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Synthesis, crystal structure and biological activity of two Mn complexes with 4-acyl pyrazolone derivatives

Yue Li  Guan-Cheng Xu  
【摘要】:A great many Schiff base complexes with transition metals have been confirmed possessing biological and pharmaceutical activities, such as anticancer, antitumor and antioxidative activities as well as the inhibition of lipid peroxidation, etc. In this paper, two Mn complexes [Mn(HLa)(La)]·(CH3CN)1.5·H2O(1) and [Mn2(Lb)2(μ-Et O)2(Et OH)2](2)(H2La=N-(1-phenyl-3- methyl-4-benzoyl-5-pyrazolone)-2-thiophenecarboxylic acid hydrazide, H2Lb=N-(1-phenyl-3-methyl-4-propenylidene-5-pyrazolone)-2-thiophenecarboxylic acid hydrazide) have been synthesized and characterized. Single crystal X-ray diffraction analysis indicated that 1 is a mononuclear complex and 2 exhibits a dinuclear centrosymmetric structure. Binding of the complexes with Herring Sperm DNA(HS-DNA) and were showed that complexes 1 and 2 could intercalate to DNA and quench the intrinsic fluorescence of BSA in a static quenching process. Further, the inhibitory effects of the complexes on the cell population growth of the human esophageal cancer Eca-109 cells and the cervical cancer He La cells were determined by MTT assay, which indicated that both 1 and 2 significantly inhibited the growth of Eca-109 and He La cells, the inhibitory activity of complex 1 is stronger than that of 2. We further observed that complex 1 inhibited the growth of He La cells through inducing the apoptosis and arresting cell cycle at S phase.

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