Efficient synthesis of eudistomin U and evaluation of its cytotoxicity.
| Autor: | Roggero CM; Providence College, Department of Chemistry and Biochemistry, 1 Cunningham Square, Providence, RI 02918, USA., Giulietti JM; Providence College, Department of Chemistry and Biochemistry, 1 Cunningham Square, Providence, RI 02918, USA., Mulcahy SP; Providence College, Department of Chemistry and Biochemistry, 1 Cunningham Square, Providence, RI 02918, USA. Electronic address: smulcahy@providence.edu. |
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| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2014 Aug 01; Vol. 24 (15), pp. 3549-51. Date of Electronic Publication: 2014 May 27. |
| DOI: | 10.1016/j.bmcl.2014.05.049 |
| Abstrakt: | Eudistomin U is a member of a subclass of naturally occurring indole alkaloids known as β-carbolines. These molecules are reported to have diverse biological activity and high binding affinity to DNA, which make them attractive targets for total synthesis. We describe an efficient, five-step synthesis of eudistomin U by employing two key reactions: a Bischler-Napieralski cyclization and a Suzuki cross coupling. We also describe the cytotoxicity of eudistomin U against various cancer cell lines and human pathogens, in which we observed potent antibacterial activity against Gram-positive bacteria. (Copyright © 2014 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
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