Synthesis of Novel Benzothiazolo[3,2-a]pyridimidin-4-ones with Potential Cytotoxic and Pro-Apoptotic Potential

摘要

The combination of cyclocondensation with palladium catalysed cross-coupling reactions, afforded a variety of 8-functionalized benzothiazolo[3,2-a]pyridimidin-4-ones in good to excellent yields. The anti-proliferative potential of the synthetic compounds was evaluated in human cervical adenocarcinoma cells (HeLa) and hamster normal fibroblasts (BHK-21). Three of the test derivatives exhibited the strongest cytotoxicity in HeLa cells with the median inhibitory concentration (IC50) of 0.93, 1.55 and 1.84 μM, respectively. Moreover, their anti-proliferative effect was three times less strong in normal fibroblasts, asserting their possible anti-cancer potential.