合成 2-(噻吩-2-基或-3-基)-4-呋喃基-6-芳基吡啶衍生物，并评价其拓扑异构酶 I 和 II 抑制活性、细胞毒性以及构效关系。

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.

机构信息

College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.

College of Pharmacy, Pharmacy & Division of Life & Pharmaceutical Sciences, Ewha Womans University, Seoul 120-750, Republic of Korea.

出版信息

Bioorg Med Chem. 2010 Mar 15;18(6):2245-2254. doi: 10.1016/j.bmc.2010.01.065. Epub 2010 Feb 4.

DOI:10.1016/j.bmc.2010.01.065

PMID: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.

摘要

设计、合成了一系列 2-(噻吩-2-基或-3-基)-4-呋喃基-6-芳基吡啶衍生物，并对它们的拓扑异构酶 I 和 II 抑制活性以及对几种人癌细胞系的细胞毒性进行了评价。化合物 10-19 表现出中等的拓扑异构酶 I 和 II 抑制活性，而化合物 20-29 表现出显著的拓扑异构酶 II 抑制活性。构效关系研究表明，4-(5-氯呋喃-2-基)-2-(噻吩-3-基)部分在显示拓扑异构酶 II 抑制方面具有重要作用。

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合成 2-(噻吩-2-基或-3-基)-4-呋喃基-6-芳基吡啶衍生物，并评价其拓扑异构酶 I 和 II 抑制活性、细胞毒性以及构效关系。

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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