Vinblastin-23-oyl amino acid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514 17, 514 18, 514 19, 540478, C07D51904, C07D 4716, A61K 3140

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active

046394567

ABSTRACT:
Vinblastine derivatives of the formula ##STR1## wherein R.sub.1 is an ester of a .alpha.-aminoacid selected from the group consisting of glycine, alanine, valine, leucine, isoleucine, serine, threonine, aspartic acid, glutamic acid, aspargine, glutamine, arginine, lysine, cysteine, cystine, methionine, phenylalanine, tyrosine, tryptophan, proline, histidine, hydroxy-lysine, hydroxyproline, or of a peptide consisting of 1-6 identical or different such amino-acids, and the ester group, which may be straight or branched, being a carboalkoxy group having 2-9 carbon atoms, and R.sub.2 is hydrogen or a C.sub.2 -C.sub.9 alkanoyl group, R.sub.5 is H or OH, R.sub.6 is CH.sub.3, CHO or H and X=H or Br and their pharmaceutically acceptable mineral or organic acid addition salts. The compounds are useful as antitumor drugs.

REFERENCES:
patent: 4029663 (1977-06-01), Gutowski et al.
patent: 4144237 (1979-03-01), Kutney
patent: 4203898 (1980-05-01), Cullinan et al.
patent: 4388305 (1983-06-01), Trouet et al.
patent: 4430269 (1984-02-01), Pearce
Lewin et al., Heterocycles, vol. 14, No. 12, pp. 1915-1920 (1980).

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