Human cancer inhibitory pentapeptide methyl esters

摘要

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: $10a)\; R1\; =\; i-Pr\; ;\; R\; =\; -NH(Me)2\; ;\; R2\; =\; -CH2CH2CH2NH-cbz\; 10b)\; R1\; =\; i-Pr\; ;\; R\; =\; -NH\; (Me)2\; ;11a)\; R1\; =\; -\; (CH2)4NH-cbz\; ;\; R\; =\; -NH\; (cbz)\; ;11b)R\; =\; -NH(cbz)\; ;\; R2\; =\; -CH2CH2CH2NH-cbz\; 11c)R\; =\; -NH(cbz)\; ;\; R2\; =\; -CH2-S-Me\; m$