Design, synthesis and biological activity of cationic porphyrins bearing mixed 3-quinolyl and 4-pyridyl meso groups

Tao Lu, Dong Fang Shi, Dae Kyu Sun, Hai Yong Han, Laurence H. Hurley

Research output: Contribution to journalArticle

Abstract

Aim: To search for the potent telomerase inhibitors with structures of cationic porphyrins to improve the interactions between G-quadruplex and porphyrins by systematically varying the meso substituents. Methods: Porphyrins bearing mixed 3-quinolyl/4-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole, and then followed by methylation and ion exchange. The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity. Results: All compounds were found to be potent and approximately equivalent in terms of their ability to inhibit the action of telomerase in a cell-free assay. Compound 4 had the best inhibitory activity on c-Myc. Conclusion: Cationic porphyrins would be the potential anticancer candidates.

Original languageEnglish (US)
Pages (from-to)393-397
Number of pages5
JournalJournal of China Pharmaceutical University
Volume36
Issue number5
StatePublished - Oct 1 2005

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Keywords

  • G-quadruplex
  • Porphyrin
  • Synthesis
  • Telomerase
  • Telomerase inhibitors
  • c-Myc inhibitory activity

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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