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Issue 18, 2018
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Tryptanthrin derivative copper(II) complexes with high antitumor activity by inhibiting telomerase activity, and inducing mitochondria-mediated apoptosis and S-phase arrest in BEL-7402

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Abstract

The copper(II) complexes of tryptanthrin (Try) and 8-bromo-tryptanthrin (BrTry), [CuII(Try)2Cl2] (Try-Cu) and [CuII(BrTry)2Cl2] (BrTry-Cu), were synthesized and fully characterized by spectroscopic methods and single-crystal X-ray diffraction analysis. The copper(II) centers in the Try-Cu and BrTry-Cu complexes adopted an approximately six-coordinated distorted octahedral geometry. The anticancer activities of Try-Cu and BrTry-Cu were evaluated in vitro against four human cancer cell lines (BEL-7402, T-24, MGC80-3, and HepG2 cells) and one normal human liver cell line (HL-7702 cells). It was found that Try-Cu exhibited selective cytotoxicity against the four selected cancer cells (IC50 = 4.02–9.03 μM) but low cytotoxicity toward the normal human liver HL-7702 cells. Further studies revealed that Try-Cu exhibited its cytotoxic activity mainly by inducing DNA damage and thus causing cell cycle arrest in the S phase, as well as stimulating mitochondrial dysfunction and inhibiting telomerase by interacting with the c-myc promoter.

Graphical abstract: Tryptanthrin derivative copper(ii) complexes with high antitumor activity by inhibiting telomerase activity, and inducing mitochondria-mediated apoptosis and S-phase arrest in BEL-7402

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Publication details

The article was received on 16 Jun 2018, accepted on 12 Aug 2018 and first published on 13 Aug 2018


Article type: Paper
DOI: 10.1039/C8NJ03005G
Citation: New J. Chem., 2018,42, 15479-15487
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    Tryptanthrin derivative copper(II) complexes with high antitumor activity by inhibiting telomerase activity, and inducing mitochondria-mediated apoptosis and S-phase arrest in BEL-7402

    Q. Qin, B. Zou, M. Tan, S. Wang, Y. Liu and H. Liang, New J. Chem., 2018, 42, 15479
    DOI: 10.1039/C8NJ03005G

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