999C1a:GA13-26526S - Výsledky hledání - Digitální repozitář

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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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam
	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. Úplný záznam

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