Synthesis,Cytotoxicity, Induction of Apoptosis,and Interaction with DNA of Dinuclear Platinum(II) Complexes |
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Authors: | Gang Xu Chuanzhu Gao Prof Shaohua Gou Zhe Cao |
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Affiliation: | 1. Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189 (China);2. Jiangsu Province Hi‐Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189 (China);3. School of Life Science and Technology, Kunming University of Science and Technology, Kunming 650093 (China) |
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Abstract: | Six dicarboxylato‐bridged dinuclear platinum(II) complexes S1 – S6 , with a newly designed chiral ligand, 2‐{(1R,2R)‐2‐aminocyclohexyl]amino}propanoic acid ( HL ), were prepared and spectrally characterized. The in vitro cytotoxicity of all resulting platinum(II) complexes was evaluated against human HCT‐116, MCF‐7, and HepG‐2 tumor cell lines. The results show that all compounds exhibit positive biological activity toward HCT‐116 and MCF‐7 cell lines, of which complexes S3 , S4 , and S5 , with succinate and its derivatives as bridges, showing better activity than the positive controls. Moreover, double‐dyeing flow cytometric resection experiments indicate that the target compounds inhibit tumor cell growth by inducing apoptosis; gel electrophoresis experiments demonstrate the compounds′ ability to prompt pET22b plasmid DNA degradation in almost the same way as oxaliplatin. |
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Keywords: | 1R 2R‐diaminocyclohexyl amino acids antitumor agents apoptosis platinum DNA degradation |
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