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Retracted: Studies of proteasome inhibition and antitumor activity by novel amino acid-polypyridine-copper complexes

Journal 2019 · IF 1.241 · 56(12): 3354-3362 · 发表于 2019 年 9 月 13 日
作者: Zi-Bo Yang,Dong-Dong Li,Xiu-Mei Zhao,Lu-Yao Wang,Lin-Lin Dai
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摘要

Five innovative ternary copper (II) complexes [Cu (OH-PIP)(Phe)Cl]( 1 ), [Cu (OH-PIP)(Gly)(H 2 O)]NO 3 ·2H 2 O ( 2 ), [Cu (OH-PIP)(Ala)(Cl)]·H 2 O ( 3 ), [Cu (OH-PIP)(Met)]PF 6 ·2H 2 O ( 4 ), and [Cu (OH-PIP)(Gln)(H 2 O)]Cl·3H 2 O ( 5 ) have been synthesized and characterized by infrared spectroscopy, elemental analysis, and single crystal X-ray diffraction analysis. X-ray crystallography showed that all Cu atoms were five-coordinated in a square-pyramidal configuration. They are screened for in vitro cytotoxicity against a panel of human cancer cell lines CAL-51, MDA-MB-231, HeLa, MCF-7, SGC-7901, A549, K562, and SMMC-7721. The most promising results were achieved for complexes 1 to 5 , with the IC 50 values in the range of 0.082μM to 0.69μM (against CAL-51 cell lines). The anticancer activities against CAL-51, MDA-MB-231, and MCF-7 were higher than that of Carboplatin. The mechanism studies showed that complexes 1 to 5 could inhibit proteasome activity, induce apoptosis, and inhibit cell proliferation, indicating their great potential as proteasome inhibitors for triple-negative breast cancer therapy.

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