Pentapeptide methyl esters

Details Pentapeptide methyl esters Pentapeptide methyl esters

C - Chemistry, Metallurgy

07

K

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

Patent

CA 2154203

Herein disclosed are several pentapeptide methyl ester derivatives of dolastatin 10, using both naturally occurring and modified amino acids. The selected modified amino acids are constituents of dolastatin 10 which is a structurally distinct peptide with excellent in vitro and in vivo antineoplastic activity. The structures of these compounds are as shown below: Image 10a) R1 = i- Pr ; R = -NH(Me)2 ; R2 = -CH2CH2CH2NH-cbz 10b) R1 = i-Pr ; R = -NH(Me)2 ; R2 = Image 11a) R1 = -(CH2)4NH-cbz ; R = -NH(cbz) ; R2 = Image 11b) R1 = Image ; R = -NH(cbz) ; R2 = -CH2CH2CH2NH-cbz 11c) R1 = Image ; R = -NH(cbz) ; R2 = -CH2-S-Me 29

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