Tetrapeptide derivative having antitumor activity

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 4 to 5 amino acid residues in defined sequence

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C07K 500, C07K 700, C07K 1700, A61K 3800

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active

056543999

ABSTRACT:
A tetrapeptide derivative represented by the following formula or a salt thereof has a higher cyto-static activity than dolastatin 10, and is useful as an antitumor agent: ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each represent a hydrogen atom, a lower alkyl group or an aralkyl group;

REFERENCES:
patent: 4816444 (1989-03-01), Pettit et al.
patent: 4978744 (1990-12-01), Pettit et al.
patent: 5017691 (1991-05-01), Lee et al.
Pettit et al., J. Am. Chem. Soc., "The Isolation and Structure of a Remarkable Marine Animal Antineoplastic Constituent: Dolastain 10.sup.1a ", vol. 109, pp. 6883-6885 (1987).
Schroder et al., The Peptides, vol. 1, "Formation of the Peptide Bond", pp. 76-136 (1965).
Bai et al., Biochemical Pharmacology, "Structure-Activity Studies with Chiral Isomers and with Segments of the Antimitotic Marine Peptide Dolastatin 10", vol. 40, No. 8, pp. 1859-1864 (1990).
Pettit et al., J. Med. Chem., "Chiral Modifications of Dolastatin 10: The Potent Cytostatic Peptide (19aR)-Isodolastatin 10.sup.1 ", vol. 33, pp. 3132-3133 (1990).

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