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作 者:吴静 惠朴真 郑慧林 袁平川 汪春飞 王慧 谷晓霞[1,2] WU Jing;HUI Puzhen;ZHENG Huilin;YUAN Pingchuan;WANG Chunfei;WANG Hui;GU Xiaoxia(College of Pharmacy,Wannan Medical College,Wuhu,Anhui 241002,China;Institute of Synthesis and Application of Medical Materials,Wannan Medical College,Wuhu,Anhui 241002,China)
机构地区:[1]皖南医学院药学院,芜湖241002 [2]皖南医学院医用材料合成应用研究所,芜湖241002
出 处:《无机化学学报》2024年第12期2422-2428,共7页Chinese Journal of Inorganic Chemistry
基 金:安徽省高校自然科学研究项目(No.2024AH051920,2023AH051762);国家级大学生创新创业训练计划项目(No.202310368050)资助。
摘 要: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。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 cisplatin.Among them,complex 1 had the highest inhibitory effects on tumor cells with its IC_(50) value(half‑inhibitory concentration)being(4.8±0.2)μmol·L^(-1) against MGC‑803 cells.These demonstrated a potential anti‑cancer candidate 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 concentration of complex 1.CCDC:2354708,2;2354849,3.
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