Browsing by Author "El- Beshti, Hager Sadek"
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thesis.listelement.badge DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY OF NOVEL ANTITUMOR ACTIVE PLATINUM AND COPPER BASED COMPLEXES CONTAINING QUINOXALINE LIGANDS(2022-03-10) El- Beshti, Hager Sadek; ÖZALP YAMAN, Şeniz; chemistryAcross the globe, today, cancer accounts for many fatalities, thus calling for better and updated antineoplastic agents within biomedicine and health sciences. In this regard, inorganic chemistry for pharmaceutic purposes is essential in creating drugs based in metal to fight cancer as such medicine has been shown to be potentially effective to fight cancer in humans. In light of this background, this research focuses on synthesis and anticancer activity of (2,3-di-pyridin-2-yl-quinoxaline), (2,3-di-thenyl-2-yl quinoxaline), (2,3,2',3'-tetra-pyridin-2-yl-[6,6']biquinoxaline) and (2,3,2',3'-tetra thenyl-2-yl-[6,6']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 (HSA) of the complexes were assessed with UV titration, thermal decomposition, viscometric, and fluorometric measurements. The nature of the binding of the complexes on DNA were revealed as electrostatic interaction between the cationic metal complex ions and the negative phosphate groups of CT DNA upon removal of one or two labile chloride ion(s), except Pt(tpbq)Cl2, Pt(ttbq)Cl2, and Cu(tpbq)Cl2; van der Waals and hydrogen bonds interaction were proposed for these complexes. In addition, our complexes induced a surface contact through the hygroscopic region of serum albumin. Antitumor activity of the complexes against human glioblastoma A172, LN229, and U87 cell lines and human lung A549, human breast MDA-231, human cervix HeLa, and human prostate PC-3 cell lines were investigated by examining cell viability (MTT), oxidative stress, apoptosis-TUNEL, in vitro migration an invasion, in vitro Comet DNA demage, 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(dtq)2Cl2, 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. Wound healing and invasion analysis results also supported the higher anticancer activity of those complexes.