Bioorganic & medicinal chemistry letters

Structural modification of 3-arylisoquinolines to isoindolo [2, 1-b] isoquinolinones for the development of novel topoisomerase 1 inhibitors with molecular docking …

HTM Van, WJ Cho

Index: Van, Hue Thi My; Cho, Won-Jea Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 9 p. 2551 - 2554

Full Text: HTML

Citation Number: 41

Abstract

Isoindolo [2, 1-b] isoquinolinones 9a–i were designed and synthesized as constrained forms of 3-arylisoquinolines through an intramolecular cyclization reaction. Among the synthesized compounds, 9d exhibited potent topoisomerase 1 inhibitory activity with cytotoxicities against three different tumor cell lines. A Surflex-dock docking study was performed to clarify the topoisomerase 1 inhibitory activity of 9d.