Development of differential cytotoxic compounds containing nitrosourea and benzothiazine nucleus
Nyati, M.K.; Rai, D.; Gupta, R.R.; Dev, P.K.
In Vivo 11(1): 95-99
1997
ISSN/ISBN: 0258-851X PMID: 9067778 Document Number: 475010
The in vivo activity of 4 new benzothiazinyl -nitrosourea compounds was investigated against Sarcoma-180 (S-180) and Ehrlich Ascitic Carcinoma (EAE) induced ascitic and solid tumors. EAC solid tumor was found to be the most sensitive, where one compound (no 4) inhibited tumor growth to only 3 per cent of the control value. All the 4 compound tested were found to be toxicologically more selective than 5-fluorouracil and 6-mercaptopurine drugs. The reason for this selective toxicity may be attributed to the inhibition of isocyanate moiety in these compounds which causes toxicity to normal cells via a carbamoylation reaction. However, they may still remain potent, since they decompose into an alkylating carbonium species and a charge transfer complex which may interact with DNA via alkylation and intercalation reactions, respectively.