulletin of the Korean Chemical Society / v.35, no.1, 2014 , pp. 129-134 More about this Journal

Abstract

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 $IC_{50}$ values from $0.54{\mu}M$ (Ic, Jurkat E6-1) to $7.73{\mu}M$ (Ib, K562), indicating that they are cell permeable and the benzimidazolyl-based ligands are flexible enough to occupy the binding site of HDAC.

Keywords

Histone deacetylases; SAHA; Molecular docking; Antitumor activity;

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