Anti-Cancer Discovery & Therapy (Track)


Liliana Agnieszka Mazur, B. Modzelewska-Banachiewicz, R. Bursa, J. Wietrzyk, K. Kepinska


In recent years a considerable effort has been focused on the development of new metal-based anticancer drugs with different modes of DNA interactions like hydrogen-bonding and π.π stacking interactions that bind and cleave DNA under physiological conditions. [1, 2] Copper(II) complexes seem to be the best candidates as they are less toxic than e.g. platinum derivatives, possess biologically accessible redox potential and demonstrate high nucleobase affinity. Due to these
properties they can bind and cleave the DNA molecules under both oxidative and hydrolytic conditions.

The results of our research on novel N1-acylamidrazone derivatives and their Cu(II) complexes indicated that the latter are of interest as potential antitumor drugs. The antiproliferative effect of the parent ligands and their Cu(II) complexes was tested in vitro in the cultures of different [HT-29/CX-1, HL-60 and MCF-7] tumor cell lines. The tested metal complexes significantly inhibited the growth of colon carcinoma cell lines (HT-29, CX-1). What is more, they exhibited about 50-fold lower cell toxicity as compared to cisplatin, which makes them particularly interesting as drugs. Similarly, very low toxicity was observed for the parent amidrazone ligands but their efficiency in tumor cell growth inhibition was much lower. Thus, the pharmacological tests revealed that the coordination effect improves the biological activity of all analyzed amidrazone ligands. However, the potential of the Cu(II) complexes studied so far depends on the type of ligand as well as overall structure and composition of the complex.

Keywords: N1-acylamidrazones, Cu(II) complexes, anticancer activity.


[1] I. Meistermann , V. Moreno, M.J. Prieto, E. Molderheim, E. Sletten, S. Khalid, P.M. Rodger, M.J. Hannon, Proc. Natl. Acad. Sci. U.S.A. 99 (2002) 5069.

[2] P. Jaividhya, R. Dhivya, M.A. Akbarsha, M. Palaniandavar, J. Inorg. Biochem. 114 (2012) 94.