Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study of hydroxylated 2,4-diphenyl-6-aryl pyridines

  • Bioorg Med Chem. 2010 May 1;18(9):3066-77. doi: 10.1016/j.bmc.2010.03.051.
Radha Karki  1 ,  Pritam Thapa ,  Mi Jeong Kang ,  Tae Cheon Jeong ,  Jung Min Nam ,  Hye-Lin Kim ,  Younghwa Na ,  Won-Jea Cho ,  Youngjoo Kwon ,  Eung-Seok Lee
Affiliations
  • 1. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
PMID: 20392646 DOI: 10.1016/j.bmc.2010.03.051
Abstract

A new series of 2,4-diphenyl-6-aryl pyridines containing hydroxyl group(s) at the ortho, meta, or para position of the phenyl ring were synthesized, and evaluated for Topoisomerase I and II inhibitory activity and cytotoxicity against several human Cancer cell lines for the development of novel Anticancer agents. Structure-activity relationship study revealed that the substitution of hydroxyl group(s) increased Topoisomerase I and II inhibitory activity in the order of meta > para > ortho position. Substitution of hydroxyl group on the para position showed better cytotoxicity.