| Autor: |
Wen-Shan, Li, Chie-Hong, Wang, Shengkai, Ko, Tzu Ting, Chang, Ya Ching, Jen, Ching-Fa, Yao, Shivaji V, More, Shu-Chuan, Jao |
| Rok vydání: |
2012 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 55(4) |
| ISSN: |
1520-4804 |
| Popis: |
Current chemical and biological interest in indole-3-carbinol (I3C) and its metabolites has resulted in the discovery of new biologically active indoles. As part of a program aimed at the development of indole analogues, tetraindoles 1-15 were prepared and their antiproliferative effects on human breast cancer cells were evaluated. The results show that the 5-hydroxy-tetraindole 8 (SK228) has optimum antiproliferative activity against breast adenocarcinoma (MCF 7 and MDA-MB-231) cells and that this activity involves G(2)-phase arrest of the cell cycle with a distinctive increase in the expression of cyclin B1 and phospho-cdc2. Further observations suggest that 5-hydroxy-tetraindole 8 induces apoptosis through externalization of membrane phosphatidylserine, DNA fragmentation, and activation of caspase-3. Given the fact that I3C and its metabolites have been shown to improve therapeutic efficacy and to have a broad range of antitumor activities in human cancer cells, the current findings have important pharmacological relevance as they open a promising route to the development of a potential chemotherapeutic application of tetraindoles as agents for the treatment of breast cancer. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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