N'1,N'3-二烷基-N'1,N'3-二-(烷基亚磺酰基)丙二酰肼的合成及抗肿瘤活性： elesclomol 的发现。
Syntheses and antitumor activities of N'1,N'3-dialkyl-N'1,N'3-di-(alkylcarbonothioyl) malonohydrazide: the discovery of elesclomol.
机构信息
Synta Pharmaceuticals Corp, Lexington, MA 02421, USA.
出版信息
Bioorg Med Chem Lett. 2013 Sep 15;23(18):5070-6. doi: 10.1016/j.bmcl.2013.07.032. Epub 2013 Jul 25.
PMID:23937981
Abstract
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.
摘要
我们设计并合成了一系列 N'（1）、N'（3）-二烷基-N'（1）、N'（3）-二（烷基碳硫代酰基）丙二酰肼类化合物作为靶向氧化应激和诱导 Hsp70 的抗癌药物。通过构效关系（SAR）研究，发现了 STA-4783（elesclomol），这是一种新型小分子药物，已在多项临床试验中作为与紫杉醇联合使用的抗癌药物进行评估。
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