• Title/Summary/Keyword: topoisomerase

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Synthesis of New 3-Arylisoquinolinamines: Effect on Topoisomerase I Inhibition and Cytotoxicity

  • Cho, Won-Jae;Min, Sun-Young;Le, Thanh-Nguyen;Kim, Tae-Sung
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.180.1-180.1
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    • 2003
  • Eukaryotic DNA topoisomerase I (top I) is an essential enzyme that act to relax supercoiled DNA during the transcription, replication and mitosis. Intracellular levels of top I are elevated in a number of human solid tumors, relative to the respective normal tissues, suggesting that controlling the topI level is important to treat cancer. Top I poisons show their antitumor activities by stabilizing the cleavable ternary complex consisting of top I enzyme, DNA, and drug. Thus, top I is a promising target for the development of new cancer chemotherapeutics against a number of solid tumors. (omitted)

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Design. Synthesis and Antitumor Evaluation of Terpyridine Derivatives Containing Pyridines at 4'- Position

  • Lim, Hyun-Tae;Moon, Yoon-Soo;Zhao, Longxuan;Kim, Eun-Kyung;Kim, Tae-Hyung;Lee, Eung-Seok
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.347.3-347.3
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    • 2002
  • Recent study indicated that terpyridine and its derivatives displayed highly active antitumor properties. In this presentation. derivatives of terpyridines having three pyridine moieties at 2',4',6'-position of central pyridine skeleton were prepared, and evaluated their cytotoxicity against several human cancer cell lines and topoisomerase I inhibitory activities. Most of the prepared compounds showed strong cytotoxicity compared to doxorubicln. In addition. several compounds displayed better cytotoxicity than that of doxorubicin. In addition, several compounds displayed better cytotoxicity than that of doxorubicin. Structure-activity relationship study was perfomed to be indicated that [2.2':6',2']terpyidine skeleton is important to show strong xytotoxicity. Significant topoxicity. Significant topoisomerase I inhibitory activity was not observed for prepared compounds.

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