Antiproliferative Activity of Platinum(ii) and Copper(ii) Complexes Containing Novel Biquinoxaline Ligands

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2024

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Oxford Univ Press

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Chemical Engineering
(2010)
Established in 2010, and aiming to train the students with the capacity to meet the demands of the 21st Century, the Chemical Engineering Department provides a sound chemistry background through intense coursework and laboratory practices, along with fundamental courses such as Physics and Mathematics within the freshman and sophomore years, following preparatory English courses.In the final two years of the program, engineering courses are offered with laboratory practice and state-of-the-art simulation programs, combining theory with practice.

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Nowadays, cancer represents one of the major causes of death in humans worldwide, which renders the quest for new and improved antineoplastic agents to become an urgent issue in the field of biomedicine and human health. The present research focuses on the synthesis of 2,3,2MODIFIER LETTER PRIME,3MODIFIER LETTER PRIME-tetra(pyridin-2-yl)-6,6MODIFIER LETTER PRIME-biquinoxaline) and (2,3,2MODIFIER LETTER PRIME,3MODIFIER LETTER PRIME-tetra(thiophen-2-yl)-6,6MODIFIER LETTER PRIME-biquinoxaline) containing copper(II) and platinum(II) compounds as prodrug candidates. The binding interaction of these compounds with calf thymus DNA (CT-DNA) and human serum albumin were assessed with UV titration, thermal decomposition, viscometric, and fluorometric methods. The thermodynamical parameters and the temperature-dependent binding constant (KMODIFIER LETTER PRIMEb) values point out to spontaneous interactions between the complexes and CT-DNA via the van der Waals interactions and/or hydrogen bonding, except Cu(ttbq)Cl2 for which electrostatic interaction was proposed. The antitumor activity of the complexes against several human glioblastomata, lung, breast, cervix, and prostate cell lines were investigated by examining cell viability, oxidative stress, apoptosis-terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling, in vitro migration and invasion, in vitro-comet DNA damage, and plasmid DNA interaction assays. The U87 and HeLa cells were investigated as the cancer cells most sensitive to our complexes. The exerted cytotoxic effect of complexes was attributed to the formation of the reactive oxygen species in vitro. It is clearly demonstrated that Cu(ttbq)Cl2, Pt(ttbq)Cl2, and Pt(tpbq)Cl2 have the highest DNA degradation potential and anticancer effect among the tested complexes by leading apoptosis. The wound healing and invasion analysis results also supported the higher anticancer activity of these two compounds. Graphical Abstract Antitumor activity of biqunoxaline complexes.

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Kayi, Hakan/0000-0001-7300-0325; Cetin, Yuksel/0000-0001-5101-3870; Ozalp Yaman, Seniz/0000-0002-4166-0529; Elbeshti, Hager/0000-0002-3027-0859

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Cu(II) and Pt(II) biquinoxalines, DNA/HSA binding, DNA cleavage, Apoptosis, Invasion/migration assay, ROS generation

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16

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2

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