@article{0a929d3b27b54aecb264cd3b8ff2cf53,
title = "Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors",
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 (Zolinza{\texttrademark}).",
keywords = "HDAC, HDAC inhibitor, Hydroxamic acid, Isoindoklinone, Pancreatic cancer, p21",
author = "Shoukou Lee and Chihiro Shinji and Kiyoshi Ogura and Motomu Shimizu and Satoko Maeda and Mayumi Sato and Minoru Yoshida and Yuichi Hashimoto and Hiroyuki Miyachi",
note = "Funding Information: The work described in this paper was partially supported by a Grant-in-Aid for Scientific Research from The Ministry of Education, Culture, Sports, Science and Technology, Japan. The authors thank Prof. Nishino, Graduate School of Life Science and Systems Engineering, Kyushu Institute of Technology, for data on the HDAC inhibitory activity of Zolinza, and Dr. Keisuke Imai, Lead Discovery Research Labs., Astellas Pharma Inc., for computational docking studies. ",
year = "2007",
month = sep,
day = "1",
doi = "10.1016/j.bmcl.2007.06.038",
language = "English",
volume = "17",
pages = "4895--4900",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "17",
}
