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Herrmann, A. ; Roesner, M.* ; Werner, T.* ; Hauck, S.M. ; Koch, A. ; Bauer A. ; Schneider, M. ; Brack-Werner, R.

Potent inhibition of HIV replication in primary human cells by novel synthetic polyketides inspired by Aureothin.

Sci. Rep. 10:1326 (2020)

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Overcoming the global health threat of HIV infection requires continuous pipelines of novel drug candidates. We identified the gamma-pyrone polyketides Aureothin/Neoaureothin as potent hits by anti-HIV screening of an extensive natural compound collection. Total synthesis of a structurally diverse group of Aureothin-derivatives successfully identified a lead compound (#7) superior to Aureothin that combines strong anti-HIV activity (IC90<45 nM), photostability and improved cell safety. Compound #7 inhibited de novo virus production from integrated proviruses by blocking the accumulation of HIV RNAs that encode the structural components of virions and include viral genomic RNAs. Thus, the mode-of-action displayed by compound #7 is different from those of all current clinical drugs. Proteomic analysis indicated that compound #7 does not affect global protein expression in primary blood cells and may modulate cellular pathways linked to HIV infection. Compound #7 inhibited multiple HIV genotypes, including HIV-type 1 and 2 and synergistically inhibited HIV in combination with clinical reverse transcriptase and integrase inhibitors. We conclude that compound #7 represents a promising new class of HIV inhibitors that will facilitate the identification of new virus-host interactions exploitable for antiviral attack and holds promise for further drug development.

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