Synthesis, structural characterization and antitumor activity evaluations of copper complex with tetraazamacrocyclic ligand

Cu (II) complex with 1,4,7,10-tetrakis(2-cyanoethyl-)-1,4,7,10 tetraazacycl ododecane was prepared and characterized by X-ray diffraction. Four nitroge n atoms of macrocyclic ligand and oxygen atom of water molecule defined a t etragonal pyramidal polyhedron surrounding the central copper atom. Prelimi nary pharmacological tests showed that it had antitumor activity against P3 88 and BEL-7404 cell lines in vitro. Also it exhibited perturbation effects to K562 tumor cell lines at G(0)-G(1) stage and further studies showed tha t it can cleave supercoiled DNA( pBR 322) to nicked and linear DNA in aerob ic condition. (C) 1999 Elsevier Science Ltd. All rights reserved.