@article{fdi:010081107, title = {{S}ynthesis and antiviral evaluation of (1,4-disubstituted-1,2,3-triazol)-(e)-2-methyl-but-2-{E}nyl nucleoside phosphonate prodrugs}, author = {{A}buduaini, {T}. and {R}oy, {V}. and {M}arlet, {J}. and {G}audy-{G}raffin, {C}. and {B}rand, {D}. and {B}aronti, {C}{\'e}cile and {T}ouret, {F}. and {C}outard, {B}. and {M}c{B}rayer, {T}. {R}. and {S}chinazi, {R}. {F}. and {A}grofoglio, {L}. {A}.}, editor = {}, language = {{ENG}}, abstract = {{A} series of hitherto unknown (1,4-disubstituted-1,2,3-triazol)-({E})-2-methyl-but-2-enyl nucleosides phosphonate prodrugs bearing 4-substituted-1,2,3-triazoles were prepared in a straight approach through an olefin acyclic cross metathesis as the key synthetic step. {A}ll novel compounds were evaluated for their antiviral activities against {HBV}, {HIV} and {SARS}-{C}o{V}-2. {A}mong these molecules, only compound 15j, a hexadecyloxypropyl ({HDP})/(isopropyloxycarbonyl-oxymethyl)-ester ({POC}) prodrug, showed activity against {HBV} in {H}uh7 cell cultures with 62% inhibition at 10 mu {M}, without significant cytotoxicity ({IC}50 = 66.4 mu {M} in {H}ep{G}2 cells, {IC}50 = 43.1 mu {M} in {H}ep{G}2 cells) at 10 mu {M}.}, keywords = {nucleosides ; olefin cross metathesis ; ultrasound ; copper-catalyzed ; azide-alkyne cycloaddition ({C}u{AAC}) ; antiviral properties ; {HBV} ; {HIV} ; {SARS}-{C}o{V}-2}, booktitle = {}, journal = {{M}olecules}, volume = {26}, numero = {5}, pages = {1493 [18 p.]}, year = {2021}, DOI = {10.3390/molecules26051493}, URL = {https://www.documentation.ird.fr/hor/fdi:010081107}, }