2,6-二噻吩基-4-呋喃基吡啶：合成、拓扑异构酶 I 和 II 抑制、细胞毒性、构效关系及对接研究。
2,6-Dithienyl-4-furyl pyridines: Synthesis, topoisomerase I and II inhibition, cytotoxicity, structure-activity relationship, and docking study.
机构信息
College of Pharmacy, Yeungnam University, Kyongsan 712-749, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2010 Jan 1;20(1):42-7. doi: 10.1016/j.bmcl.2009.11.041. Epub 2009 Nov 14.
PMID:19954977
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.
摘要
为了开发新型抗肿瘤药物，我们制备了 2,6-二噻吩基-4-呋喃基吡啶衍生物，并对其拓扑异构酶 I 和 II 的抑制活性以及对几种人癌细胞系的细胞毒性进行了评价。在所制备的 21 种化合物中，化合物 24 表现出较强的拓扑异构酶 I 抑制活性。此外，还进行了与拓扑异构酶 I 和化合物 24 的对接研究。
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