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IR@PKUHSC  > 北京大学药学院  > 化学生物学系  > 期刊论文
学科主题: 药学
题名:
Unprecedented synthesis, in vitro and in vivo anti-cancer evaluation of novel triazolonaphthalimide derivatives
作者: 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
发表日期: 2012
DOI: 10.1016/j.ejmech.2011.11.025
卷: 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
项目资助者: PKUCare Pharmaceutical RD Center
WOS记录号: WOS:000301169800058
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54021
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
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.
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