Title of article :
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 Original Research Article
Author/Authors :
Pritam Thapa، نويسنده , , Radha Karki، نويسنده , , Hoyoung Choi، نويسنده , , Jae Hun Choi، نويسنده , , Minho Yun، نويسنده , , Byeong-Seon Jeong، نويسنده , , Mi-Ja Jung، نويسنده , , Jung Min Nam، نويسنده , , Younghwa Na، نويسنده , , Won-Jea Cho، نويسنده , , Youngjoo Kwon، نويسنده , , Eung Seok Lee، نويسنده ,
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.
Keywords :
2-(Thienyl-2-yl)-4-furyl-6-aryl pyridine , 2-(Thienyl-3-yl)-4-furyl-6-aryl pyridine , Topoisomerase I and II inhibition , Cytotoxicity
