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

  • Eur J Med Chem. 2012 Jun:52:123-36. doi: 10.1016/j.ejmech.2012.03.010.
Pritam Thapa  1 ,  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
Affiliations
  • 1. College of Pharmacy, Yeungnam University, 214-1 Dae-dong, Gyeongsan 712-749, Republic of Korea.
PMID: 22503656 DOI: 10.1016/j.ejmech.2012.03.010
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.