Summary
The antineoplastic activity of 7 ester derivatives and 15 amide derivatives of N-[N′-(2-chloroethyl)-N′-nitrosocarbamoyl (CNC)]-aminoacids was examined in transplanted rat leukemia L 5222. All esters except the ethylester of CNC-l-isoleucine showed only a moderate antitumor activity. CNC-l-isoleucine ethylester effected some cures and showed the lowest toxicity of this series of compounds.
The amide derivatives on the other hand were highly active in L 5222; all compounds effected cures in the dose range investigated.
This is a preview of subscription content, log in via an institution to check access.
References
Ehresmann K, Zelezny O, Eisenbrand G (1984) Syntheses of potentially antineoplastic amides and esters of N-[N′-(2-chroroethyl)-N′-nitrosocarbamoyl] amino acids. II. Arch Pharm (Weinheim) 317:481–487
Eisenbrand G, Habs M, Zeller WJ, Fiebig HH, Berger M, Zelezny O, Schmähl D (1981) New nitrosoureas — therapeutic and long-term toxic effects of selected compounds in comparison to established drugs. In: Serrou B, Schein PS, Imbach J-I (eds) Nitrosoureas in cancer treatment. Elsevier/North Holland, Amsterdam, pp 175–191
Spreafico F, Filippeschi S, Falautano P, Eisenbrand G, Fiebig HH, Habs M, Zeller WJ, Berger M, Schmähl D, van Putten LM, Smink T, Csanyi E, Somfai-Relle S (1981). In: Prestayko AW, Crooke ST, Baker LM, Carter SK, Schein PS (eds), Nitrosoureas: Current status and new developments. Academic Press, New York, pp 27–42
Suami T, Kato T, Takino H, Hisamatsu T (1982) 2-Chloroethylnitrosourea congeners of amino acid amides. J Med Chem 25:829–832
Zeller WJ, Eisenbrand G (1981) Examination of newly synthesized 2-chloroethylnitrosoureas on rat leukemia L 5222. Oncology 38:39–42
Zeller WJ, Eisenbrand G, Fiebig HH (1978) Chemotherapeutic activity of new 2-chloroethylnitrosoureas in rat L 5222 leukemia: Comparison of bifunctional and water-soluble derivatives with 1,3-bis(2-chloroethyl)-I-nitrosourea. J Natl Cancer Inst 60:345–348
Zeller WJ, Eisenbrand G, Fiebig HH (1979) Examination of four newly synthesized 2-chloroethylnitrosoureas in comparison with BCNU, CCNU, MeCCNU, chlorozotocin and hydroxyethyl-CNU in preterminal rat leukemia L 5222. J Cancer Res Clin Oncol 95:43–49
Zeller WJ, Berger M, Eisenbrand G, Tang W, Schmähl D (1982) Chemotherapeutic activity of 2-chlorethylnitrosocarbamoyl derivatives of amino acids in a transplanted rat leukemia (L 5222). Arzneimittelforsch 32:484–486
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Zeller, W.J., Ehresmann, K. & Eisenbrand, G. Antineoplastic activity of esters and amides of N-[N′-(2-chloroethyl)-N′-nitrosocarbamoyl]-aminoacids. J Cancer Res Clin Oncol 108, 249–251 (1984). https://doi.org/10.1007/BF00402478
Received:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF00402478