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Unprecedented synthesis, in vitro and in vivo anti-cancer evaluation of novel triazolonaphthalimide derivatives
Li, Shasha; Zhong, Wenhe; Li, Zhongjun; Meng, Xiangbao
关键词Naphthalimide Triazole N-oxide Dna Intercalator Anti-cancer
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2012
DOI10.1016/j.ejmech.2011.11.025
47页:546-552
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]HETEROCYCLIC FUSED NAPHTHALIMIDES ; BENZYNE CLICK CHEMISTRY ; COMBI-TARGETING CONCEPT ; AMINOALKYL SIDE-CHAINS ; DNA-BINDING PROPERTIES ; BIOLOGICAL EVALUATION ; ANTITUMOR-ACTIVITY ; BENZOTRIAZOLE DERIVATIVES ; SOLID TUMOR ; N-OXIDE
英文摘要

An efficient synthesis method for fusing triazole ring onto the naphthalimide core was described. The anti-cancer activities of the generated triazolonaphthalimide derivatives were evaluated with five cancer cell lines. The compounds generally displayed higher potency than amonafide. 4d,4e carrying two amino side chains showed the strongest cytotoxicities. N-oxide 5, a prodrug of 4a, was designed and synthesized. The agent was expected to be activated under the hypoxic condition in tumor tissue. Compared with 4a, 5 manifested much lower cytotoxicity both in cancer cell lines and human normal cells in the in vitro assays. However, N-oxide 5 performed potent anti-cancer activity in vivo using S-180 sarcoma bearing mice. All the results suggested that 5 was a promising anti-cancer agent. (C) 2011 Elsevier Masson SAS. All rights reserved.

语种英语
WOS记录号WOS:000301169800058
资助机构PKUCare Pharmaceutical RD Center
引用统计
被引频次:8[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/54021
专题北京大学药学院_化学生物学系
作者单位Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Li, Shasha,Zhong, Wenhe,Li, Zhongjun,et al. Unprecedented synthesis, in vitro and in vivo anti-cancer evaluation of novel triazolonaphthalimide derivatives[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,47:546-552.
APA Li, Shasha,Zhong, Wenhe,Li, Zhongjun,&Meng, Xiangbao.(2012).Unprecedented synthesis, in vitro and in vivo anti-cancer evaluation of novel triazolonaphthalimide derivatives.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,47,546-552.
MLA Li, Shasha,et al."Unprecedented synthesis, in vitro and in vivo anti-cancer evaluation of novel triazolonaphthalimide derivatives".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 47(2012):546-552.
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