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

A series of 3' and 4'-substituted avarone derivs. I (R = H, NHMe, NHEt; R' = serine, cysteic acid, etc.; or RR' = adenine) were synthesized and tested in culture systems as antitumor and antiviral agents in comparison to avarol and avarone (I; R = R' = H). 3'-Alkylamino derivs. showed potent cytostatic activities against murine L1210 and human B (Raji) and T (C8166, H9) lymphoblast cells (ID50 range 1.7-3.7 mM). Avarol and avarone were six times less active. While none of the derivs. showed anti-human immunodeficiency virus (HIV) activity superior to that of the parent compds., most of them, avarol and avarone included, were potent and selective inhibitors of poliovirus multiplication.