Synthesis and cytotoxicity evaluation of 4-amino-4-dehydroxylarctigenin derivatives in glucose-starved A549 tumor cells
| Autor: | Kun Zhao, Xianwen Gan, Lihong Hu, Qiang Yu, Min Lei |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Clinical Biochemistry
Substituent Pharmaceutical Science Apoptosis Tumor cells Biochemistry Lignans Structure-Activity Relationship chemistry.chemical_compound 4-Butyrolactone Cell Line Tumor Drug Discovery Humans Furans Cytotoxicity Molecular Biology Arctigenin Natural product Organic Chemistry Antineoplastic Agents Phytogenic Glucose chemistry Cancer cell Normal tissue toxicity Molecular Medicine Lead compound |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 25:435-437 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2014.12.061 |
| Popis: | The natural product arctigenin (ATG) demonstrated preferential cytotoxicity to cancer cells under glucose starvation. A series of 4-amino-4-dehydroxylarctigenin derivatives based on lead compound ATG were designed and synthesized by bioisosteric modifications. Their cytotoxicities were evaluated in glucose-starved A549 tumor cells and the results indicated that the 4-amino-4-dehydroxylarctigenin showed more potent cytotoxicity than arctigenin, and the further substituent group on 4-amino would result in the cytotoxicities decreased significantly. 4-Substituted-arctigenin could selectively target on glucose-starved A549 tumor cells which provide an alternative strategy for anticancer drug development with minimal normal tissue toxicity. |
| Databáze: | OpenAIRE |
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