Synthesis and biological evaluation of a novel class of coumarin derivatives

被引:15
作者
Li, Hong [1 ]
Wang, Xiaomin [2 ]
Xu, Guichao [1 ]
Zeng, Li [1 ]
Cheng, Kai [1 ]
Gao, Pengchao [3 ]
Sun, Qing [1 ]
Liao, Wei [1 ]
Zhang, Jianwei [1 ]
机构
[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
关键词
Amino acid; Coumarin; Peptide; Anti-tumor; Cytotoxicity; IN-VITRO; ACID; DNA; COMPLEXES; ANTITUMOR; DIFFERENTIATION; INHIBITORS; PEPT1;
D O I
10.1016/j.bmcl.2014.09.051
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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.
引用
收藏
页码:5274 / 5278
页数:5
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