Abstract |
' 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.
|
Authors | U Sanyal, S Bhattacharya, U Sadhu, S Dutta, H Das, M Ghosh |
Journal | Cancer letters
(Cancer Lett)
Vol. 70
Issue 1-2
Pg. 1-6
(Jun 15 1993)
ISSN: 0304-3835 [Print] Ireland |
PMID | 8330289
(Publication Type: Journal Article)
|
Chemical References |
- Antineoplastic Agents
- Hydantoins
- Nitrogen Mustard Compounds
- cypenhymustine
|
Topics |
- Animals
- Antineoplastic Agents
(chemical synthesis, therapeutic use)
- Carcinoma, Ehrlich Tumor
(drug therapy)
- Dose-Response Relationship, Drug
- Drug Screening Assays, Antitumor
- Hydantoins
(chemical synthesis, therapeutic use)
- Lethal Dose 50
- Lymphoma
(drug therapy)
- Male
- Mice
- Mice, Inbred Strains
- Nitrogen Mustard Compounds
(chemical synthesis, therapeutic use)
- Sarcoma 180
(drug therapy)
|