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Antitumor action of N-(2-chloroethyl)-N-nitrosocarbamoyl derivatives of biologically active polypeptide hormone fragments

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The antitumor action of the 2-chloroethylnitrosocarbamoyl derivatives of peptides related to the 9–13 amino acid residues of α-MSH/ACTH and of the C-terminal tetrapeptide analogue of gastrin have been investigated. Series of 2-chloroethylnitrosoureas attached to amino acids, di-, tri-, tetra-, or pentapeptides were examined in a primary screening system. Among these compounds the Pro-Val-, Lys-Pro-Val-, and Trp-Gly-Lys-Pro-Val-containing 2-chloroethylnitrosocarbamoyl groups were the most effective in the L1210 system. The human melanoma xenograft line was also affected by these agents, while colorectal xenografts were insensitive. A combination of tripeptide-2-chloroethyl-nitrosourea with BCNU induced more than additive growth inhibition of L1210 leukemia.

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Correspondence to A. Jeney.

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Jeney, A., Kopper, L., Nagy, P. et al. Antitumor action of N-(2-chloroethyl)-N-nitrosocarbamoyl derivatives of biologically active polypeptide hormone fragments. Cancer Chemother. Pharmacol. 16, 129–132 (1986).

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  • Melanoma
  • Antitumor Action
  • Human Melanoma
  • Screening System
  • BCNU