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Substituted dibenzoc,hcinnolines: topoisomerase I-targeting anticancer agents

Yu, Younong ; Singh, Sudhir K ; Liu, Angela ; Li, Tsai-Kun ; Liu, Leroy F ; Lavoie, Edmond J

Bioorganic & medicinal chemistry, 03 April 2003, Vol.11(7), pp.1475-91 [Peer Reviewed Journal]

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  • Title:
    Substituted dibenzoc,hcinnolines: topoisomerase I-targeting anticancer agents
  • Author: Yu, Younong ; Singh, Sudhir K ; Liu, Angela ; Li, Tsai-Kun ; Liu, Leroy F ; Lavoie, Edmond J
  • Description: Several substituted dibenzo[c,h]cinnolines were synthesized and evaluated for their potential to target topoisomerase I and for their relative cytotoxic activity. Select benzo[i]phenanthridines are capable of stabilizing the cleavable complex formed with topoisomerase I and DNA. This study was initiated to examine whether dibenzo[c,h]cinnolines, which are in essence aza analogues of benzo[i]phenanthridines, possess similar pharmacological properties. 2,3-Dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine is one of the more potent benzo[i]phenanthridine derivatives in regard to topoisomerase I-targeting activity and cytotoxicity. The structure-activity relationship observed with these substituted dibenzo[c,h]cinnolines parallels that observed for benzo[i]phenanthridine derivatives. Compared to similarly substituted benzo[i]phenanthridines, the dibenzo[c,h]cinnoline analogues exhibit more potent topoisomerase I-targeting activity and cytotoxicity. The relative IC(50) values obtained in assessing...
  • Is Part Of: Bioorganic & medicinal chemistry, 03 April 2003, Vol.11(7), pp.1475-91
  • Identifier: ISSN: 0968-0896 ; PMID: 12628673 Version:1
  • Subjects: Topoisomerase I Inhibitors ; Antineoplastic Agents -- Chemical Synthesis ; Enzyme Inhibitors -- Chemical Synthesis ; Phenanthrenes -- Chemical Synthesis
  • Language: English

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