作者: Gui-Bin Liang , Yan-Cheng Yu , Jian-Hua Wei , Wen-Bin Kuang , Zhen-Feng Chen
DOI: 10.1016/J.EJMECH.2019.112033
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摘要: Abstract A serial of naphthalenebenzimidizole-Pt complexes 1–6 were designed and synthesized as antitumor agents. In vitro assay results showed that exhibited moderate to high antiproliferative activity against Hela, HepG2, SKOV-3, NCI–H460, BEL-7404 A549 cancer cell lines, while they displayed obvious sensitivity selectivity SMMC-7721 U251 cell lines low toxicity normal HL-7702 cells, in comparison with cisplatin. In vivo indicated complex 1 5 important in vivo the NCI-460 models, cisplatin, respectively. Complexes better A549CDDP SKOV3CDDP than IC50 values 6.98 ± 0.47 μM, 5.62 ± 0.88 μM 13.13 ± 2.11 μM, 5.30 ± 0.33 μM, respectively, potential antiproliferation SKOV3 7.32 ± 0.51 μM, 5.19 ± 0.49 μM 14.92 ± 0.11 μM, 12.19 ± 0.92 μM, indicating introduction naphthalenebenzimidizole into platinum-metal system may overcome resistance. Mechanistic studies representative exerted effect mainly by covalent binding DNA upregulation expression level intracellular topo I, showing different action mechanism from