Summary
The chemotherapeutic activity of 12 newly synthesized nitrosoureas was compared in tests using Yoshida sarcoma ascites cells implanted into the wall of the descending colon in Sprague-Dawley rats. Cyclophosphamide and the nitrosoureas, BCNU, MeCCNU, and chlorozotocin served as positive controls. Among the nitrosoureas tested, 1-(2-hydroxyethyl)-3-(2-chloroethyl)-3-nitrosourea (hydroxyethyl-CNU), chlorozotocin, 1-(2-chloroethyl)-1-nitroso-3-(4-morpholino) urea, 1-(2-chloroethyl)-1-nitroso-3-(1-piperidino) urea, 4-[1-(2-chloroethyl)-1-nitroso]-3-[4-(2,6-dimethylmorpholino)] urea, and 1-(2-chloroethyl)-1-nitroso-3-(3,4-methylenedioxybenzyl) urea were found to be the most active compounds in this tumor model. Based on the present results, morpholino-CNU is considered the most promising compound among these newly synthesized BCNU analogues.
Zusammenfassung
Die chemotherapeutische Wirkung von 12 neu entwickelten Nitrosoharnstoffen wurde vergleichend an Yoshida-Sarkom-Asziteszellen experimentell untersucht, die in die Wand des Colon descendens von Sprague-Dawley-Ratten implantiert worden waren. Cyclophosphamid sowie die Nitrosoharnstoffe BCNU, MeCCNU und Chlorozotocin dienten als positive Kontrolle. Unter den untersuchten Nitrosoharnstoffen zeigten 1-(2-Hydroxyethyl)-3-(2-chlorethyl)-3-nitrosoharnstoff (Hydroxyethyl-CNU), Chlorozotocin, 1-(2-Chlorethyl)-1-nitroso-3-(4-morpholino)-harnstoff, 1-(2-Chlorethyl)-1-nitroso-3-(1-piperidino)-harnstoff, 4-[1-(2-Chlorethyl)-1-nitroso]-3-[4-(2,6-dimethylmorpholino)]-harnstoff und 1-(2-Chlorethyl)-1-nitroso-3-(3,4-methylendioxybenzyl)-harnstoff die stärkste Aktivität in diesem Tumormodell. Auf Grund der vorliegenden Ergebnisse ist Morpholino-CNU als die erfolgversprechendste Substanz unter den neu synthetisierten BCNU-Analogen anzusehen.
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Habs, M., Reinbold, H., Eisenbrand, G. et al. Antitumor activity of new nitrosoureas on Yoshida sarcoma ascites cells implanted into the colon wall of rats. J Cancer Res Clin Oncol 101, 285–302 (1981). https://doi.org/10.1007/BF00410114
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DOI: https://doi.org/10.1007/BF00410114