Synthesis, characterization and anti-proliferative activity of heterocyclic hypervalent organoantimony compounds

• Six heterocyclic hypervalent organoantimony compounds were synthesized.
• They showed good anti-proliferative activity in human alveolar adenocarcinoma cell line A549.
• Their inhibition effect on A549 is achieved by cell cycle arrest and apoptosis.
• It is the first example using heterocyclic hypervalent organoantimony compounds against tumor-cell line.

Three heterocyclic hypervalent organoantimony chlorides RN(CH2C6H4)2SbCl (2a R = t-Bu, 2b R = Cy, 2c R = Ph) and their chalcogenide derivatives [RN(CH2C6H4)2Sb]2O (3a R = t-Bu, 3b R = Cy, 3c R = Ph) were synthesized and characterized by techniques such as 1H NMR, 13C NMR, X-ray diffraction, and elemental analysis. It is found that the anti-proliferative activity detected over these compounds can be attributed to the coordination bond between the antimony and nitrogen atoms of these compounds. Moreover, a preliminary study on mechanistic action suggests that the inhibition effect is ascribable to cell cycle arrest and cell apoptosis.

Six hypervalent organoantimony compounds were synthesized and characterized. The preliminary study shows that the inhibition effect is achieved by cell cycle arrest and apoptosis.Figure optionsDownload as PowerPoint slide