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Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards
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
2014-07-01
DOI10.3390/molecules19078803
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
WOS记录号WOS:000340036200008
项目编号81273370
资助机构National Natural Science Foundation of China (NSFC) ; PKU Care Pharmaceutical RD Center
引用统计
被引频次:2[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/400002259/61363
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
推荐引用方式
GB/T 7714
Lou, Qinghua,Ji, Liyan,Zhong, Wenhe,et al. Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards[J]. MOLECULES,2014,19(7):8803-8819.
APA Lou, Qinghua.,Ji, Liyan.,Zhong, Wenhe.,Li, Shasha.,Yu, Siwang.,...&Meng, Xiangbao.(2014).Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards.MOLECULES,19(7),8803-8819.
MLA Lou, Qinghua,et al."Synthesis and Cytotoxicity Evaluation of Naphthalimide Derived N-Mustards".MOLECULES 19.7(2014):8803-8819.
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