2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study

  • Bioorg Med Chem Lett. 2010 Jan 1;20(1):42-7. doi: 10.1016/j.bmcl.2009.11.041.
Arjun Basnet  1 ,  Pritam Thapa ,  Radha Karki ,  Hoyoung Choi ,  Jae Hun Choi ,  Minho Yun ,  Byeong-Seon Jeong ,  Yurngdong Jahng ,  Younghwa Na ,  Won-Jea Cho ,  Youngjoo Kwon ,  Chong-Soon Lee ,  Eung-Seok Lee
Affiliations
  • 1. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
PMID: 19954977 DOI: 10.1016/j.bmcl.2009.11.041
Abstract

For the development of novel antitumor agents, 2,6-dithienyl-4-furyl pyridine derivatives were prepared and evaluated for their Topoisomerase I and II inhibitory activity as well as cytotoxicity against several human Cancer cell lines. Among the 21 prepared compounds, compound 24 exhibited strong Topoisomerase I inhibitory activity. In addition, a docking study with Topoisomerase I and compound 24 was performed.