2. Academic Validation
  3. 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

  • 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

Affiliation

  • 1 Synta Pharmaceuticals Corp, Lexington, MA 02421, USA. schen@syntapharma.com
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.

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