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2,4,6-三取代吡啶衍生物的合成、拓扑异构酶I抑制作用及构效关系研究

Synthesis, topoisomerase I inhibition and structure-activity relationship study of 2,4,6-trisubstituted pyridine derivatives.

作者信息

Zhao Long-Xuan, Moon Yoon-Soo, Basnet Arjun, Kim Eun-kyung, Jahng Yurngdong, Park Jae Gyu, Jeong Tae Cheon, Cho Won-Jea, Choi Sang-Un, Lee Chong Ock, Lee Sun-Young, Lee Chong-Soon, Lee Eung-Seok

机构信息

Department of Chemistry, Liaoning Normal University, Dalian, Liaoning 116-029, PR China.

出版信息

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1333-7. doi: 10.1016/j.bmcl.2003.11.084.

DOI:10.1016/j.bmcl.2003.11.084
PMID:14980693
Abstract

For the development of new anticancer agents, phenyl, 2-pyridyl, 2-furyl, 2-thienyl, 2-furylvinyl and 2-thienylvinyl substituted derivatives on 2,4,6-position in pyridine moiety were prepared and evaluated for their topoisomerase I inhibitory activity. Among the thirteen prepared compounds, four compounds exhibited strong topoisomerase I inhibitory activity. A structure-activity relationship study indicated that the 2-thienyl-4-furylpyridine skeleton was important for topoisomerase I inhibitory activity.

摘要

为了开发新型抗癌药物，制备了吡啶部分2,4,6位上苯基、2-吡啶基、2-呋喃基、2-噻吩基、2-呋喃基乙烯基和2-噻吩基乙烯基取代的衍生物，并对其拓扑异构酶I抑制活性进行了评估。在所制备的13种化合物中，有4种化合物表现出较强的拓扑异构酶I抑制活性。构效关系研究表明，2-噻吩基-4-呋喃基吡啶骨架对拓扑异构酶I抑制活性很重要。

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