Journal
JOURNAL OF INORGANIC BIOCHEMISTRY
Volume 130, Issue -, Pages 69-73Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2013.10.005
Keywords
Elesclomol; Copper(II) complex; Crystallographic characterization; Electrochemical property; Anticancer activity; ROS
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Elesclomol is a novel anticancer agent that has been evaluated in a number of late stage clinical trials. A new and convenient synthesis of elesclomol and its copper complex is described. X-ray crystallographic characterization and the electrochemical properties of the elesclomol copper(II) complex are discussed. The copper(II) cation is coordinated in a highly distorted square-planar geometry to each of the sulphur and amide nitrogen atoms of elesclomol. Electrochemical measurements demonstrate that the complex undergoes a reversible one-electron reduction at biologically accessible potentials. In contrast the free elesclomol is found electrochemically inactive. This evidence is in strong support of the mechanism of action we proposed for the anticancer activity of elesclomol. (C) 2013 Elsevier Inc. All rights reserved.
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