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萘酚醛席夫碱过渡金属配合物的合成、晶体结构及抗肿瘤活性

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合成了 3种萘酚醛缩色胺席夫碱过渡金属配合物[Cu(L)2(DMF)2](1)、[Ni(L)2(DMF)2](2)和[Zn(L)2](3),其中HL=N-[(2-hydroxy-1-naphthalenyl)methylene]-[(1H-indol-3-yl)ethyl]imine。利用红外光谱、元素分析和单晶X射线衍射等测试手段对配合物1~3进行了结构表征。采用MTT法对该系列配合物进行了体外抗肿瘤活性初筛,结果表明配合物1~3对人胃癌细胞MGC-803、人非小细胞肺癌细胞A549和人乳腺癌细胞MDA-MB-231都有较好的抑制作用。通过流式细胞术检测配合物1诱导肿瘤细胞凋亡的情况,结果显示配合物1诱导MGC-803细胞发生晚期凋亡;随后,细胞刮板实验表明随着配合物1浓度的增加,其对MGC-803细胞的杀伤作用增强,且杀伤作用呈剂量依赖性。
Synthesis,crystal structures,and antitumor activities of transition metal complexes incorporating a naphthol-aldehyde Schiff base ligand
To study the synthesis and antitumor activities of the transition metal complexes incorporating a novel naphthol-aldehyde Schiff base ligand,three transition metal complexes[Cu(L)2(DMF)2](1),[Ni(L)2(DMF)2](2),and[Zn(L)2](3)were synthesized using a Schiff base of N-[(2-hydroxy-1-naphthalenyl)methylene]-[(1H-indol-3-yl)ethyl]imine(HL)by liquid diffusion method.The complexes 1-3 were characterized by IR analysis,elemental analysis,and single-crystal X-ray diffraction.Moreover,their antitumor activities in vitro were screened through three human cancer cell lines(MGC-803,A549,MDA-MB-231)by the MTT assay.It revealed that complexes 1-3 showed high antitumor activities.Complex 1 showed much higher antitumor activities than complexes 2 and 3,and even than cis-platin.Among them,complex 1 had the highest inhibitory effects on tumor cells with its IC50 value(half-inhibitory concentration)being(4.8±0.2)μmol·L-1 against MGC-803 cells.These demonstrated a potential anti-cancer candi-date for complex 1,which induced MGC-803 cancer cells'late apoptosis by flow cytometry.Subsequently,the cell scraper experiment showed that the killing effect of MGC-803 cells was enhanced with the increase in the concentra-tion of complex 1.CCDC:2354708,2;2354849,3.

naphthol-aldehyde Schiff basetransition metal complexsynthesiscrystal structureantitumor activity

吴静、惠朴真、郑慧林、袁平川、汪春飞、王慧、谷晓霞

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皖南医学院药学院,芜湖 241002

皖南医学院医用材料合成应用研究所,芜湖 241002

萘酚醛席夫碱 过渡金属配合物 合成 晶体结构 抗肿瘤活性

2024

无机化学学报
中国化学会

无机化学学报

CSTPCD北大核心
影响因子:0.665
ISSN:1001-4861
年,卷(期):2024.40(12)