In order to study the structure-activity relationship of ethylenedioxy
-2-vinylphenyl)isoquinoline-1(2H)-one (2), which has exhibited signifi
cant antitumor activity, chemical modifications of 2 were performed to
yield the corresponding products (3-7). Further systematic uses of an
efficient procedure for the synthesis of 3-arylisoquinoline derivativ
es produced the substituted compounds (9a-9g), which were tested for i
n vitro antitumor activity against five different human cancer cell li
nes.