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Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides: design, synthesis, and biological activity

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期刊论文
First Author:
Li, Xiaolian
Correspondence Author:
Li, XL (reprint author), Dalian Univ Technol, State Key Lab Fine Chem, POB 89,158 Zhongshan Rd, Dalian 116012, Peoples R China.
Co-author:
Lin, Yanjie,Yuan, Yukun,Liu, Kai,Qian, Xuhong
Date of Publication:
2011-03-25
Journal:
TETRAHEDRON
Included Journals:
Scopus、SCIE
Document Type:
J
Volume:
67
Issue:
12
Page Number:
2299-2304
ISSN No.:
0040-4020
Key Words:
Triazole; Intercalation; Anticancer; Naphthalimides
Abstract:
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.

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