Abstract
‘Cypenhymustine’, 3-[2- s(2′-chloroethyl)amino ethyl]-5,5-tetramethylenehydantoin, has been synthesised as a potential analog of spiromustine (NSC 172112). The LD 50 value was determined in Swiss male mice and found to be 65.0 mg/kg by single i.p. injection. In vivo screening experiments, three parameters, namely, ascites cell count, ascites fluid measurement and increase in life span (ILS) of drug-treated over control Swiss mice were studied in three murine ascites tumours namely Ehrlich ascites carcinoma (EAC), sarcoma-180 (S-180) and Dalton's lymphoma (DL). Cypenhymustine exhibited a very high percentage of inhibition of both the ascites cell and fluid in these models and also displayed excellent reproducible ILS activity (ILS values of 151 in EAC, 157 in S-180 and 181 in DL at the optimum dose of 3 mg/kg for days 1–7 treatment following tumour transplant on day 0) having a ‘curative’ effect (1–2 animals: 6 having > 60 days survival rate). The chemical alkylating activity has been compared with spiromustine and another antitumour agent namely nor-HN 2.
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