2. Academic Validation
  3. 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

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

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.

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