Design, Docking, and Synthesis of Novel Indeno[1,2-c]isoquinolines for the Development of Antitumor Agents as Topoisomerase I Inhibitors. -An intramolecular radical cyclization is the key step in the reaction sequence to the novel indeno[1,2-c]isoquinolin-5-ones (II). The structurally related isoquinoline (VII) and (II) are tested in vitro for cytotoxicity and DNA-topoisomerase 1 (top 1) inhibitory activity. The dramatic enhancement of top 1 inhibitory activity of (VII) is explained by a docking study using the FlexX program. -(CHO*, W.-J.; LE, Q. M.; VAN, H. T. M.; LEE, K. Y.; KANG, B. Y.; LEE, E.-S.; LEE, S. K.; KWON, Y.; Bioorg. Med. Chem. Lett. 17 (2007) 13, 3531-3534; Coll. Pharm., Chonnam Natl. Univ., Gwangju 500-757, S. Korea; Eng.) -H. Haber 43-145
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