Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 16, Pages 4920-4931Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm8000828
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Funding
- CICYT [CTQ2006-03794/BQU]
- Generalitat de Catalunya [2005SGR 00662]
- ISCIII
- Institute for Research in Biomedicine
- Barcelona Science Park
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Kahalalide F (KF) is a natural product currently under phase II clinical trials. Here, we report the solid phase synthesis of 132 novel analogues of kahalalide F and their in vitro activity on a panel of up to 14 cancer cell lines. The structure - activity relationship of these analogues revealed that KF is highly sensitive to backbone stereotopical modification but not to side chain size modification. These observations suggest that this compound has a defined conformational structure and also that it interacts with chiral compounds through its backbone and not through its side chains. The N-terminal aliphatic acid appears to be a hydrophobic buoy in a membrane-like environment. Moreover, significant improvement of the in vitro activity was achieved.
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