Synthesis and evaluation of cytostatic and antiviral activities of 3' and 4'-avarone derivatives

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Abstract

A series of 3' and 4'-substituted avarone derivatives were synthesized and tested in culture systems as antitumour and antiviral agents in comparison to avarol and avarone. 3'-Alkylamino derivatives showed potent cytostatic activities against murine L1210 and human B (Raji) and T (C8166, H9) lymphoblast cells (ID50 range 1.7-3.7 μM). Avarol and avarone were six times less active. While none of the derivatives showed anti-human immunodeficiency virus (HIV) activity superior to that of the parent compounds, most of them, avarol and avarone included, were potent and selective inhibitors of poliovirus multiplication.

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De Giulio, A., De Rosa, S., Strazzullo, G., Diliberto, L., Obino, P., Marongiu, M. E., … La Colla, P. (1991). Synthesis and evaluation of cytostatic and antiviral activities of 3’ and 4’-avarone derivatives. Antiviral Chemistry and Chemotherapy, 2(4), 223–227. https://doi.org/10.1177/095632029100200403

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