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合成 2,4-二芳基色烯并吡啶并评价其拓扑异构酶 I 和 II 抑制活性、细胞毒性及构效关系。

Synthesis of 2,4-diaryl chromenopyridines 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.

出版信息

Eur J Med Chem. 2011 Aug;46(8):3201-9. doi: 10.1016/j.ejmech.2011.04.029. Epub 2011 Apr 29.

DOI:10.1016/j.ejmech.2011.04.029
PMID:21601964
Abstract

Designed and synthesized were a series of 5H-chromeno[4,3-b]pyridines with substitution at 2- and 4-positions with various 5- or 6-membered heteroaromatics as antitumor agents. They were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Structure-activity relationship study showed that 2-furyl or 2-thienyl at 2- or 4-position of central pyridine is crucial in displaying topo I or II inhibitory activity and cytotoxicity.

摘要

设计并合成了一系列 5H-色烯并[4,3-b]吡啶，其中 2-和 4-位取代有各种 5-或 6-元杂环芳烃，作为抗肿瘤药物。它们被评估了拓扑异构酶 I 和 II 的抑制活性以及对几种人癌细胞系的细胞毒性。构效关系研究表明，在中心吡啶的 2-或 4-位上的 2-呋喃基或 2-噻吩基对于显示拓扑异构酶 I 或 II 的抑制活性和细胞毒性是至关重要的。

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