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

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.

• Authors: Arjun Basnet, 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
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 1 Pg. 42-7 (Jan 01 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 19954977 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright 2009 Elsevier Ltd. All rights reserved.

Chemical References

• Antineoplastic Agents
• Pyridines
• Thiophenes
• Topoisomerase I Inhibitors
• Topoisomerase II Inhibitors
• DNA Topoisomerases, Type I
• DNA Topoisomerases, Type II

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, toxicity)
• Binding Sites
• Cell Line, Tumor
• Computer Simulation
• DNA Topoisomerases, Type I (metabolism)
• DNA Topoisomerases, Type II (metabolism)
• Drug Screening Assays, Antitumor
• Humans
• Pyridines (chemical synthesis, chemistry, toxicity)
• Structure-Activity Relationship
• Thiophenes (chemical synthesis, chemistry, toxicity)
• Topoisomerase I Inhibitors
• Topoisomerase II Inhibitors