Design, synthesis, and evaluation of dioxane-based antiviral agents targeted against the Sindbis virus capsid protein |
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Authors: | Kim Ha Young Patkar Chinmay Warrier Ranjit Kuhn Richard Cushman Mark |
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Institution: | Department of Medicinal Chemistry and Molecular Pharmacology, The Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA. |
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Abstract: | Dioxane-based antiviral agents targeted to the hydrophobic binding pocket of Sindbis virus capsid protein were designed by computer graphics molecular modeling and synthesized. Virus production using SIN-IRES-Luc and capsid assembly were monitored to evaluate antiviral activity. A compound with a three-carbon linker chain connecting two dioxane moieties inhibited virus production by 50% at a concentration of 40 microM, while (R)-hydroxymethyldioxane inhibited virus production by 50% at a concentration of 1 microM. Both compounds were not cytotoxic in uninfected BHK cells at concentrations of 1mM. |
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