Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety

Pritam Thapa, Radha Karki, Minho Yun, Tara Man Kadayat, Eunyoung Lee, Han Byeol Kwon, Younghwa Na, Won Jea Cho, Nam Doo Kim, Byeong Seon Jeong, Youngjoo Kwon, Eung Seok Lee

Research output: Contribution to journalArticlepeer-review

54 Scopus citations

Abstract

We have designed and synthesized a series of 2,4,6-triaryl pyridine derivatives containing chlorophenyl and phenolic moeity at 2- and 4- position of the central pyridine, respectively, resulting in a total of 42 compounds. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Most compounds showed better topoisomerase II inhibitory activity compared to topoisomerase I inhibitory activity. Compounds 19, 20, 26-28, and 47-50 especially showed stronger topo II inhibitory activity than etoposide.

Original languageEnglish
Pages (from-to)123-136
Number of pages14
JournalEuropean Journal of Medicinal Chemistry
Volume52
DOIs
StatePublished - Jun 2012

Keywords

  • 2,4,6-Triaryl pyridine
  • Antitumor
  • Cytotoxicity
  • Terpyridine
  • Topoisomerase I and II inhibition

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