Cytotoxic boronic acid peptide analogs

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.

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530402, A61K 3700, A01N 5508, C07K 500, C07K 700

Patent

active

051590603

ABSTRACT:
A method is provided for inhibiting growth of cancer cells comprising contacting said cells with an effective growth-inhibiting amount of a compound of the formula (II): ##STR1## or a physiologically acceptable salt thereof, wherein A.sup.1 and A.sup.2 are individually L-amino acid residue selected from the group consisting of Ala, Pro, Gly, Glu, Leu, Lys, Phe, Ser, Vl, Ile, Arg, Tyr, Thr, Asp, Asn and Gly; R.sup.1 is C.sub.1 -C.sub.6 (alkyl) which is unsubstituted or is substituted with an aromatic substituent or one or more in-chain bivalent groups selected from the group consisting of --O--, --CO--, --S--, --NH--, --CONH--, CH.dbd.CH--, and --SO.sub.2 --; Y.sup.1 and Y.sup.2 are each H, or taken together form a moiety derived from a dihydroxy compound, and R.sup.1 is H or an N-terminal protecting group.

REFERENCES:
patent: 4499082 (1985-02-01), Shenvi et al.
patent: 4537773 (1985-08-01), Shenvi
patent: 4963655 (1990-10-01), Kinder et al.
D. H. Kinder et al., J. Med. Chem., 28, 1917 (1985).
B. Goz et al., Biochem. Pharmacol., 35, 3587 (1986).
D. S. Matteson et al., J. Amer. Chem. Soc., 103, 5241 (1981).
C. A. Kettner and A. B. Shenvi, J. Biol. Chem., 259 15106 (1984).
J. A. Parsons, Peptides Hormones, Unverisity Park Press, London (1976) at pp. 1-6.

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