3'-alkylamino avarone derivatives demonstrate potent in vitro cytostatic activity against lymphoblast cells and inhibit poliovirus multiplication, though they do not improve upon parent compounds' anti-HIV activity.
May support preclinical antiviral development; leaves open clinical translation pending in vivo validation.
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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Giulio et al. (1991) studied this question.
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