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New Bicyclo[2.2.1]heptane Nucleoside Analogues as Antitumor Agents

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

Autori: Tanase C, Cocu FG, Caproiu MT, Neagu M, Manda G

Editorial: Revista de Chimie (Bucuresti), 60(2), p.147-151, 2009.


For the development of new nucleoside drugs with antitumor activity we replace the sugar moiety of pyrimidine nucleoside with a functionalized bicyclo[2.2.1]heptane fragment. The starting optically active compound (9) from prostaglandin analogues synthesis, was transformed in 4 steps in the key intermediate (13) in optically activity form, and coupled by Mitsunobu reaction to N4-benzoylcytosine and 5-fluorouracil, resulting ent-27-C-Bz and ent-27-5FU-Bz nucleoside analogues. The compounds were characterized by IR, 1H-NMR and 13C-NMR spectra.
Preliminary preclinical in vitro data show that the ent-C-Bz exerts a biphasic cytotoxic effect on Jurkat tumor cells at low and high concentrations, restricts viable cell multiplication and targets DNA synthesis. Meanwhile, ent-5-FU-Bz and 5-FU are cytotoxic at lower concentrations and hinder RNA synthesis in living tumor cells. We emphasize that ent-5-FU-Bz restricts Jurkat cells progenitors at earlier generations than the 5-FU standard, proving a potential cytostatic action. Our preliminary study reveals that the investigated nucleoside analogues are potential candidates for anti-tumor therapy of T lymphoblasts.

Cuvinte cheie: pyrimidine nucleoside analogs, Mitsunobu synthesis, antitumoral activity, NMR spectra, Jurkat lymhoblast