Synthesis, Characterization and Antitumour Activity of Di-n-Butyltin Salicyloxamate

The synthesis and characterization of di-n-butyltin and dimethyltin salicyloxamate, respectively compounds 1 and 2, are reported. Compound 1 is more active than cisplatin, 5-fluorouracil and etoposide against seven tumoural cell lines of human origin, but less active than methotrexate and doxorubucin. Diorganotin derivatives of salicylic acid and its substituted analogs exhibit antitumour activities in vitro against human tumoural cell lines 1,2. The phenolic hydroxy group of salicylic acid is not involved in its reaction with diorganotin oxides3,4. In fact, salicylic acid behaves in this respect as benzoic acid, giving rise to diorganotin disalicylates with free hydroxy groups. This report presents the synthesis and characterization of di-n-butyltin and dimethyltin salicyloxamate, respectively compounds 1 and 2, in order to find out whether the phenolic hydroxy group of salicyloxamic acid is involved when reacting with diorganotin oxides. The antitumour activity of compound 1 was determined for comparison with that of the corresponding di-n-butyltin salicylate5.