M. Medarde et al., SYNTHESIS, ANTITUMORAL AND ANTIVIRAL EVALUATION OF HALO-YATEIN AND DEMETHYL-YATEIN DERIVATIVES, Archiv der pharmazie, 328(9), 1995, pp. 640-644
Several chloro- and iodo-lignanolides have been obtained by direct hal
ogenation of aromatic rings from yatein and 4'-O-demethylyatein. They
were assayed as antineoplastics, in order to check the influence in th
e activity of substitution in both aromatic rings. Although these comp
ounds show a modest antineoplastic activity, it is far from that displ
ayed by yatein and podophyllotoxin. These results confirm that demethy
lation and the introduction of halo substituents diminish the activity
of lignans of the dibenzylbutyrolactone type.