Novel types of modified derivatives and analogues of nucleobases, nucleosides, nucleotides and nucleic acids are designed and prepared for applications in all areas of biomedicinal sciences (medicinal chemistry, biochemistry, chemical biology, bioanalysis etc.).
Basic developments of methodology for the synthesis of these modified biomolecules are performed largely using modern methods (including metal- or enzyme-catalyzed reactions). Biological activity (cytostatic, antiviral etc.) of the novel nucleobases, nucleosides and nucleotides is systematically studied in collaboration with several groups both in academia and in pharmaceutical industry. Several collaborative projects also address chemical biology of nucleic acids (i.e. DNA polymerase specificity and fidelity). Functionalized nucleic acids bearing diverse interesting and useful substituents are another goal of our group. For details, see Projects.
Janoušková, M. et al: "5-(Hydroxymethyl)uracil and -cytosine as potential epigenetic marks enhancing or inhibiting transcription with bacterial RNA polymerase" Chem. Commun. 2017, 53, 13253 – 13255.
Tichý, M. et al: "Synthesis and Cytostatic and Antiviral Profiling of Thieno-Fused 7-Deazapurine Ribonucleosides" J. Med. Chem. 2017, 60, 2411 – 2424.
Downey, A. M. et al: "Synthesis of Nucleosides through Direct Glycosylation of Nucleobases with 5-O-Monoprotected or 5-Modified Ribose: Improved Protocol, Scope, and Mechanism" Chem. Eur. J. 2017, 23, 3910 – 3917.