Novel iron(III) complexes based on 2-hydrazinylpyrimidine derivative: Synthesis, characterization and preliminary evaluation of antitumor activity

Abstract

Novel pyrimidine derivative H2L (H2L=2‑methoxy-6-(pyrimidin-2-yl-hydrazonomethyl)- phenol) and its Fe(III) complexes [FeIII(HL)2]X⋅nsolvent (X = Cl− (1), BF4− (2), PF6− (3)) were synthesized and characterized by single-crystal X-ray diffraction, powder X-ray diffraction, elemental analyses, IR and UV–vis spectra. The stability in solution, lipophilicity and antitumor activities were investigated. Their antitumor activities in vitro were evaluated by MTT assays against BGC-823 and BEL-7402 cell lines. Structural data of complexes 1–3 indicate that they are all mononuclear and the coordination geometries of FeIII are all distorted octahedral. The antitumor activity results indicated that H2L and complexes 1–3 all exhibited inhibitory activities against BGC-823 and BEL-7402 cancer cell lines. H2L was more effective in BGC-823 cells. While complexes 1–3 exhibited higher inhibitory activities against BEL-7402 cells (IC50=21.80~27.96 µM) than corresponding H2L (IC50 = 49.46 µM), which showed synergetic effect between H2L and the central iron(III) ion.