[Antibacterial and antineoplastic activity of 2,4-disubstituted 6H-5,1,3-benzothiadiazocines].

Nine 2,4-disubstituted 6H-5,1,3-benzothiadiazocines have been tested for antibacterial and cytotoxic efficacy. None of the tested compounds showed any significant antibacterial activity in comparison with ampicillin. The most cytotoxic effect was manifested by those derivatives which have morpholine or phenyl in position 2 and benzimidazole, imidazole or 1,2,4-triazole in position 4. The highest concentrations of derivatives I, VII, IX induced an acute cytotoxic effect which was manifested by cell lysis after 24 h of culturing. Derivative VII, concentration 30.5 mumol/L, and derivative IX, concentration 13.3 mumol/L, exhibited a delayed cytotoxic effect on L1210 cells. While during the first 24 and 48 h a certain part of cell population proliferated, during further 24 h a total inhibition of cell division was found. The cytotoxic concentration of derivative IX induced damage to the integrity of the cytoplasmic membrane. Benzothiadiazocines I, VII and IX induced a two-phase unbalanced growth. Based on these results, benzothiodiazocines I, VII and IX could be considered new potential anticancer drugs which are appropriate for further research.