Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents

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dc.contributor.authorDraffan, AGen_AU
dc.contributor.authorFrey, Ben_AU
dc.contributor.authorFraser, BHen_AU
dc.contributor.authorPool, Ben_AU
dc.contributor.authorGannon, Cen_AU
dc.contributor.authorTyndall, EMen_AU
dc.contributor.authorCianci, Jen_AU
dc.contributor.authorHarding, Men_AU
dc.contributor.authorLilly, Men_AU
dc.contributor.authorHufton, Ren_AU
dc.contributor.authorHalim, Ren_AU
dc.contributor.authorJahangiri, Sen_AU
dc.contributor.authorBond, Sen_AU
dc.contributor.authorJeynes, TPen_AU
dc.contributor.authorNguyen, VTTen_AU
dc.contributor.authorWirth, Ven_AU
dc.contributor.authorLuttick, Aen_AU
dc.contributor.authorTilmanis, Den_AU
dc.contributor.authorPryor, Men_AU
dc.contributor.authorPorter, Ken_AU
dc.contributor.authorMorton, CJen_AU
dc.contributor.authorLin, Ben_AU
dc.contributor.authorDuan, Jen_AU
dc.contributor.authorBethell, RCen_AU
dc.contributor.authorKukojl, Gen_AU
dc.contributor.authorSimoneau, Ben_AU
dc.contributor.authorTucker, SPen_AU
dc.date.accessioned2020-03-30T01:31:15Zen_AU
dc.date.available2020-03-30T01:31:15Zen_AU
dc.date.issued2014-11-01en_AU
dc.date.statistics2020-03-20en_AU
dc.description.abstractPrevious investigations identified 2′-C-Me-branched ribo-C-nucleoside adenosine analogues, 1, which contains a pyrrolo[2,1-f][1,2,4]triazin-4-amine heterocyclic base, and 2, which contains an imidazo[2,1-f][1,2,4]triazin-4-amine heterocyclic base as two compounds with promising anti-HCV in vitro activity. This Letter describes the synthesis and evaluation of a series of novel analogues of these compounds substituted at the 2-, 7-, and 8-positions of the heterocyclic bases. A number of active new HCV inhibitors were identified but most compounds also demonstrated unacceptable cytotoxicity. However, the 7-fluoro analogue of 1 displayed good potency with a promising cytotherapeutic margin. © 2014 Elsevier Ltd.en_AU
dc.identifier.citationDraffan, A. G., Frey, B., Fraser, B. H., Pool, B., Gannon, C., Tyndall, E. M., Cianci, J., Harding, M., Lilly, M., Hufton, R., Halim, R., Jahangiri, S., Bond., Jeynes, T. P., Nguyen V. T. T., Wirth, V., Luttick, A., Tilmanis, D., Pryor, M., Porter, K., Morton, C. J., Lin, B., Duan, J., Bethell, R. C., Kukolj, G., Sinoneau, B., & Tucker, S. P. (2014). Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents. Bioorganic & Medicinal Chemistry Letters, 24(21), 4984-4988. doi:10.1016/j.bmcl.2014.09.030en_AU
dc.identifier.govdoc8743en_AU
dc.identifier.issn0960-894Xen_AU
dc.identifier.issue21en_AU
dc.identifier.journaltitleBioorganic & Medicinal Chemistry Lettersen_AU
dc.identifier.pagination4984-4988en_AU
dc.identifier.urihttps://doi.org/10.1016/j.bmcl.2014.09.030en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9310en_AU
dc.identifier.volume24en_AU
dc.language.isoenen_AU
dc.publisherElsevier B.V.en_AU
dc.subjectViral diseasesen_AU
dc.subjectHepatitisen_AU
dc.subjectInfectious hepatitisen_AU
dc.subjectRNAen_AU
dc.subjectTherapyen_AU
dc.subjectVirusesen_AU
dc.titleDerivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agentsen_AU
dc.typeJournal Articleen_AU
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