Preparation and bioactivity of cationic porphyrins bearing mixed 3-quinolyl and 3-pyridyl meso groups

Tao Lu, Dongfang Shi, Daekyu Sun, Haiyong Han, Laurence Hurley

Research output: Contribution to journalArticle

2 Citations (Scopus)

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. METHOD: Porphyrins bearing mixed 3-quinolyl/3-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole, followed by methylation and ion-exchange. The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity. RESULT: 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.

Original languageEnglish (US)
Pages (from-to)109-115
Number of pages7
JournalJournal of China Pharmaceutical University
Volume34
Issue number2
StatePublished - Apr 2003

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Telomerase
Porphyrins
G-Quadruplexes
Pyrroles
Ion Exchange
Aldehydes
Methylation

Keywords

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

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Pharmacology

Cite this

Preparation and bioactivity of cationic porphyrins bearing mixed 3-quinolyl and 3-pyridyl meso groups. / Lu, Tao; Shi, Dongfang; Sun, Daekyu; Han, Haiyong; Hurley, Laurence.

In: Journal of China Pharmaceutical University, Vol. 34, No. 2, 04.2003, p. 109-115.

Research output: Contribution to journalArticle

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AU - Shi, Dongfang

AU - Sun, Daekyu

AU - Han, Haiyong

AU - Hurley, Laurence

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AB - 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. METHOD: Porphyrins bearing mixed 3-quinolyl/3-pyridyl meso groups were synthesized using the Adler-Longo method by condensation of aldehydes with pyrrole, followed by methylation and ion-exchange. The compounds were tested for the telomerase inhibitory activity and c-Myc inhibitory activity. RESULT: 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.

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