The ligand and its Cu(II) complexes, [CuLCl(H2O)2] and [CuL(NO3)(H2O)2] were investigated for their anticancer activity against human breast cancer cell line MCF 7. Experiment were done in triplets for concentrations 10−7 M, 10−6 M, 10−5 M and their average values then taken. The results are reported in GI50 (concentration of drug causing 50% inhibition of cell growth). The Adriamycin (ADR) was the positive control. From Table 6, it is concluded that the order of cytotoxicity is [CuL(NO3)(H2O)2] > [CuLCl(H2O)2] > ligand(L). Chelation decreases the polarity [28] and [29] of the metal ion might be because of the partial sharing of its positive charge with the donor groups and possibly the π-electron delocalization within the whole chelate ring system, thus formed during coordination. Coordination increases the lipophilic nature of the central metal atom, which allows permeation through the lipoid layer of the membrane in greater extent.