| Summary: | Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Lucie Kolbabová Supervisor: Doc. PharmDr. Tomáš Šimůnek, Ph.D. Title of diploma thesis: Study of the antipoliferative properties of the series of novel aroylhydrazone iron chelators Aroylhydrazones are tridental lipophilic iron chelators with good cell-membrane permeability. In the last decades some compounds of this chemical group have been demonstrated to have a significant antiproliferative activity. Salicylaldehyde isonicotinoyl hydrazone (SIH), an aroylhydrazone with an oral availability, showed a significant antiproliferative activity in previous experiments in our laboratory as well as the ability to protect cells from the oxidative stress- induced damage. The main disadvantage of SIH is low stability caused by rapid hydrolysis of the hydrazone bond in aqueous environment. To deal with this issue, the Department of Organic and Inorganic Chemistry of the Faculty of Pharmacy (Charles University) designed and synthesized analogues of SIH, derived from aromatic ketones, which showed significantly improved stability in rabbit plasma in comparison with the parent SIH. The aim of this study is to expand the previous experiments and it is focused on further structure modifications of the...
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