title: Synthesis of benzo-annulated tryptanthrins and their biological properties.
abstract: A series of benzo-annulated derivatives of tryptanthrin were prepared and their optical and redox properties were studied. Tryptanthrin and its benzo-annulated derivatives showed selective inhibitory activity on topo I with an increase of activity on topo II by benzo-annulation on quinazolin-4(3H)-one moiety. Although the benzo-annulation on quinazolin-4(3H)-one ring did not affect significantly on the inhibitory activities against topo I and II, the benzoannulation on indolin-3-one ring affected the inhibitory activity very much especially by linear annulation. Cytotoxicities were not significantly changed upon benzoannulation, which were not directly related either to the inhibitory activities against topo I and II or to the reduction potentials.
authors: College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
authors: Jing Lu
authors: JL
authors: Liang
authors: So-Eun
authors: SE
authors: Park
authors: Youngjoo
authors: Y
authors: Kwon
authors: Yurngdong
authors: Y
authors: Jahng
mesh_terms: D000818:Animals; D002417:Cattle; D004247:DNA / Q000378:metabolism; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011799:Quinazolines; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; C046243:tryptanthrine; D004247:DNA; C427203:calf thymus DNA; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II