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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

DNA Binding and Anticancer Activity of Novel Cyclometalated Platinum (II) Complexes

Author(s): Roghayeh Mohammadi, Reza Yousefi, Marzieh Dadkhah Aseman, S. Masoud Nabavizadeh and Mehdi Rashidi

Volume 15, Issue 1, 2015

Page: [107 - 114] Pages: 8

DOI: 10.2174/1871520614666141203143543

Price: $65


This study describes anticancer activity and DNA binding properties of two cyclometalated platinum (II) complexes with non-leaving lipophilic ligands; deprotonated 2-phenylpryidine (ppy): C1 and deprotonated benzo[h] quinolone (bhq): C2. Both complexes demonstrate significant anticancer activity and were capable to stimulate Caspase-III activity in Jurkat cancer cells. The results of Acridine orange/Ethidium bromide(AO/EtB), along with those of Caspase-III activity suggest that these complexes can induce apoptosis in the cancer cells. Moreover, C1 with flexible chemical structure indicates considerably higher anticancer activity than C2 which possesses a higher structural rigidity. Additionally, C2 represents a complex which is in part inducing cancer cell death due to the cell injury (necrosis). The absorption spectra of DNA demonstrate a hypochromic effect in the presence of increasing concentration of these complexes, reflecting DNA structural alteration after drug binding. Also, EtB competition assay and docking results revealed partial intercalation and DNA groove binding for the metal complexes. Overall, from the therapeutic point of view, ppy containing platinum complex (C1) is a favored anticancer agent, because it induces signaling cell death (apoptosis) in cancer cells, and lacks the necrotic effect.

Keywords: Anticancer activity, absorption spectra, caspase-III activity, cyclometalated platinum (II) complexes, molecular docking.

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