Syntheses and antitumor activities of N′1,N′3-dialkyl-N′1,N′3-di-(alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol
Syntheses and antitumor activities of N′1,N′3-dialkyl-N′1,N′3-di-(alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol
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DOI：
10.1016/j.bmcl.2013.07.032
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发表时间：
2013-09-15
影响因子：
2.7
通讯作者：
Sonderfan, Andrew
中科院分区：
文献类型：
--
作者：
Chen, Shoujun;Sun, Lijun;Sonderfan, Andrew
通过靶向氧化应激和Hsp 70诱导，设计并合成了一系列N '（1），N'（3）-二烷基-N '（1），N'（3）-二（烷基硫代碳酰基）丙二酰肼作为抗癌药物。结构-活性关系（SAR）研究发现了STA-4783（elesclomol），这是一种新型小分子，已在许多临床试验中作为抗癌药物与紫杉醇联合使用。(C)2013爱思唯尔有限公司保留所有权利。
A series of N'(1),N'(3)-dialkyl-N'(1),N'(3)-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. (C) 2013 Elsevier Ltd. All rights reserved.