Every year, hundreds of new nucleoside analogues are obtained in laboratories
around the world. As early as in 1964, 3’-azidothymidine (AZT) was first synthesized,
which turned out to be the main weapon in the fight against HIV viruses
20 years later. Part I of the review includes nucleosides possessing modifications
in the base moiety or having other heterocyclic bases. Nucleosides modified in the
sugar residue, because of a broad spectrum of examples, will be a subject of part II
and III of the review. In the group of analogues modified in the base moiety the following
derivatives among others are listed: 5-iodo-2’-deoxyuridine (IDU), E-5-(2-
bromovinyl)-2’-deoxyuridine (BVDU), capecitabine – prodrug form of fluorouracil,
7-deazaadenosine, BCX4430 (immucillin-A) – 9-deazaadenosine derivative active
against filoviruses such as Ebola virus (EBOV). In the group of nucleosides having
a different heterocyclic base the following derivatives are listed: ribavirin (RBV) and
its analogues – RBV triphosphate is an inhibitor of many viral enzymes involved in
the replication cycle, mizoribine (MZB) – a naturally occurring nucleosidic immunosuppressor,
5-ethynyl-1-β-"-ribofuranosyl-imidazole-4-carboxamide (EICAR)
which suppresses development of murine leukemia cell lines and has a broad spectrum
of activity against RNA and DNA viruses. The C-nucleosides group includes
e.g. oxazinomycin – a natural antibiotic with growth inhibitory properties against
gram (+), gram (–) bacteria and sarcoma, and formycin A isolated from Streptomyces
lavendulae, which has cytostatic and antiviral activity.
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