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学科主题: 药学
题名:
Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards
作者: Lou, Qinghua; Ji, Liyan; Zhong, Wenhe; Li, Shasha; Yu, Siwang; Li, Zhongjun; Meng, Xiangbao
关键词: cytotoxicity ; DNA alkylating agent ; DNA intercalator ; synthesis ; N-mustard ; naphthalimide
刊名: MOLECULES
发表日期: 2014-07-01
DOI: 10.3390/molecules19078803
卷: 19, 期:7, 页:8803-8819
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Organic
研究领域[WOS]: Chemistry
关键词[WOS]: BIOLOGICAL-ACTIVITY ; ANTITUMOR-ACTIVITY ; BIS-NAPHTHALIMIDES ; ALKYLATING-AGENTS ; ANTICANCER AGENT ; RESISTANT TUMOR ; POTENT ; DERIVATIVES ; DESIGN ; ANALOGS
英文摘要:

A series of N-mustards, which was conjugated to mono-or bis-naphthalimides with a flexible amine link, were synthesized and evaluated for cytotoxicity against five cancer cell lines (HCT-116, PC-3, U87 MG, Hep G2 and SK-OV-3). Several compounds displayed better activities than the control compound amonafide. Further evaluations by fluorescence spectroscopy studies and DNA-interstrand cross-linking assays revealed that the derivatives showed both alkylating and intercalating properties. Among the derivatives, the bis-naphthalimide N-mustard derivative 11b was found to exhibit the highest cytotoxic activity and DNA cross-linking ability. Both 11b and 7b induce HCT-116 cell apoptosis by S phase arrest.

语种: 英语
所属项目编号: 81273370
项目资助者: National Natural Science Foundation of China (NSFC) ; PKU Care Pharmaceutical RD Center
WOS记录号: WOS:000340036200008
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/61363
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:
Lou, Qinghua,Ji, Liyan,Zhong, Wenhe,et al. Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards[J]. MOLECULES,2014,19(7):8803-8819.
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