Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
复制标题
DOI：
10.1016/j.bmcl.2007.06.038
复制
发表时间：
2007-09-01
影响因子：
2.7
通讯作者：
Miyachi, Hiroyuki
中科院分区：
文献类型：
--
作者：
Lee, Shoukou;Shinji, Chihiro;Miyachi, Hiroyuki
我们设计并合成了带有4-（3-吡啶基）苯基作为帽结构的异羟肟酸衍生物，并发现它们具有有效的历史脱乙酰酶（HDAC）抑制活性。代表性化合物17 a显示出比临床上使用的HDAC抑制剂辛二酰苯胺异羟肟酸（Zolinza（TM））更有效的对胰腺癌细胞的生长抑制活性和更大的p21（WAF 1/CIP 1）表达上调。(C)2007爱思唯尔有限公司保留所有权利。
We designed and synthesized hydroxamic acid derivatives bearing a 4-(3-pyridyl)phenyl group as a cap structure, and found that they exhibit potent historic 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 (TM)). (C) 2007 Elsevier Ltd. All rights reserved.