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EVALUATION OF NAPRO-NU, A 2-CHLOROETHYLNITROSOUREA DERIVATIVE OF NAPHTHALIMIDE, AS A RATIONALLY DESIGNED MIXED-FUNCTION ANTICANCER AGENT
Napro-NU has been synthesized as a new mixed-function anticancer agent from 1,8-naphthalic anhydride. Chemical alkylating activity of Napro-NU exceeded that of N-di(2-chloroethyl)amine as a standard alkylating compound. Napro-NU has displayed an excellent and reproducible antitumor activity in vivo against Sarcoma-180 and Ehrlich ascites carcinoma being more effective than fluorouracil judging by the increase in median survival times of treated animals. Napro-NU also significantly increased the life span of mice bearing highly advanced tumors for 10 days before the drug challenge. The compound under study did not adversely affect hematopoiesis. Drug-induced hepatotoxicity and nephrotoxicity also were not detected. Meanwhile screening in vitro in 6 different human tumor cell lines did not reveal any significant cytotoxic activity.
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