EVALUATION OF NAPROMUSTINE, A NITROGEN MUSTARD DERIVATIVE OF NAPHTHALIMIDE, AS A RATIONALLY DESIGNED MIXED-FUNCTION ANTICANCER AGENT
Napromustine, a new nitrogen mustard of substituted naphthalimide, has been synthesized as a new mixed-function anticancer agent from N-(3-bromopropyl) naphthalimide. Chemical alkylating activity of Napromustine exceeded that of N-di(2-chloroethyl)amine as a standard alkylating compound. Napromustine has displayed an excellent and reproducible antitumor activity in vivo against Sarcoma-180 and Ehrlich ascites carcinoma comparable to that of fluorouracil judging by the increase in median survival times of treated animals. Napromustine 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 affect hematopoiesis or induce hepatotoxicity and nephrotoxicity. This compound inhibits the synthesis of DNA and RNA in S-180 tumor cells. Meanwhile in vitro screening in 3 different human tumor cell lines did not reveal any significant cytotoxic activity.
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