Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives

Long Xuan Zhao, Tae Sung Kim, Soo Hyun Ahn, Tae Hyung Kim, Eun kyung Kim, Won Jea Cho, Heesung Choi, Chong Soon Lee, Jung Ae Kim, Tae Cheon Jeong, Ching jer Chang, Eung Seok Lee

Research output: Contribution to journalArticle

93 Citations (Scopus)

Abstract

For the development of new anticancer agents, 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were designed and evaluated for their topoisomerase I inhibitory activity and antitumor cytotoxicity. Structure-activity relationship studies indicated that 2,2′:6′,2″-terpyridine derivatives were highly cytotoxic toward several human tumor cell lines, whereas 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives were potent topoisomerase I inhibitors.

Original languageEnglish
Pages (from-to)2659-2662
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number19
DOIs
Publication statusPublished - 2001 Oct 8
Externally publishedYes

    Fingerprint

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

Zhao, L. X., Kim, T. S., Ahn, S. H., Kim, T. H., Kim, E. K., Cho, W. J., Choi, H., Lee, C. S., Kim, J. A., Jeong, T. C., Chang, C. J., & Lee, E. S. (2001). Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2′:6′,2″-, 2,2′:6′,3″- and 2,2′:6′,4″-terpyridine derivatives. Bioorganic and Medicinal Chemistry Letters, 11(19), 2659-2662. https://doi.org/10.1016/S0960-894X(01)00531-5