Evaluation of 'cypenhymustine', a new anticancer compound, in murine tumour models.
'Cypenhymustine', 3-[2-[bis(2'-chloroethyl)-amino] ethyl]-5,5- tetramethylenehydantoin, has been synthesised as a potential analog of spiromustine (NSC 172112). The LD50 value was determined in Swiss male mice and found to be 65.0 mg/kg by single i.p. injection. In 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-HN2.
Sanyal
U
U
Department of Chemotherapy, Chittaranjan National Cancer Institute, Calcutta, India.
Bhattacharya
S
S
Sadhu
U
U
Dutta
S
S
Das
H
H
Ghosh
M
M
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006827:Hydantoins / Q000138:chemical synthesis / Q000627:therapeutic use*; D007928:Lethal Dose 50; D008223:Lymphoma / Q000188:drug therapy; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D009588:Nitrogen Mustard Compounds / Q000138:chemical synthesis / Q000627:therapeutic use*; D012510:Sarcoma 180 / Q000188:drug therapy
D000970:Antineoplastic Agents; D006827:Hydantoins; D009588:Nitrogen Mustard Compounds; C082180:cypenhymustine