Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 22, Pages 5274-5278Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.09.051
Keywords
Amino acid; Coumarin; Peptide; Anti-tumor; Cytotoxicity
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Funding
- Academic Human Resources Development in Institutions of Higher Learning Under the Jurisdiction of Beijing Municipality [PHR201007114]
- National Basic Research Program of China [2011CB504100]
- National Natural Scientific Foundation of China [81030062]
- Key National Science AMP
- Technology Specific Projects [2011ZX09102-003-01]
- Beijing Pharmacological Society [2013BI-01]
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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.
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