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

  • Bioorg Med Chem Lett. 2013 Sep 15;23(18):5070-6. doi: 10.1016/j.bmcl.2013.07.032.
Shoujun Chen  1 ,  Lijun Sun ,  Keizo Koya ,  Noriaki Tatsuta ,  Zhiqiang Xia ,  Timothy Korbut ,  Zhenjian Du ,  Jim Wu ,  Guiqing Liang ,  Jun Jiang ,  Mitsunori Ono ,  Dan Zhou ,  Andrew Sonderfan
Affiliations
PMID: 23937981 DOI: 10.1016/j.bmcl.2013.07.032
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.

Keywords
Anticancer; Discovery; Elesclomol; Hsp70 induction; Oxidative stress; ROS; SAR; STA-4783; Taxol enhancer.