Abstract
A series of platinum(II) complexes of the type [NEt 4][PtLBr 3] where L is a 2-styrylbenzothiazole or 2-styrlbenzole was prepared. The complexes were characterized by their melting points, elemental analyses, UV-Vis and far-infrared spectra, and 1H and 195Pt NMR spectroscopy. The NMR data are consistent with coordination of the benzoheterazole ligands to the Pt ion through the nitrogen atom. The ligands and the complexes were assayed for cytotoxicity against U937 human histiocytic lymphoma cells. It was observed that the ligands displayed very poor cytotoxicity, while the Pt(II) complexes demonstrated marked cytotoxicities and a structure-activity correlation was established. Pt(II) complexes containing S as the heteroatom in the benzoheterazole ring were generally more active than their O-containing counterpart. The position and type of substituents in the styryl moeity were also important for biological activity. Our data indicate that adjacent methoxy functionalities were present in the most potent drugs tested. Further development of active Pt(II) complexes with improved solubilities is warranted.
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