Synthesis of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives and evaluation of their topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

  • Bioorg Med Chem. 2010 Mar 15;18(6):2245-2254. doi: 10.1016/j.bmc.2010.01.065.
Pritam Thapa  1 ,  Radha Karki  1 ,  Hoyoung Choi  1 ,  Jae Hun Choi  1 ,  Minho Yun  1 ,  Byeong-Seon Jeong  1 ,  Mi-Ja Jung  2 ,  Jung Min Nam  2 ,  Younghwa Na  3 ,  Won-Jea Cho  4 ,  Youngjoo Kwon  2 ,  Eung-Seok Lee  1
Affiliations
  • 1. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
  • 2. College of Pharmacy, Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.
  • 3. College of Pharmacy, Catholic University of Daegu, Kyongsan 712-702, Republic of Korea.
  • 4. College of Pharmacy, Chonnam National University, Kwangju 500-757, Republic of Korea.
PMID: 20188578 DOI: 10.1016/j.bmc.2010.01.065
Abstract

A series of 2-(thienyl-2-yl or -3-yl)-4-furyl-6-aryl pyridine derivatives were designed, synthesized, and evaluated for their Topoisomerase I and II inhibition and cytotoxic activity against several human Cancer cell lines. Compounds 10-19 showed moderate Topoisomerase I and II inhibitory activity and 20-29 showed significant Topoisomerase II inhibitory activity. Structure-activity relationship study revealed that 4-(5-chlorofuran-2-yl)-2-(thiophen-3-yl) moiety has an important role in displaying Topoisomerase II inhibition.