Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors

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• 作者：Shoukou Lee ; Chihiro Shinji ; Kiyoshi Ogura ; Motomu Shimizu ; Satoko Maeda ; Mayumi Sato ; Minoru Yoshida ; Yuichi Hashimoto ; Hiroyuki Miyachi
• 关键词：HDAC ; HDAC inhibitor ; Isoindoklinone ; Hydroxamic acid ; Pancreatic cancer ; p21
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 September 2007
• 卷：17
• 期：17
• 页码：4895-4900
• 文件大小：252 K

摘要

We designed and synthesized hydroxamic acid derivatives bearing a 4-(3-pyridyl)phenyl group as a cap structure, and found that they exhibit potent histone deacetylase (HDAC) inhibitory activity. A representative compound, 17a, showed more potent growth-inhibitory activity against pancreatic cancer cells and greater upregulation of p21^WAF1/CIP1 expression than the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (Zolinza™).