Syntheses and antitumor activities of N¡ä1,N¡ä3-dialkyl-N¡ä1,N¡ä3-di-(alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol
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- 作者：Shoujun Chen ; Lijun Sun ; Keizo Koya ; Noriaki Tatsuta ; Zhiqiang Xia ; Timothy Korbut ; Zhenjian Du ; Jim Wu ; Guiqing Liang ; Jun Jiang ; Mitsunori Ono ; Dan Zhou ; Andrew Sonderfan
- 关键词：STA-4783 ; Elesclomol ; Discovery ; Anticancer ; Taxol enhancer ; Hsp70 induction ; SAR ; Oxidative stress ; ROS
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2013
- 出版时间：15 September, 2013
- 年：2013
- 卷：23
- 期：18
- 页码：5070-5076
- 全文大小：1040 K
文摘
A series of N¡ä1,N¡ä3-dialkyl-N¡ä1,N¡ä3-di(alkylcarbonothioyl) malonohydrazides have been designed and synthesized as anticancer agents by targeting oxidative stress and Hsp70 induction. Structure-activity relationship (SAR) studies lead to the discovery of STA-4783 (elesclomol), a novel small molecule that has been evaluated in a number of clinical trials as an anticancer agent in combination with Taxol.