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|Title:||Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents|
|Citation:||Draffan, 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.2014.09.030|
|Abstract:||Previous 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.|
|Gov't Doc #:||8743|
|Appears in Collections:||Journal Articles|
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