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.
Synthesis and evaluation of cytostatic and antiviral activities of 3' and 4' avarone derivatives
A De Giulio;G Strazzullo;
1991
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
