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.
Drug Development Laboratory, University of Kansas Cancer Center, Kansas City.
Y
Y
Luo
Y F
YF
Ren
T C
TC
Chou
A Y
AY
Chen
C
C
Yu
L F
LF
Liu
C C
CC
Cheng
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004273:DNA, Neoplasm / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D006868:Hydrolysis; D011799:Quinazolines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D011799:Quinazolines; C057924:batracylin; D004250:DNA Topoisomerases, Type II