期刊
MEDCHEMCOMM
卷 4, 期 8, 页码 1171-1174出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md20353k
关键词
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资金
- CICYT [BQU-CTQ2012-30930]
- FIS [PI10/00338]
- Generalitat de Catalunya [2009SGR 1024]
- Institute for Research in Biomedicine Barcelona (IRB Barcelona)
- Barcelona Science Park
- La Caixa-IRB Barcelona grant
A series of C2-arylated analogues of the diketopiperazine brevianamide F has been synthesized using a mild Pd-catalyzed CH-activation procedure. Biological evaluation of the new derivatives in different cell lines shows that this modification is responsible for the remarkable change in activity, turning a mild antibiotic and antifungal natural product (brevianamide F) into novel antitumoral compounds. Furthermore, the approach stated represents a new straightforward and versatile methodology with promising applications in peptidomimetics and medicinal chemistry.
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