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Bioorg Med Chem Lett. 2014 Oct 1;24(19):4768-4772. doi: 10.1016/j.bmcl.2014.06.080. Epub 2014 Jul 5.

Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.

Author information

1
Shanghai Huilun Life Sciences & Technology Co. Ltd, Shanghai 201108, China. Electronic address: chengjianjun83@163.com.
2
Shanghai Huilun Life Sciences & Technology Co. Ltd, Shanghai 201108, China.

Abstract

Phenyl imidazolidin-2-one was introduced as the linker for novel HDAC inhibitors. A focused library of 20 compounds was designed and synthesized, among which eight compounds showed equivalent or higher potencies against HDAC1 as compared to vorinostat. In vitro antitumor activity assays in HCT-116, PC-3 and HL-60 cancer cells revealed six compounds with potent antitumor activities, and compound 1o showed 6- to 9-fold higher potencies compared to vorinostat. In an HCT-116 nude mice xenograft model, compound 1o displayed significant antitumor activity in both continuous and intermittent dosing schedules.

KEYWORDS:

Antitumor; Histone deacetylases; Hydroxamate; Vorinostat

PMID:
25182565
DOI:
10.1016/j.bmcl.2014.06.080
[Indexed for MEDLINE]

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