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

Bioorganic & medicinal chemistry letters (2009-12-04)
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
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.

MATERIALS
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Product Description

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