| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1359548 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jianjun Cheng, Jihong Qin, Sihua Guo, Hangdeng Qiu, Yun Zhong,