Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides: design, synthesis, and biological activity
Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides: design, synthesis, and biological activity
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DOI：
10.1016/j.tet.2011.01.063
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发表时间：
2011-03-25
期刊：
影响因子：
2.1
通讯作者：
Qian, Xuhong
中科院分区：
文献类型：
--
作者：
Li, Xiaolian;Lin, Yanjie;Qian, Xuhong
采用“点击反应”法，简便地合成了两个新的3-1,2,3-三唑-1,8-萘酰亚胺5 - a-e、7 - a-e系列化合物。评价了它们的生物活性。化合物5a-e对MCF-7细胞的毒性更强，而7a-e对7721细胞的毒性更强，其中7a对MCF-7和7721细胞系的IC50值分别为0.348 mu M和0.258 mu M。由于与1,2,3-三唑相连的苯基，化合物5a不仅表现出更高的DNA亲和力，而且比化合物7a具有更有效的DNA损伤能力。(C) 2011 Elsevier Ltd.版权所有。
Two novel series of 3-1,2,3-triazol-1,8-naphthalimides 5a-e, 7a-e were synthesized easily by employing 'click reaction'. Their bioactivities were evaluated. Compounds 5a-e were found to be more toxic against MCF-7 cells while 7a-e were more potent against 7721 cells, in particular 7a, the IC50 value of which against cell lines of MCF-7 and 7721 was 0.348 mu M and 0.258 mu M, respectively. Due to the phenyl group linked to 1,2,3-triazole, compound 5a not only showed higher DNA affinity but also more efficient DNA damaging ability than compound 7a. (C) 2011 Elsevier Ltd. All rights reserved.