Bioanalytické hodnocení nových potenciálních léčiv odvozených od thiosemikarbazonu II.

• Main Author: Kollárová, Zuzana
• Other Authors: Kovaříková, Petra
• Format: Dissertation
• Language: Slovak
• Published: 2012
• Online Access: http://www.nusl.cz/ntk/nusl-315715

9 ABSTRACT Charles University in Prague Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control Candidate: Zuzana Kollárová Supervisor: PharmDr. Petra Kovaříková Title of diploma thesis: Bioanalytical evaluation of new potential agents derived from thiosemicarbazone II. Nowadays, malignant neoplasms (cancer) are listed as the 4th most frequent cause of death. Therefore, its successful therapy and proper drug treatment attract scientific attention all over the world. New potent anticancer agent, 2-benzoylpiridine-4-ethyl-3- thiosemicarbazone (Bp4eT), developed by Prof. D. Richardson (University of Sydney, Australia) was identified as a leading compound of the 2-benzoylpiridine thiosemicarbazone series. These compounds, known as iron chelators, were originally developed to treat metabolic iron overload but recent investigations revealed their antiproliferative properties and highly selective mechanism of action in the therapy of malignant neoplasms. In this study optimal conditions for HPLC-MS analysis of Bp4eT and its degradation products were developed. Also, di(2-pyridilketone)-4-phenyl-3-thiosemikarbazone (Dp4pT) was chosen as an internal standard. Previous studies, during which Bp4eT was incubated with rat and human liver microsomal fractions, confirmed oxidative way...