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New Nucleoside Analogues With Modified Sugar Moiety

Domenii publicaţii > Chimie + Tipuri publicaţii > Articol în revistã ştiinţificã

Autori: Tanase C, Cocu FG, Caproiu MT, Draghici C, Neagoe I, Manda G

Editorial: Revista de Chimie (Bucuresti), 58(8), p.822-829, 2007.

Rezumat:

The development of new drugs with antitumor and antiviral activity that exhibit greater efficacy, more favorable toxicity profile, less-susceptible to cross-resistance request a continuous effort to synthesize also new biologically active nucleoside analogues, modified at the base or, more frequently, at the sugar moiety.
In this effort we replace the sugar moiety with a functionalized oxabicyclo [3.3.0]octane fragment from Cloprostenol prostaglandin analogue synthesis, in optically activity form, maintaining unmodified the pyrimidine bases and build the new nucleoside using adequate synthetic methods. The compounds were characterized by IR, 1H-NMR and 13C-NMR spectra.
Preliminary in vitro preclinical investigations were performed for establishing the potential anti-neoplastic action of the newly synthesized nucleoside analogues. Experimental data reveal that U-34 and IU-34, but not T-34, might be potential candidates for anti-tumor therapy. Some issues are raised regarding IU-34 that inhibits tumor progression, but also the immune response. The action of U-34 is highly dependent on the tumor cell type and it exerts no major effect on normal resting lymphocytes.

Cuvinte cheie: nucleoside analogs, Jurkat lymphoblasts, U937 cell line, mononuclear cells