Autor: Brulíková, L.; Hlaváč, J.
Název práce v češtině: Syntéza analog uridinu substituovaných v poloze 5 a studium jejich biologické aktivity.
Název práce v angličtině: SYNTHESIS OF 5-MODIFIED URIDINE ANALOGUES AND STUDY OF THEIR CYTOTOXIC ACTIVITY

Abstrakt česky: Pozornost této práce je zaměřena na syntézu 5-substituovaných pyrimidinových nukleobází a studium jejich biologicke aktivity. Byla syntetizována série 5-alkoxymethyl a 5-[alkoxy-(4-nitrophenyl)-methyl]uridinů a studována cytotoxická aktivita v závislosti na délce alkylového řetězce.
Abstrakt anglicky: Our interest has been aimed at the 5 position of pyrimidine nucleobases and discovery of new anticancer agent. A series of uridine analogues modified at the 5-positon by either 5-alkoxymethyl or 5-[alkoxy-(4-nitrophenyl)-methyl] moiety were synthesized (Scheme 1). Firstly, we have focused on the synthesis of 5-[alkoxy-(4-nitrophenyl)-methyl]-uridines with the alkyl chain lengths C6-C9. Nucleosides were formed as a mixture of two diastereoisomers that have been separated and tested for their cytotoxic activity in vitro against different cancer cell lines. Relationships between structure and above mentioned activity were studied. Cytotoxic activity has been slightly increased in some cases by the transformation of bases to nucleosides. Furthermore, we have found growing tendency of cytotoxic activity with the growing length of alkyl chain. Subsequently, we have modified the 5 position of uridine by 5-alkoxymethyl moiety and relationships between structure and cytotoxic activity will be studied. With respect to the mentioned growing tendency of anticancer activity of 5-[alkoxy-(4-nitrophenyl)-methyl]-uridines the derivatives with longer chain seem to be promising in future biological activity studies.
Jazyk v originále: angličtina
Publikace abstraktu: ChemZi 5/9, 93, 2009
Forma prezentace: přednáška

Místo konání: Vysoké Tatry, Tatranské Matliare (Slovensko)
Datum konání: September 7 – 11

Způsob financování: MSM 619895216