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

S Lee, C Shinji, K Ogura, M Shimizu, S Maeda…

Index: Lee, Shoukou; Shinji, Chihiro; Ogura, Kiyoshi; Shimizu, Motomu; Maeda, Satoko; Sato, Mayumi; Yoshida, Minoru; Hashimoto, Yuichi; Miyachi, Hiroyuki Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 17 p. 4895 - 4900

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Citation Number: 36

Abstract

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 p21WAF1/CIP1 expression than the clinically used HDAC inhibitor suberoylanilide hydroxamic acid ( ...