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Synthesis of tetrapyridoporphyrazines with potential photodynamic activity
Vavrečková, Magda ; Zimčík, Petr (advisor) ; Kučerová, Marta (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department Department of Pharmaceutical Chemistry and Drug Control Candidate Magda Vavrečková Supervisor Doc. PharmDr. Petr Zimčík, Ph.D. Title of Thesis Synthesis of tetrapyridoporphyrazines with potential photodynamic activity Substituted tetrapyridoporphyrazines represent new structural type of potential photosensitizers with interesting properties for application in photodynamic therapy. The aim of this work was to synthesize two types of tetrapyridoporphyrazines with hydrophilic substituents as potential photosensitizers. Photosensitizers are substances with an ability to produce singlet oxygen after activation by light. Singlet oxygen is the key toxic species in photodynamic therapy. 2-Chloro-5,6-dimethylpyridine-3,4-dicarbonitrile (1) was prepared in the first step by condensation of tetracyanoethylene and butan-2-one. In the next step, a hydrophilic substituent was attached by nucleophilic substitution. The first precursor was prepared by reaction of compound 1 with 2-mercaptoethanol in the presence of sodium hydroxide. Similarly, the second precursor was obtained by reaction of compound 1 with diethylaminoethanol in the presence of sodium hydride. The third step involved cyclotetramerization with magnesium butoxide as...
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Chalcones and their analogues as potential drugs VII
Švédová, Lucie ; Kučerová, Marta (advisor) ; Palát, Karel, st. (referee)
CHALCONES AND THEIR ANALOGS AS POTENTIAL DRUGS VII Lucie Švédová Department of pharmaceutical chemistry and drug control, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic Abstract of the rigorous thesis: This synthetic thesis is focused on searching of potential drugs from the group of chalcone derivatives and links up to the long-term studied topic at our department. Antibacterial and antifungal effects are the main examined biological activities. In the theoretical part of this thesis there were arranged various antineoplastic effects of naturally occuring or synthetic chalcones. The bibliographic searches involve items from the last decade. Possible interventions on the level of control processes, proteosynthesis and nucleic acid synthesis, influence on mitosis, apoptosis and the P-glycoprotein and the action on angiogenesis and cancer invasivity were summarized. In addition antioxidant activity and other mechanisms of chemoprevention were introduced as well. Different methods of chalcone synthesis were summed up in conclusion. In the frame of the experimental part substituted derivatives and heterocyclic analogs of chalcones were synthetized by means of condensation reaction. All the synthetic products were characterized by...
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