Résumé : A mononuclear copper (II) complex of N-2-hydroxyhippuric acid (2HHA), [Cu(HA)(H2O)2], has been synthesized and characterized by spectroscopic and X-ray powder diffraction studies. Crystal structure of [Cu(HA)(H2O)2] reveals a distorted square-pyramidal geometry around the metal center. The crystal packing in the complex exhibits a three-dimensional framework formed by intermolecular O[BOND]; H···O and C[BOND]H···O hydrogen bonds. Toxicity and antitumor properties of the complex have been studied in vivo. The complex, capable of depleting glutathione (GSH) at nontoxic doses, may be utilized to sensitize drug-resistant cells where resistance is due to an elevated level of GSH. Copyright © 2009 John Wiley & Sons, Ltd.