A structure-activity relationship study of batracylin analogues.

A number of isoindolo[1,2-b]quinazolines and some benzo[4,5]isoquinolino[1,2-b]quinazolines as structural modification analogues of the antitumor compound batracylin were synthesized and evaluated against HL-60 cell growth and in topoisomerase II-mediated DNA cleavage assays. Of the compounds studied, 10,12-dihydro-7,8-methylenedioxyisoindolo[1,2-b]quinazolin-1 2(10H)-one (1d), 2-amino-10,12-dihydroisoindolo[1,2-b]quinazolin-12(10H)-one (1p), and 2-amino-7,8-methylenedioxy-10,12-dihydroisoindolo[1,2-b] quinazolin-12(10H)-one (1ab) exhibited good inhibitory activities against HL-60 cell lines as well as induction of topo II-mediated DNA cleavage activities.