Novel trans-dichloridoplatinum(II) complexes with 3- and 4-acetylpyridine: Synthesis, characterization, DFT calculations and cytotoxicity

Novel complexes of platinum(II) with 3- (1) or 4-acetylpyridine (2) have been synthesized and characterized by elemental analyses, IR, 1H and 13C NMR spectroscopy. Single crystal X-ray diffraction revealed the trans geometry of complex 2. DFT calculations confirm formation of trans isomers for both complexes. The complexes have been tested for their cytotoxicity against HeLa (human cervical cancer), U2OS (human osteosarcoma), U2OScisR (human osteosarcoma cisplatin resistant), B16 (murine melanoma), MDA-453, MDA-361, and MCF-7 (human breast cancer), LS-174 (human colon cancer) and FemX (human melanoma) cell lines. The most promising compound trans-dichloridobis(4-acetylpyridine)platinum(II) (2) overcomes cisplatin resistance of U2OScisR cells after 48 h of drug exposure.

Graphical abstractNovel complexes of platinum(II) with 3- (1) or 4-acetylpyridine (2) have been tested for their cytotoxicity against HeLa, U2OS, U2OScisR, B16, MDA-453, MDA-361, MCF-7, LS-174 and FemX cells. The most promising compound 2 overcomes cisplatin resistance of U2OScisR cells in 48 h.Figure optionsDownload full-size imageDownload as PowerPoint slide