title: Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex.
abstract: 11-hydroxyindeno[1,2-c]isoquinolines 12a-c were prepared as constrained forms of 3-arylisoquinolines through an intramolecular cyclization reaction. Among the synthesized compounds, the 11-(i)butoxy analog 15l displayed potent in vitro cytotoxicity against four different tumor cell lines as well as topoisomerase 1 inhibitory activity. A FlexX docking study was performed to explain the topoisomerase 1 activity of 15l.
authors.affiliation: College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 500-757, Republic of Korea.
authors.forename: Hue Thi My
authors.initials: HT
authors.lastname: Van
authors.forename: Quynh Manh
authors.initials: QM
authors.lastname: Le
authors.forename: Kwang Youl
authors.initials: KY
authors.lastname: Lee
authors.forename: Eung-Seok
authors.initials: ES
authors.lastname: Lee
authors.forename: Youngjoo
authors.initials: Y
authors.lastname: Kwon
authors.forename: Tae Sung
authors.initials: TS
authors.lastname: Kim
authors.forename: Thanh Nguyen
authors.initials: TN
authors.lastname: Le
authors.forename: Suh-Hee
authors.initials: SH
authors.lastname: Lee
authors.forename: Won-Jea
authors.initials: WJ
authors.lastname: Cho
mesh_terms: D045744:Cell Line, Tumor; D004264:DNA Topoisomerases, Type I / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D006860:Hydrogen Bonding; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D059004:Topoisomerase I Inhibitors