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	Bi-substrate inhobitors of human pyrimidine 5’-nucleosidases Šimák, Ondřej ; Pachl, Petr ; Jandušík, T. ; Brynda, Jiří ; Buděšínský, Miloš ; Rosenberg, Ivan The work is aimed at the synthesis of bi-substrate inhibitors of 5’-nucleosidases. The pyrimidine nucleobase of lead compound was derivatized in the 5-position with various phosphonic acids differing in conformational flexibility and in the length of alkyl side chain carrying phosphonate group. The phosphonic acid with optimal linker can reach the phosphate binding side and make strong interaction with the enzyme. Inhibition activity of such inhibitors and crystal structure of inhibitor-enzyme complex will be presented. Detailed record
	Enzymatic decomposition of a locked nucleoside phosphoramidate monitored by 31P NMR spectroscopy Procházková, Eliška ; Hřebabecký, Hubert ; Nencka, Radim ; Dračínský, Martin Phosphoramidate derivatives are often used as prodrugs of modified nucleosides. The crucial step for the biologically active compound release in cells is then enzymatic hydrolysis of the phosphoramidate derivative. The enzymatic decomposition of a nucleoside prodrug 1 was monitored using 31P NMR spectroscopy and the structure of the reaction products was determined by 1D and 2D (COSY, HSQC, HMBC) NMR experiments and compared with the products obtained with non-enzymatic hydrolysis of the prodrug. Detailed record
	Conformation analysis of nucleoside analogues containing selenium and tellurium in five-membered pseudosugar ring Poštová Slavětínská, Lenka ; Pohl, Radek ; Rejman, Dominik The conformation analysis of synthetized thymine and adenosine nucleoside analogues with selenium and tellurium in five-membered pseudosugar ring has been studied. The experimental NMR measurement was complemented with DFT molecular modeling studies. It was found, that ratio between individual conformers in solution depends on the nature of the heteroatom in the five-membered pseudosugar ring. Detailed record
	Pyrrolidine nucleotides conformationally constrained via hydrogen bonding Pohl, Radek ; Poštová Slavětínská, Lenka ; Rejman, Dominik Conformation of pyrroPME nucleotide analogues was studied by means of NMR at different pD values in D2O solutions. Surprisingly, two stable conformers were found at pD > 9 for both cis and trans configurations and their ratio depended on the acid-base properties of nucleobase attached to pyrrolidine ring. The results of conformational analysis suggest that the conformation of the pyrrolidine ring is locked via intramolecular hydrogen bond between negatively charged phosphonate oxygen atom and protonized pyrrolidine nitrogen. Detailed record
	Activation of human RNase L by 5’-C-phosphonate-modified oligoadenylates Petrová, Magdalena ; Buděšínský, Miloš ; Zborníková, Eva ; Panova, Natalya ; Novák, Pavel ; Rosenberg, Ivan Adeno’sine 5’-(S)-C-phosphonate (pCOHX) was prepared as monomer suitable for oligonucleotide synthesis. Modified tetramers pCOHXAAA and pCOHXAApCOHX were assembled on solid phase and evaluated for their ability to activate human RNase L. Detailed record
	Phosphanucleosides containing 1-hydroxymethylphospholane 1-oxide ring Páv, Ondřej ; Zborníková, Eva ; Buděšínský, Miloš ; Rosenberg, Ivan Novel phosphanucleosides containing 1-hydroxymethylphospholane 1-oxide ring were synthesized as compounds with potential biological activity. A ring-closing metathesis was employed to prepare a phospholene precursor, which was then converted into either 4-azido-3-hydroxy-1-hydroxymethylphospholane 1-oxide or 3-azido-1- hydroxymethylphospholane 1-oxide derivatives. Subsequently, nucleobase was introduced using a nucleobase construction. The biological activity of prepared compounds was evaluated. Detailed record
	Sulfur-containing phosphonate monomers for oligonucleotide synthesis Kostov, Ondřej ; Zborníková, Eva ; Buděšínský, Miloš ; Novák, Pavel ; Rosenberg, Ivan A series of novel compounds, protected S-MOP nucleoside-5’-O-methylphosphonothioates, was prepared as monomers for solid phase synthesis of phosphonothioate oligonucleotides. In addition we have examined the synthetic potential of nucleoside-5’-O-methyl-(H)-phosphinates for phosphonate oligonucleotide assembly. Detailed record
	Switchable intramolecular hydrogen bond in polysubstituted 5-nitrosopyrimidines Procházková, Eliška ; Čechová, Lucie ; Žurek, Jiří ; Janeba, Zlatko ; Dračínský, Martin The formation of strong intramolecular hydrogen bonds was observed in a series of 2-amino-5-nitrosopyrimidines with alkylamino and arylamino substituents in the positions 4 and 6. Mixtures of two rotamers differing in the orientation of the nitroso group were observed in the NMR spectra of the compounds where two distinct intramolecular hydrogen bonds could be formed. In several cases, we were able to isolate and characterize the two hydrogen bond isomers (two conformers) by column chromatography. The ratio of the two rotamers in equilibrium depends strongly on the character of the substituents in the positions 4 and 6 and can be finely tuned in a broad range of conformation ratios. The experimental results were supported by DFT calculations. Detailed record

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