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

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• 作者：Gordana M. Raki&#x107 ; Sanja Grguri&#x107 ; -Š ; ipka ; Goran N. Kaluđ ; erovi&#x107 ; Santiago Gó ; mez-Ruiz ; Snež ; ana K. Bjelogrli&#x107 ; Siniš ; a S. Radulovi&#x107 ; Ž ; ivoslav Lj. Teš ; i&#x107
• 关键词：Platinum(II) ; Antitumoral activity ; DFT ; X-ray
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：May 2009
• 年：2009
• 卷：44
• 期：5
• 页码：1921-1925
• 全文大小：265 K

文摘

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.