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 |
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| Authors: | Pritam Thapa Radha Karki Hoyoung Choi Jae Hun Choi Minho Yun Byeong-Seon Jeong Mi-Ja Jung Jung Min Nam Younghwa Na Won-Jea Cho Youngjoo Kwon Eung-Seok Lee |
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| Institution: | 1. College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea;2. College of Pharmacy, Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea;3. College of Pharmacy, Catholic University of Daegu, Kyongsan 712-702, Republic of Korea;4. College of Pharmacy, Chonnam National University, Kwangju 500-757, Republic of Korea |
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| 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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