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Issue 11, 2016
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Improved antiviral activity of a polyamide against high-risk human papillomavirus via N-terminal guanidinium substitution

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Abstract

We report the synthesis of two novel pyrrole–imidazole polyamides with N-terminal guanidinium or tetramethylguanidinium groups and evaluate their antiviral activity against three cancer-causing human papillomavirus strains. Introduction of guanidinium improves antiviral activity when compared to an unsubstituted analog, especially in IC90 values. These substitutions change DNA-binding preferences, while binding affinity remains unchanged.

Graphical abstract: Improved antiviral activity of a polyamide against high-risk human papillomavirus via N-terminal guanidinium substitution

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Publication details

The article was received on 05 Jul 2016, accepted on 04 Oct 2016 and first published on 05 Oct 2016


Article type: Research Article
DOI: 10.1039/C6MD00371K
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2016,7, 2076-2082
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    Improved antiviral activity of a polyamide against high-risk human papillomavirus via N-terminal guanidinium substitution

    C. H. Castaneda, M. J. Scuderi, T. G. Edwards, G. D. Harris Jr., C. M. Dupureur, K. J. Koeller, C. Fisher and J. K. Bashkin, Med. Chem. Commun., 2016, 7, 2076
    DOI: 10.1039/C6MD00371K

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