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  • Title: 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.
    Author: Thapa P, Karki R, Choi H, Choi JH, Yun M, Jeong BS, Jung MJ, Nam JM, Na Y, Cho WJ, Kwon Y, Lee ES.
    Journal: Bioorg Med Chem; 2010 Mar 15; 18(6):2245-2254. PubMed ID: 20188578.
    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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