|
|
Analytical and bioanalytical assessment of novel anticancer drugs
Šesták, Vít ; Štěrbová, Petra (advisor) ; Bednář, Petr (referee) ; Šatínský, Dalibor (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Mgr. Vít Šesták Supervisor - specialist: PharmDr. Ján Stariat, Ph.D. Supervisor: doc. PharmDr. Petra Kovaříková, Ph.D. Title: Analytical and bioanalytical assessment of novel anticancer drugs Pharmaceutical analysis plays an indispensable role in the development of novel safer, cheaper and more effective drugs and chaperones them from their first synthesis throughout their existence. To date, the method most commonly used in pharmaceutical analysis is liquid chromatography (LC) with various detection modalities. Separation via LC enables analysis of very complex mixtures such as biological samples or samples from stability studies. The soaring interest in LC hyphenated with mass spectrometry (MS) in pharmaceutical analysis is partly due to its increasing affordability and mainly due to its ability to separate the molecules of the analyte according to their mass-to-charge ratio (m/z). The additional dimension of separation grants it a superior selectivity. In addition, MS provides priceless information on the structure of the analyte - be it the m/z or fragmentation spectra. In its theoretical part, this dissertation deals with basic description of liquid...
|
|
|
Bioanalytical evaluation of novel drug candidates from the group of thiosemicarbazones I.
Šesták, Vít ; Kovaříková, Petra (advisor) ; Kučera, Radim (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of pharmaceutical chemistry and drug analysis Candidate: Vít Šesták Supervisor: PharmDr. Petra Kovaříková, PhD. Title of the Master's Thesis: Bioanalytical assessment of new prospective drugs derived from thiosemicarbazone I. Abstract Development of novel anti-cancer drugs which would boost current therapeutic regimes and/or overcome the resistance against common chemotherapy ranks among the most progressive fields of modern drug discovery. Selective targeting of intracellular iron (Fe) has been recognized as a new strategy for anti-cancer drug development. Biocompatible Fe chelators structurally derived from thiosemicarbazone belong to the most intensively studied anti-cancer agents. Apart from Triapine, currently in phase II of a clinical trial, the systematic investigation led to development of a new generation of iron chelators - di-2-pyridylketone thiosemicarbazones (DpTs). Based on the outcomes of numerous in vitro and in vivo experiments and di-2-pyridylketone-4,4-dimethyl-3-thiosemicarbazone (Dp44mT) was selected as the lead compound for further development. The aim of this study was to develop an LC-MS method for the analysis of Dp44mT and its main phase I metabolites in biological materials (plasma, urine and faeces)....
|
|
|
Extraction of amphetamines and synthetic cathinones from breast milk using liquid membrane microextraction techniques
Zajíčková, Šárka ; Bavlovič Piskáčková, Hana (advisor) ; Šesták, Vít (referee)
Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Faculty of Pharmacy in Hradec Králové Candidate Mgr. Šárka Zajíčková Consultant Mgr. Hana Bavlovič Piskáčková, Ph.D. Title of Thesis Extraction of amphetamines and synthetic cathinones from breast milk using liquid membrane microextraction techniques Amphetamine-type stimulants (ATSs) refer to a group of pharmacological and toxicological agents that have a common phenethylamine structural backbone. In addition to their limited pharmacological use, they are primarily abused as recreational drugs due to their psychostimulant effects. They currently represent the second largest group of illicit used drugs in the world. the second largest group of illicit used drugs in the world. The main representatives of this group include amphetamine (AMF, speed), methamphetamine (MAMF, pervitin) or 3,4-methylenedioxy-N-methamphetamine (MDMA, ecstasy). This ATSs also includes synthetic cathinones, which belong to the group of new psychoactive substances (NPS), which are primarily synthesized in order to circumvent the law, because they are often not included in the list of prohibited drugs. All of these compounds are low molecular weak bases which are widely distributed to tissues and biological fluids, including placenta and breast...
