2. Academic Validation
  3. 2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

2,4,6-Trisubstituted pyridines: Synthesis, topoisomerase I and II inhibitory activity, cytotoxicity, and structure-activity relationship

  • Bioorg Med Chem. 2007 Jul 1;15(13):4351-9. doi: 10.1016/j.bmc.2007.04.047.
Arjun Basnet 1,  Pritam Thapa,  Radha Karki,  Younghwa Na,  Yurngdong Jahng,  Byeong-Seon Jeong,  Tae Cheon Jeong,  Chong-Soon Lee,  Eung-Seok Lee
Affiliations

Affiliation

  • 1 College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
PMID: 17493824 DOI: 10.1016/j.bmc.2007.04.047
Abstract

Designed and synthesized were a series of pyridines substituted at 2, 4, and 6 positions with various 5- or 6-memberd heteroaromatics as antitumor agents. They were evaluated their Topoisomerase I and II inhibitory activities along with cytotoxicities against several human Cancer cell lines. Among the prepared compounds, 10-20 showed significant Topoisomerase I or II inhibitory activities, and 21-26 showed considerable cytotoxicities against several human Cancer cell lines. Structure-activity relationship study indicates that 4'-pyridine at 6-position of central pyridine plays a key role in biological activity.

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