Abstract:
The present invention provides antitumor peptides of formula (I): A-B-NR -CHD-CH(OCH3)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R R N-CHX-CO, wherein R is a methyl group or an ethyl group, R is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.
Abstract:
The present invention provides antitumor peptides of formula (I): A-B-NR3-CHD-CH(OCH¿3?)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R?1R2¿N-CHX-CO, wherein R1 is a methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C¿2?-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.
Abstract:
The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N,N-dimethyl-2-ethylphenylglycyl, or an amino acid residue of the formula R1R2N-CHX-CO, wherein R1 is a-methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of Formula I in a pharmaceutically acceptable composition.
Abstract:
The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N,N-dimethyl-2-ethylphenylglycyl, or an amino acid residue of the formula R1R2N-CHX-CO, wherein R1 is a-methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of Formula I in a pharmaceutically acceptable composition.
Abstract:
The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N,N-dimethyl-2-ethylphenylglycyl, or an amino acid residue of the formula R1R2N-CHX-CO, wherein R1 is a-methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of Formula I in a pharmaceutically acceptable composition.