A Structured–Activity Relationship Study of Batracylin Analogues |
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| Authors: | Luo Yilin Ren Yun-Feng Chou Ting-Chao Chen Allan Y Yu Chiang Liu Leroy F Cheng C C |
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| Institution: | (1) Drug Development Laboratory, University of Kansas Cancer Center and Department of Pharmacology, Toxicology and Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas, 66160-7419;(2) Laboratory of Biochemical Pharmacology, Memorial Sloan-Kettering Cancer Center, New York, New York, 10021;(3) Department of Biological Chemistry, The Johns Hopkins University School of Medicine, Baltimore, Maryland, 21205 |
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| Abstract: | A number of isoindolol ,2-b]quinazolines and some benzo4,5]isoquinolinol,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-methy lenedioxyisoindolo 1,2-b] quinazolin-12(10H)-one (1d), 2-amino-10,12-dihydroisoindolol ,2-b]quinazolin- 12(10H)-one (1p), and 2-amino-7,8-methylenedioxy-10,12-dihydroisoindolol ,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. |
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| Keywords: | isoindolo[l 2-b]quinazolines cytotoxicity DNA topoisomerase colon adenocarcinoma 38 structure– activity relationship |
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