Syntheses and antitumor activities of N′ 1, N′ 3-dialkyl-N′ 1, N′ 3-di-(alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol

…, G Liang, J Jiang, M Ono, D Zhou, A Sonderfan

文献索引：Chen, Shoujun; Sun, Lijun; Koya, Keizo; Tatsuta, Noriaki; Xia, Zhiqiang; Korbut, Timothy; Du, Zhenjian; Wu, Jim; Liang, Guiqing; Jiang, Jun; Ono, Mitsunori; Zhou, Dan; Sonderfan, Andrew Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 18 p. 5070 - 5076

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被引用次数: 9

摘要

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.