| Abstract |
The topic of the project will be the synthesis of novel base-modified nucleosides and nucleotides (N- or C-nucleosides), including those with an additional functional group (redox or fluorescent marker). Cytostatic and antiviral activity of the resulting nucleosides will be studied. The corresponding nucleoside triphosphates will be prepared and studied as potential inhibitors or substrates for DNA or RNA polymerases and some of them will be used for construction of modified nucleic acids.
Key references:
1. Štambaský, J.; Hocek, M.; Kočovský, P. "C-Nucleosides: Synthetic Strategies and Biological Applications" Chem. Rev. 2009, 109, 6729-6764.
2. Raindlová, V.; Pohl, R.; Šanda, M.; Hocek, M. "Direct polymerase synthesis of reactive aldehyde-functionalized DNA and its conjugation and staining with hydrazines" Angew. Chem. Int. Ed. 2010, 49, 1064-1066.
3. Nauš, P.; Pohl, R.; Votruba, I.; Džubák, P.; Hajdúch, M.; Ameral, R.; Birkuš, G.; Wang, T.; Ray, A. S.; Mackman, R.; Cihlar, T.; Hocek, M. "6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents" J. Med. Chem. 2010, 53, 460-470.
4. Urban, M.; Joubert, N.; Purse, B.; Hocek, M.; Kuchta, R. "Mechanisms by which Human DNA Primase Chooses to Polymerize a NTP" Biochemistry 2010, 49, 727-735. |
