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学科主题: 药学
题名:
Synthesis and biological evaluation of a novel class of coumarin derivatives
作者: Li, Hong1; Wang, Xiaomin2; Xu, Guichao1; Zeng, Li1; Cheng, Kai1; Gao, Pengchao3; Sun, Qing1; Liao, Wei1; Zhang, Jianwei1
关键词: Amino acid ; Coumarin ; Peptide ; Anti-tumor ; Cytotoxicity
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2014-11-15
DOI: 10.1016/j.bmcl.2014.09.051
卷: 24, 期:22, 页:5274-5278
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: ACTIVATED PROTEIN-KINASE ; MALIGNANT MELANOMA-CELLS ; IN-VITRO ; ACID ; DNA ; COMPLEXES ; ANTITUMOR ; BINDING ; PEPT1
英文摘要:

In this study, several novel coumarin derivatives, 7-hydroxy-2-oxo-2H-chromene-3-carboxyl-Trp-Trp-AA-OBzl compounds, were designed and synthesized as potential anticancer agents. Their in vitro cytotoxic activities were evaluated using methylthiazoltetrazolium (MTT) assay. The anti-tumor activity of the newly coumarin derivatives was determined in a S180 bearing mouse model and some of the compounds demonstrated tumor growth inhibition similar to the positive control, doxorubicin. Compared to doxorubicin, most of the compounds exhibited enhanced immunologic function suggesting a relatively minor toxic effect. The intercalation of the coumarin derivatives synthesized with calf thymus (CT) DNA was also studied. (C) 2014 Elsevier Ltd. All rights reserved.

语种: 英语
所属项目编号: PHR201007114 ; 2011CB504100 ; 81030062 ; 2011ZX09102-003-01 ; 2013BI-01
项目资助者: Academic Human Resources Development in Institutions of Higher Learning Under the Jurisdiction of Beijing Municipality ; National Basic Research Program of China ; National Natural Scientific Foundation of China ; Key National Science &amp ; Technology Specific Projects ; Beijing Pharmacological Society
WOS记录号: WOS:000343901400029
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/56836
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
2.Capital Med Univ, Minist Educ, Key Lab Neurodegenerat Disorders, Dept Physiol, Beijing 100069, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China

Recommended Citation:
Li, Hong,Wang, Xiaomin,Xu, Guichao,et al. Synthesis and biological evaluation of a novel class of coumarin derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(22):5274-5278.
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