Synthesis of 2,4-diaryl chromenopyridines and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

  • Eur J Med Chem. 2011 Aug;46(8):3201-9. doi: 10.1016/j.ejmech.2011.04.029.
Uttam Thapa  1 ,  Pritam Thapa ,  Radha Karki ,  Minho Yun ,  Jae Hun Choi ,  Yurngdong Jahng ,  Eunyoung Lee ,  Kyung-Hwa Jeon ,  Younghwa Na ,  Eun-Mi Ha ,  Won-Jea Cho ,  Youngjoo Kwon ,  Eung-Seok Lee
Affiliations
  • 1. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
PMID: 21601964 DOI: 10.1016/j.ejmech.2011.04.029
Abstract

Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for Topoisomerase I and II inhibitory activities as well as cytotoxicities against several human Cancer cell lines. Structure-activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying Topo I or II inhibitory activity and cytotoxicity.