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Synthesis of xanthone derivates for in vitro and in vivo biological activity studies
Široká, Jitka ; Zimčík, Petr (advisor) ; Opletalová, Veronika (referee)
Synthesis of xanthone derivatives for in vitro and in vivo biological activity studies J. Siroka Xanthone derivatives are heterocyclic compounds with the dibenzo-γ-pyrone as the main molecular moiety. They contain different types of substituents in different positions, leading to a large variety of pharmacological activities. 3,4-Dihydroxyxanthone was revealed as a hit compound in a study involving the investigation of the inhibitory effect of oxygenated xanthones on several human tumor cell lines. In order to obtain enough quantity for in vivo assays and for further molecular modifications, the synthesis of 3,4-dihydroxyxanthone was accomplished: the condensation of 1,2,3-trimethoxyphenol with the appropriate substituted benzoyl chloride (2-methoxybenzoyl chloride) afforded benzophenone (2-hydroxy-2',3,4- trimethoxy benzophenone) which was further cyclized to give 3,4-dimethoxyxanthone. The 3,4-dimethoxyxanthone was demethylated to furnish 3,4- dihydroxyxanthone. Additionally, the synthesis of reactive formylated derivatives of xanthones, 1- formyl-3,4-dihydroxyxanthone and 1-formyl- 3,4-dimethoxyxanthone, was attempted by Duff formylation. Only 1-formyl-3,4- dihydroxyxanthone was obtained. Due to a small amount of 3,4-dihydroxyxanthone obtained from the first synthesis, the synthesis was repeated...
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Development of Electrophoretic Methods for the Analysis of Biologically Active Compounds using Complex Formation
Široká, Jitka ; Polášek, Miroslav (advisor) ; Štěrbová, Petra (referee) ; Opatřilová, Radka (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Analytical Chemistry Candidate Mgr. Jitka Široká Supervisor Doc. RNDr. Miroslav Polášek, CSc. Title of Doctoral Thesis Development of electrophoretic methods for the analysis of biologically active compounds using complex formation The disertation is dealing with the development of capillary electrophoretic methods with spectrophotometric detection for the determination of biologically active substances in forensic, clinical and pharmaceutical fields. Theoretical background to the individual experimental parts is presented in the Introduction. Basic principles of capillary electrophoresis are explained, problems of separation selectivity and sensitivity are discussed and the analytes under study are characterised. The first experimental part is devoted to electrophoretic determination of chlorophenylpiperazine isomers (ortho, meta, para) in confiscated pills using cyclodextrins as selectors in acidic phosphate buffer. The second experimental part is devoted to the determination of urinary 8-hydroxy-2'-deoxyguanosine (an oxidation stress biomarker) using complex formation with borate including sample pretreatment prior analysis and on-line preconcentration by sample stacking in a detection cell with long optical path....
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Synthesis of xanthone derivates for in vitro and in vivo biological activity studies
Široká, Jitka ; Zimčík, Petr (advisor) ; Opletalová, Veronika (referee)
Synthesis of xanthone derivatives for in vitro and in vivo biological activity studies J. Siroka Xanthone derivatives are heterocyclic compounds with the dibenzo-γ-pyrone as the main molecular moiety. They contain different types of substituents in different positions, leading to a large variety of pharmacological activities. 3,4-Dihydroxyxanthone was revealed as a hit compound in a study involving the investigation of the inhibitory effect of oxygenated xanthones on several human tumor cell lines. In order to obtain enough quantity for in vivo assays and for further molecular modifications, the synthesis of 3,4-dihydroxyxanthone was accomplished: the condensation of 1,2,3-trimethoxyphenol with the appropriate substituted benzoyl chloride (2-methoxybenzoyl chloride) afforded benzophenone (2-hydroxy-2',3,4- trimethoxy benzophenone) which was further cyclized to give 3,4-dimethoxyxanthone. The 3,4-dimethoxyxanthone was demethylated to furnish 3,4- dihydroxyxanthone. Additionally, the synthesis of reactive formylated derivatives of xanthones, 1- formyl-3,4-dihydroxyxanthone and 1-formyl- 3,4-dimethoxyxanthone, was attempted by Duff formylation. Only 1-formyl-3,4- dihydroxyxanthone was obtained. Due to a small amount of 3,4-dihydroxyxanthone obtained from the first synthesis, the synthesis was repeated...
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