Human cancer inhibitory peptide amides

Details Human cancer inhibitory peptide amides Human cancer inhibitory peptide amides

C - Chemistry, Metallurgy

07

K

C07K 7/02 (2006.01) A61K 38/07 (2006.01) A61K 38/08 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2154205

This application discloses seven newly synthesized pentapeptide amides and four tetrapeptide amides. The synthesis utilized both naturally occurring and modified amino acids; the modified amino acids are constituents of the well known dolastatin 10 and dolastatin 15 which are structurally distinct peptides with excellent antineoplastic activity. These peptides were constructed by introducing a peptide bond between selected amino acids and modified amino acids and coupling the resulting di- and tri-peptides to obtain peptides having a high anticancer activity against a series of human cancer cell lines. Image 8 a) R = Met-NH-2ClPh 8 g) R = Met-NH-Q 8 b) R = Met-NH-4ClPh 10 a) R = Doe 8 c) R = Phe-NH-3ClPh 10 b) R = NH-2ClPEA 8 d) R = Phe-NH-4ClPh 10 c) R = NH-3ClPEA 8 e) R = Met-NH-BnThz 10 d) R = NH-4ClPEA 8 f) R = Pro-NH-BnThz

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