Improved Antiviral Activity of a Polyamide Against High-Risk Human Papillomavirus Via N-Terminal Guanidinium Substitution

通过N端胍基取代提高聚酰胺对高危型人乳头瘤病毒的抗病毒活性

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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 IC(90) values. These substitutions change DNA-binding preferences, while binding affinity remains unchanged.

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