PMC:7376974 / 39722-41516 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PMC/sourceid/7376974","sourcedb":"PMC","sourceid":"7376974","source_url":"https://www.ncbi.nlm.nih.gov/pmc/7376974","text":"Based on these studies, another class of multivalent fullerene dendrimers was then designed. A fast and controlled synthetic route was developed to achieve giant globular multivalent fullerenes, containing hundreds of functional groups. The first study was performed with tridecafullerenes containing 120 mannoses.69 The molecular structure is composed of 12 hexakis C60 surrounding a C60 core (Figure 6, route B). Compared to the previous study, an IC50 3 orders of magnitude lower was measured on the inhibition of Ebola virus (Table 3).66,68 In order to present more carbohydrates at the periphery of the dendrimer, a trialkynyl pentaerythritol derivative allowed to afford a tridecafullerene with 360 carbohydrates. In this case, the molecule was synthesized with a C60 tridecafullerene bearing α(1,2)mannobioside.70 The use of this disaccharide was already investigated, showing an increase of affinity with DC-sign receptors by a factor of 3–4.71 The synthetic strategy exploited also the use of strain-promoted copper-free cycloaddition of azides to alkynes (SPAAC) for the coupling of the core fullerene to the surrounding fullerenes. SPAAC allows an easier purification avoiding the removal of cytotoxic copper ions. The inhibition performance of this molecule was studied in vitro with viral pseudoparticles of Dengue and Zika. The comparison was made between 360 and 120 disaccharides tridecafullerenes and 36 disaccharide monofullerene. The results highlighted a picomolar IC50 inhibition on both Zika and Dengue models for the 360 disaccharide glycofullerene (Table 3). The ability to inhibit other types of viruses allows the use of glycofullerenes as broad spectrum antiviral drugs. 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