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申请号:202010111354.9 公开号:CN111217861A 主分类号:C07F17/02
申请人:【中文】曲阜师范大学【EN】QUFU NORMAL University 申请日:2020.02.24 公开日:2020.06.02
摘要:【中文】本发明公开了一种铁–铱异核金属配合物及其制备方法和应用。其结构式如式(I)所示,R为氢、烷基和芳基。通过测试目标配合物对人类肺泡基底上皮癌细胞(A549)和子宫颈癌细胞(Hela)生长的抑制率实验,并与二茂铁联吡啶衍生物、金属铱二聚体,基础金属铱联吡啶配合物及顺铂对比,目标配合物均具有良好的抗癌活性,特别是顺式构型的配合物,证实了二茂铁与金属铱配合物的协同抗癌效果。取代基R由甲基→苯基,配合物的活性提升,证实了提高配体的供电子能力对提升目标配合物抗癌活性的协同作用。目标配合物可以在细胞内的溶酶体内积累,并导致溶酶体损伤,从而导致癌细胞凋亡。 【EN】The invention discloses an iron-iridium heteronuclear metal complex and a preparation method and application thereof. The structural formula is shown as a formula (I), and R is hydrogen, alkyl and aryl. Through testing the inhibition rate experiments of the target complex on the growth of human alveolar basement epithelial cancer cells (A549) and cervical cancer cells (Hela), and comparing the inhibition rate experiments with ferrocene bipyridyl derivatives, metal iridium dimers, basic metal iridium bipyridyl complexes and cisplatin, the target complex has good anticancer activity, and particularly the complex with cis-configuration proves the synergistic anticancer effect of ferrocene and the metal iridium complexes. The substituent R is methyl → phenyl, and the activity of the complex is improved, so that the synergistic effect of improving the electron supply capability of the ligand on improving the anticancer activity of the target complex is proved. The target complex may accumulate in intracellular lysosomes and cause lysosomal damage, leading to apoptosis of cancer cells.
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申请号:202010111378.4 公开号:CN111217732A 主分类号:C07C335/40
申请人:【中文】曲阜师范大学【EN】QUFU NORMAL University 申请日:2020.02.24 公开日:2020.06.02
摘要:【中文】本发明公开了一种具有溶酶体靶向的荧光型金属铱双聚体及其制备方法和应用。其结构式如式(I)所示,R为氢、烷基和芳基。通过测试目标化合物(1~4)对人类肺泡基底上皮肿瘤细胞(A549)和子宫颈肿瘤细胞(Hela)生长的抑制率实验,并与硫代氨基脲–三苯胺席夫碱类配体、基础金属铱二聚体及顺铂对比,表明目标化合物均具有良好的抗肿瘤活性。另外,取代基R由氢→烷基→芳基,目标化合物的活性有所提升。三苯胺的引入及化合物特殊的结构赋予化合物良好的荧光特性,其可以在细胞内的溶酶体内积累,并导致溶酶体损伤,从而导致肿瘤细胞凋亡。 【EN】The invention discloses a fluorescent metal iridium dimer with lysosome targeting, and a preparation method and application thereof. The structural formula is shown as a formula (I), and R is hydrogen, alkyl and aryl. The target compound (1-4) has good anti-tumor activity through the experiment of the inhibition rate of the target compound on the growth of human alveolar basal epithelial tumor cells (A549) and cervical tumor cells (Hela) and the comparison with a thiosemicarbazide-triphenylamine Schiff base ligand, a basic metal iridium dimer and cisplatin. In addition, the substituent R is hydrogen → alkyl → aryl, the activity of the target compound is enhanced. The introduction of triphenylamine and the special structure of the compound endow the compound with good fluorescence property, the triphenylamine can be accumulated in lysosomes in cells and cause lysosomal damage, thereby causing tumor cellsAnd (4) apoptosis.
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