A STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF BATRACYLIN ANALOGS

A number of isoindolo[1,2-b]quinazolines and some benzo[4,5]isoquinoli no[1,2-b]quinazolines as structural modification analogues of the anti tumor compound batracylin were synthesized and evaluated against HL-60 cell growth and in topoisomerase 11-mediated DNA cleavage assays. Of the compounds studied, 10,12A thylenedioxyisoindolo[1,2-b]quinazolin-1 2(10H)-one (1d), 0,12-dihydroisoindolo[1,2-b]quinazolin-12(10H)-one (1 p), and 0,12-dihydroisoindolo[1,2-b]quinazolin-12[10H]-one (lab) exhib ited good inhibitory activities against HL-60 cell lines as well as in duction of topo II-mediated DNA cleavage activities.