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Organic Chemistry

Tutor Prof. Ing. Michal Hocek, CSc. DSc.

Michal Hocek

Topic Synthesis of novel nucleosides and nucleotides bearing tri- or tetracyclic heterocyclic bases

Novel hetero-fused analogues of deazapurine nucleosides and nucleotides will be designed and prepared for studying of their cytostatic and antiviral activity. Most of them will be based on new or scarcely studied tri- or tertacyclic heterocyclic systems. In addition to testing of biological activity, selected nucleosides will be converted to NTPs and studied as potential inhibitors or substrates for polymerases in enzymatic synthesis of modified nucleic acids.

Leading references:
1. Tichý, M.; Pohl, R.; Tloušťová, E.; Weber, J.; Bahador, G.; Lee, Y.-J.; Hocek, M. "Synthesis and Biological Activity of Benzo-Fused 7-Deazaadenosine Analogues. 5- and 6-Substituted 4-Amino- or 4-Alkylpyrimido[4,5-b]indole Ribonucleosides" Bioorg. Med. Chem. 2013, 21, 5362-5372.
2. Nauš, P.; Caletková, O.; Konečný, P.; Džubák, P.; Bogdanová, K.; Kolář, M.; Vrbková, J.; Slavětínská, L.; Tloušťová, E.; Perlíková, P.; Hajdúch M.; Hocek, M. "Synthesis, cytostatic, antimicrobial and anti-HCV activity of 6-substituted 7-(het)aryl-7-deazapurine ribonucleosides" J. Med. Chem. 2014, 57, 1097-1110.
3. Tichý, M.; Smoleń, S.; Tloušťová, E.; Pohl, R.; Oždian, T.; Hejtmánková, K.; Lišková, B.; Gurská, S.; Džubák, P.; Hajdúch, M.; Hocek, M. "Synthesis and Cytostatic and Antiviral Profiling of Thieno-fused 7-Deazapurine Ribonucleosides" J. Med. Chem. 2017, 60, 2411-2424.