2. Academic Validation
  3. 2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study

2-Thienyl-4-furyl-6-aryl pyridine derivatives: synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship study

  • Bioorg Med Chem. 2010 Jan 1;18(1):377-86. doi: 10.1016/j.bmc.2009.10.049.
Pritam Thapa 1,  Radha Karki,  Uttam Thapa,  Yurngdong Jahng,  Mi-Ja Jung,  Jung Min Nam,  Younghwa Na,  Youngjoo Kwon,  Eung-Seok Lee
Affiliations

Affiliation

  • 1 College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
PMID: 19939682 DOI: 10.1016/j.bmc.2009.10.049
Abstract

Designed and synthesized 60 2-thienyl-4-furyl-6-aryl pyridine derivatives were evaluated for their Topoisomerase I and II inhibitory activities at 20 microM and 100 microM and cytotoxicity against several human Cancer cell lines. Compounds 8, 9, 11-29 showed significant Topoisomerase II inhibitory activity and compounds 10 and 11 showed significant Topoisomerase I inhibitory activity. Most of the compounds (7-21) possessing 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety showed higher or similar cytotoxicity against HCT15 cell line as compared to standards. Most of the selected compounds displayed moderate cytotoxicity against MCF-7, HeLa, DU145, and K562 cell lines. Structure-activity relationship study revealed that 2-(5-chlorothiophen-2-yl)-4-(furan-3-yl) moiety has an important role in displaying biological activities.

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