Chen, Shoujun, Lijun Sun, Keizo Koya, Noriaki Tatsuta, Zhiqiang Xia, Timothy Korbut, Zhenjian Du, et al. 2013. “Syntheses and Antitumor Activities of N’1,N’3-Dialkyl-N’1,N’3-Di-(alkylcarbonothioyl) Malonohydrazide: The Discovery of Elesclomol.”. Bioorganic & Medicinal Chemistry Letters 23 (18): 5070-6.
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.