|
|
|
Analytical and bioanalytical assessment of novel anticancer drugs
Šesták, Vít ; Štěrbová, Petra (advisor) ; Bednář, Petr (referee) ; Šatínský, Dalibor (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Mgr. Vít Šesták Supervisor - specialist: PharmDr. Ján Stariat, Ph.D. Supervisor: doc. PharmDr. Petra Kovaříková, Ph.D. Title: Analytical and bioanalytical assessment of novel anticancer drugs Pharmaceutical analysis plays an indispensable role in the development of novel safer, cheaper and more effective drugs and chaperones them from their first synthesis throughout their existence. To date, the method most commonly used in pharmaceutical analysis is liquid chromatography (LC) with various detection modalities. Separation via LC enables analysis of very complex mixtures such as biological samples or samples from stability studies. The soaring interest in LC hyphenated with mass spectrometry (MS) in pharmaceutical analysis is partly due to its increasing affordability and mainly due to its ability to separate the molecules of the analyte according to their mass-to-charge ratio (m/z). The additional dimension of separation grants it a superior selectivity. In addition, MS provides priceless information on the structure of the analyte - be it the m/z or fragmentation spectra. In its theoretical part, this dissertation deals with basic description of liquid...
|
|
|
Analytical and bioanalytical assessment of novel anticancer drugs
Šesták, Vít ; Štěrbová, Petra (advisor) ; Bednář, Petr (referee) ; Šatínský, Dalibor (referee)
Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Candidate: Mgr. Vít Šesták Supervisor - specialist: PharmDr. Ján Stariat, Ph.D. Supervisor: doc. PharmDr. Petra Kovaříková, Ph.D. Title: Analytical and bioanalytical assessment of novel anticancer drugs Pharmaceutical analysis plays an indispensable role in the development of novel safer, cheaper and more effective drugs and chaperones them from their first synthesis throughout their existence. To date, the method most commonly used in pharmaceutical analysis is liquid chromatography (LC) with various detection modalities. Separation via LC enables analysis of very complex mixtures such as biological samples or samples from stability studies. The soaring interest in LC hyphenated with mass spectrometry (MS) in pharmaceutical analysis is partly due to its increasing affordability and mainly due to its ability to separate the molecules of the analyte according to their mass-to-charge ratio (m/z). The additional dimension of separation grants it a superior selectivity. In addition, MS provides priceless information on the structure of the analyte - be it the m/z or fragmentation spectra. In its theoretical part, this dissertation deals with basic description of liquid...
|
|
|
Bioanalytical evaluation of novel drug candidates from the group of thiosemicarbazones I.
Šesták, Vít ; Kovaříková, Petra (advisor) ; Kučera, Radim (referee)
Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of pharmaceutical chemistry and drug analysis Candidate: Vít Šesták Supervisor: PharmDr. Petra Kovaříková, PhD. Title of the Master's Thesis: Bioanalytical assessment of new prospective drugs derived from thiosemicarbazone I. Abstract Development of novel anti-cancer drugs which would boost current therapeutic regimes and/or overcome the resistance against common chemotherapy ranks among the most progressive fields of modern drug discovery. Selective targeting of intracellular iron (Fe) has been recognized as a new strategy for anti-cancer drug development. Biocompatible Fe chelators structurally derived from thiosemicarbazone belong to the most intensively studied anti-cancer agents. Apart from Triapine, currently in phase II of a clinical trial, the systematic investigation led to development of a new generation of iron chelators - di-2-pyridylketone thiosemicarbazones (DpTs). Based on the outcomes of numerous in vitro and in vivo experiments and di-2-pyridylketone-4,4-dimethyl-3-thiosemicarbazone (Dp44mT) was selected as the lead compound for further development. The aim of this study was to develop an LC-MS method for the analysis of Dp44mT and its main phase I metabolites in biological materials (plasma, urine and faeces)....
|
guest ::
RSS feed.