New derivatives of CNC-amino acids and -oligopeptides: experimental antitumor activity.
The experimental antitumor activity of a series of new nitrosoureas is described in which the chloroethylnitrosocarbamoyl (CNC) group is attached to different carrier molecules: amino acids and oligopeptides. Of a group of 10 CNC-amino acid amide derivatives the majority displayed high therapeutic activity in L 5222 leukemia. Some compounds, especially the proline and sarcosine derivatives, showed favorable therapeutic ratios; 12 CNC-oligopeptides displayed a more or less pronounced therapeutic activity in L 1210 leukemia. Compounds bearing a free carboxy group were less active than the corresponding unsubstituted or N-methyl substituted amides.
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D000596:Amino Acids / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy / Q000401:mortality; D007942:Leukemia, Experimental / Q000188:drug therapy / Q000401:mortality; D008297:Male; D009607:Nitrosourea Compounds / Q000627:therapeutic use*; D009842:Oligopeptides / Q000627:therapeutic use*; D051381:Rats; D011919:Rats, Inbred Strains
D000596:Amino Acids; D000970:Antineoplastic Agents; D009607:Nitrosourea Compounds; D009842:Oligopeptides