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In vitro study of novel catalytic inhibitors of topoisomerase II.
Trnka, Tomáš ; Šimůnek, Tomáš (advisor) ; Macháček, Miloslav (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Tomáš Trnka Supervisor: Prof. PharmDr. Tomáš Šimůnek, PhD. Title of diploma thesis: In vitro study of new catalytic topoisomerase II inhibitors A wide range of drugs of different groups can be used for the pharmacotherapy of cancer. One of them are anthracycline antibiotics, which have been used in chemotherapy since the second half of the 20th century. Despite of their usage, there is still widespread concern about myocardial damage due to their cardiotoxic effect. The only cardioprotective agent, which is used is dexrazoxane (DEX). The mechanism of its effect has been traditionally supposed to consist on iron ion chelation, but recently, attention has shifted to its effects on topoisomerase II (TOP2), which could be the key element in the development of anthracycline cardiotoxicity. Apart from the positive effects on treatment, DEX has been also connected with its negative impact, due to the possible occurrence of acute lymphoblastic leukemia (ALL) or myelodysplastic syndrome. The aim of our work was to assess the effects of other TOP2 catalytic inhibitors - novobiocin (NB), merbarone (MER), BNS-22, suramin (SUR) and also XK-469, for which was synthesized a series of analog substances...
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In vitro study of novel catalytic inhibitors of topoisomerase II.
Trnka, Tomáš ; Šimůnek, Tomáš (advisor) ; Macháček, Miloslav (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Biochemical Sciences Candidate: Tomáš Trnka Supervisor: Prof. PharmDr. Tomáš Šimůnek, PhD. Title of diploma thesis: In vitro study of new catalytic topoisomerase II inhibitors A wide range of drugs of different groups can be used for the pharmacotherapy of cancer. One of them are anthracycline antibiotics, which have been used in chemotherapy since the second half of the 20th century. Despite of their usage, there is still widespread concern about myocardial damage due to their cardiotoxic effect. The only cardioprotective agent, which is used is dexrazoxane (DEX). The mechanism of its effect has been traditionally supposed to consist on iron ion chelation, but recently, attention has shifted to its effects on topoisomerase II (TOP2), which could be the key element in the development of anthracycline cardiotoxicity. Apart from the positive effects on treatment, DEX has been also connected with its negative impact, due to the possible occurrence of acute lymphoblastic leukemia (ALL) or myelodysplastic syndrome. The aim of our work was to assess the effects of other TOP2 catalytic inhibitors - novobiocin (NB), merbarone (MER), BNS-22, suramin (SUR) and also XK-469, for which was synthesized a series of analog substances...
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Comparing the feelings of participants in the intensive course of the Feldenkrais method in 2014 and 2016
Trnka, Tomáš ; Vařeková, Jitka (advisor) ; Strnad, Pavel (referee)
Title: Comparing the feelings of participants in the intensive course of the Feldenkrais method in 2014 and 2016 Background: The Moshé Feldenkrais exercise system - Awareness Through Movement (ATM) uses slow, conscious movements to support motor learning. Exercise not only improves motor patterns, but also improves other body functions, including the psyche. However, there are few research papers that examined the effects on larger scope. Objectives: The aim of the research was to compare the subjective feelings of participants of the intensive ATM courses organized annually at the Faculty of Physical Education and Sport of Charles University in 2014 and 2016. Methods: In order to achieve the aim of the research, quantitative qualitative comparison of the results of the questionnaire survey from two three-day courses of the Feldenkrais method in 2014 and 2016 was used. The structure of the questionnaires was based on the basic demographic data of the participants, their motivation to take part in the course and the subjective evaluation of the course (benefit from exercise, reduction of pain etc.). Likert scale was used to subjectively evaluate the course (exercise enjoyment, pain reduction, etc.). Results: In 2014, 121 participants attended the ATM course and 99 completed questionnaires were...
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Study of porphyrins substituted wich glycosylated steroids
Zelenka, Karel ; Trnka, Tomáš (advisor) ; Jindřich, Jindřich (referee) ; Kefurt, Karel (referee) ; Pouzar, Vladimir (referee)
I I 4. Conclusions This work is focused on syntheses of new zeso-substituted porphyrins containing glycosylated-steroid moieties and study oftheir physico-chemical and supramolecular propertres. In the first part oť this work, procedure for the synthesis of B glycosides 4 or 5 is described. No ťormation of ortohoesters was observed. Next part of this work consists oť searching for suitable protecting group for a saccharide part oť molecule and preparation of steroidaldehydes.Protectedglycosides10, ll,tó, 17,|9a+l9band20wereprepared.Suitable method for preparation ofaldehydes 14, 15, 23,24,29,30 an.34 is described (chapter 3.1). Following part of work describes preparation of porphyrins with protected sugar moiety. Symmetrical Al type porphyrins 35-41 were prepared. Also preparatio n of trans-A2ts1 ýpe porphyrins 43, 44 and A]B type 45, 4ó is described. Preparation oť porphyrins 47.50 with deprotected hydroxyl groups is described (Chapter 3.2). Solvent driven aggregation behavior oť the porphyrins was studied in aqueous solvent mixtures' Formation of aggregates of porphyrin 45 was proved using uv-vis spectroscopy (Chapter 3.3). Considering use oť prepared porphyrins in electrochemistry as a possible electrochemical sensors, polarographic and voltametric studies oť porphyrins 47-19 were per|ormed and showed...
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Preparation of bifunctional organocatalysts
Rohaľová, Dominika ; Veselý, Jan (advisor) ; Trnka, Tomáš (referee)
This bachelor thesis deals with the synthesis of bifunctional thiourea catalysts and corresponding building blocks derived from levoglukosane. The first part was of this thesis is focused on the preparation 1,6:2,3-dianhydro-4-azido-4-deoxy-β-D-mannose. The second part of the thesis is deals with the preparation od bifunctional catalyst. Keywords Asymmetric synthesis, organocatalysis, saccharides, bifunctional calatysts, thiourea, morpholine.
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Synthesis of cycles using organocatalysis and catalysis with metal complexes
Hurný, David ; Veselý, Jan (advisor) ; Trnka, Tomáš (referee)
This thesis deals with an enantioselective synthesis of cyclic compounds by using a combination of organocatalysis and transition metal catalysis. The thesis deals mainly with usage of aminocatalyst for activation of aldehydes and copper catalyst for activation of terminal triple bond. The first part is focused on the preparation of starting compounds for cyclizations (α-oxoesters, α- substituted nitroalkanes and α-substituted aldehydes). The second part concerns carbocyclization itself and optimization of reaction conditions to achieve highly stereoselective reaction. Powered by TCPDF (www.tcpdf.org)
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