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Cyclodextrin-drug conjugates equipped with targeting groups as anticancer agents
Lamačová, Lucie Josefa ; Jindřich, Jindřich (advisor) ; Smrček, Stanislav (referee)
This diploma thesis deals with the synthesis of conjugates of cyclodextrin with the anticancer drug 5-fluorouracil and folic acid, which works as a targeting group. 5-Fluorouracil is connected to cyclodextrin via an acid-labile linker, which is expected to be cleaved in decreased pH in the proximity of malignant tissue or in the endosome. Malignant tissue also overexpresses receptor for folic acid, and this phenomenon is used for targeted delivery of therapeutic agents. Cyclodextrins are cyclic oligosaccharides, which are known for their ability to complex various compounds into their hydrophobic cavity and increase solubility, stability and bioavailability of these compounds. A synthetic approach for the preparation of conjugate of cyclodextrin with 5-fluorouracil and folic acid was designed and the conjugate was subsequently synthesized. Key words: cyclodextrin, fluorouracil, targeting group, folic acid, drug delivery
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2-(Phosphonomethoxy)ethyl derivatives of 6-fluoro-3-hydroxypyrazine-2-carboxamide
Lamačová, Lucie Josefa ; Jindřich, Jindřich (advisor) ; Baszczyňski, Ondřej (referee)
This bachelor thesis deals with the preparation of derivatives of acyclic nucleoside phosphonates with nitrogenous base favipiravir. There are many examples of acyclic nucleoside phosphonates that are used as antiviral drugs due to their structure. Favipiravir shows antiviral activity against the influenza virus. The target compounds thus might have the potential to be biologically active, which will be tested in virological laboratories at KU Leuven in Belgium. First, the methods for preparation of 2-(phosphonomethoxy)ethyl derivative of favipiravir was designed, then for its diphosphate and a prodrug with pivaloyloxymethyl groups to increase the bioavailability of the compound. Thus, 2-(phosphonomethoxy)ethyl derivatives of favipiravir and its de-fluoro analogue were prepared. Key words: acyclic nucleoside phosphonates, T-705, favipiravir, T-1105, influenza, antiviral activity
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