Special Issue "Nucleotide Analogues: Modifications, Biological Activities and Applications"
Deadline for manuscript submissions: 31 August 2019
Prof. Roberto Romeo
Università degli Studi di Messina, Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, Messina, Italy
Interests: organic synthesis; radical processes; pericyclic reactions; drug discovery; modified nucleosides; nanomaterials
Nucleosides play a very important role in many biological processes; accordingly, modifications of the nucleoside structure are widely exploited for the design and development of new drugs, especially in the fields of virology and cancer research. In this search, structural modifications on the sugar moiety of natural nucleosides and/or modifications of the heterocyclic base can be performed.
The first option involved changes in the (2-deoxy)-D-ribofuranose moiety as the inversion of hydroxyl group configuration, the elimination towards dideoxy- or dideoxy-dydehydro-nucleosides, the substitution/functionalization by various groups, or cleavage of the sugar ring leading to acyclic nucleosides. Other deeper structural modifications include the replacement of the oxygen atom by a methylene group, sulfur or nitrogen atom or the additional insertion of a second heteroatom in the sugar moiety. Nucleoside analogues endowed with the unnatural L-configuration have also been shown to possess interesting antiviral properties.
The second alternative takes into account structural modifications concerning the purine or pyrimidine nucleobases. Many nucleosides of natural origin, containing modified heterocyclic bases with respect to “normal” nucleobases, have been found to be bioactive. Furthermore, many unnatural bases have been synthesized and many of them are good substrates for DNA and RNA polymerases. In this context, great interest has been addressed towards C-nucleosides, for their higher stability toward the cleavage of the nucleoside bond due to the replacement of C-N by the non hydrolyzable C-C bond.
The research of new synthetic procedures towards nucleoside analogs is a field continuously explored as a consequence of the urgent demand for new therapeutic agents in which an improved biological activity is assisted by a low toxicity towards the host cell. This Special Issue covers all aspects related to the synthesis and molecular actions in organisms of new derivatives. Specific interests include the design of nanostructured materials for a controlled release of bioactive nucleotides. The efforts in this field, in concert with improved synthetic advances, will provide strong impetus for the next wave of design and development of nucleoside therapeutics.
Prof. Roberto Romeo
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- Base-modified nucleosides
- Sugar ring-modified nucleosides
- Acyclic nucleosides
- Delivery systems