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ID: ALA1140672

Journal: Bioorg Med Chem Lett

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

Authors: Lee S, Shinji C, Ogura K, Shimizu M, Maeda S, Sato M, Yoshida M, Hashimoto Y, Miyachi H.

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 p21(WAF1/CIP1) expression than the clinically used HDAC inhibitor suberoylanilide hydroxamic acid (Zolinza).

CiteXplore: 17588744

DOI: 10.1016/j.bmcl.2007.06.038