Elucidation and synthesis of selected pentapeptides

Details Elucidation and synthesis of selected pentapeptides Elucidation and synthesis of selected pentapeptides

C - Chemistry, Metallurgy

07

K

C07K 7/02 (2006.01) A61K 38/08 (2006.01) C07K 1/02 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2114156

The sea hare Dolabella auricularia has yielded many structurally distinct peptides which possess antineoplastic activity. Presently the compound denominated "dolastatin 10" represents then most important of such peptides because of its demonstrated potential as an anticancer drug. The present invention relates to the systematic creation of five unique pentapeptides by selectively coupling a tripeptide - trifluoroacetate salt with a preselected dipeptide-trifluoroacetate salt which provide active molecules capable of emulating the measured therapeutic effect of dolastatin 10. The pentapeptides hereof have the structure shown below: Image wherein R is selected from the following group of substituents: Image

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