European Journal of Medicinal Chemistry 2009-05-01

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

Gordana M Rakić, Sanja Grgurić-Sipka, Goran N Kaluderović, Santiago Gómez-Ruiz, Snezana K Bjelogrlić, Sinisa S Radulović, Zivoslav Lj Tesić, Gordana M. Rakić, Sanja Grgurić-Šipka, Goran N. Kaluđerović, Santiago Gómez-Ruiz, Snežana K. Bjelogrlić, Siniša S. Radulović, Živoslav Lj. Tešić

文献索引：Eur. J. Med. Chem. 44(5) , 1921-5, (2009)

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摘要

Novel complexes of platinum(II) with 3- (1) or 4-acetylpyridine (2) have been synthesized and characterized by elemental analyses, IR, (1)H and (13)C 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 48h of drug exposure.