稀土三元配合物的合成、表征及其抗菌活性研究

以稀土氯化物、联咪唑和噻吩甲酰三氟丙酮为原料制备了一系列新型稀土三元配合物Ln(TTA)3L(Ln=Nd3+,Eu3+,Er3+;TTA=噻吩甲酰三氟丙酮;L=联咪唑),抗菌实验结果显示,三元配合物抑菌圈直径为12～17 mm,对大肠杆菌、金黄色葡萄球菌具有一定的抑制作用,且对大肠杆菌的抑制效果较好。     

钇三元配合物的合成、表征及其抗菌活性研究

以YCl3.6H2O、2,6-吡啶二羧酸(PDA)和噻吩甲酰三氟丙酮(TTA)为原料,制备了钇的三元配合物,用元素分析、红外光谱、X射线光电子能谱对配合物进行了表征,确定了配合物的化学组成为:Na[Y(TTA)2(PDA)].3H2O(反应时间为1 h)和Na2[Y(TTA)3(PDA)].3H2O(反应时间为0.5 h)。抗菌实验表明,Na[Y(TTA)2(PDA)].3H2O对大肠杆菌和金黄色葡萄球菌的抑菌圈直径分别约为14,12 mm,Na2[Y(TTA)3(PDA)].3H2O分别约为16,14 mm,说明配合物对大肠杆菌、金黄色葡萄球菌具有一定的抑制作用,且对大肠杆菌的抑制效果较好。     

水杨醛缩丙氨酸Schiff碱氧钒-多吡啶三元混配配合物的合成及表征

本文合成了三个水杨醛缩丙氨酸Schiff碱氧钒-多吡啶二三元混配配合物,通过EA、IR、UV、EPR、熔点等技术对其进行了分析和表征,并推测其可能的结构式。     

安息香缩氨基硫脲及其配合物的合成,表征和生物活性研究

合成了安息香缩氨基硫脲及其与Ｃｕ（Ⅱ），Ｍｎ（Ⅱ），Ｚｎ（Ⅱ），Ｎｉ（Ⅱ），Ｃｏ（Ⅱ）的配合物，通过元素分析，摩尔电导率，磁化率，紫外光谱和红外光谱等进行了表征。测定了配体及配合物的生物活性。实验发现，配体无抗菌活性，形成配合物后具有抗菌活性。     

Metal complexes of Taxol precursor: 1. Synthesis,characterization and antitumor activity of the copper complex of 10-deacetylbaccatin thiosemicarbazone

Incorporation of the thiosemicarbazone pharmacophore in the otherwise inactive baccatin nucleus, viz. 10-deacetylbaccatin (10-DAB), on complexation with copper renders a highly antiproliferative compound Cu-DABTSC. When tested on a human breast cancer cell line, MCF-7, it was observed that 10-DAB treated cells were growth arrested but viable whereas Cu-DABTSC was lethal to cells at comparative doses.     

缩聚活性的铽配合物合成、表征及其性质

通过HCl气体在无水乙醇中,与Tb4O7反应生成无水TbCl3,再与具有胺基的配体反应,合成了一种两端带有胺基的呈缩聚活性的铽配合物。用元素分析、红外光谱和紫外光谱对配合物的组成和结构进行了表征,并借摩尔电导、差热-热重和荧光光谱对配合物进行了研究。配合物的起始分解温度为230℃左右,粉末状态下具有较高的荧光强度,单色性好,在DMF中可作为聚合单体应用。     

席夫碱稀土铈配合物的合成、表征及抗菌活性

利用四乙酰丙酮铈配合物[Ce（acac）4]和Salphen型水杨醛缩邻苯二胺（Schiff碱）合成了双齿Salphen型席夫碱铈金属配合物（SB-Ce）,用红外光谱（FTIR）、紫外-可见光谱（UV-Vis）和差热-热重（TG-DTA）分析进行结构表征,将SB-Ce配合物用于抑菌活性实验。结果表明,SB-Ce对大肠杆菌、枯草杆菌、金黄色葡萄球菌和酵母菌都有一定的抑菌活性,其中对金黄色葡萄球菌的抑菌性最好。     

Antimicrobial and nuclease activity of mixed polypyridyl ruthenium(II) complexes

The ruthenium(II) complexes with 2,9-dimethyl-1,10-phenanthroline (dmphen) and terpyridine derivatives have been synthesized and screened for their antimicrobial potency. The interaction of these complexes with Herring Sperm DNA was investigated by thermal denaturation, viscosity measurements, gel electrophoresis and spectrophotometric methods. The results indicate that the complexes bound to DNA via partial intercalative mode. The salt-dependent binding of these complexes has been determined by UV–Vis spectrophotometric titration. The contribution of the non-electrostatic binding free energy (ΔG_t^o) to the total binding free energy change (ΔG^o) is found to be ~ 88% at [Na⁺] = 0.075 M. The large value suggests that the stabilization of the DNA binding is mostly due to the contribution of non-electrostatic process.     

新型三硅氧烷表面活性剂的合成与表征

合成了一种新型的三硅氧烷表面活性剂Me3SiOSiMeROSiMe3[R=(CH2)3NHCH2CH(OH)CH2(OCH2CH2)xOCH3,x=1,2]。通过低聚乙二醇单甲醚和环氧氯丙烷在相转移催化剂(P.T.C)的存在下合成出低聚乙二醇甲醚缩水甘油醚,产物再与氨丙基三硅氧烷进行开环反应,得到目标产物。通过气相色谱(GC)和氢核磁共振(1HNMR)确定了目标产物的纯度与结构。     

稀土-蛋氨酸-邻菲咯啉配合物的合成、表征及抗菌活性研究

采用冷凝回流法合成了4种新型稀土(镧、铕、钐和钕)-蛋氨酸-邻菲咯啉三元配合物,通过元素分析、EDTA-滴定、摩尔电导、红外光谱,确定了配合物的组成为RE(Met)_3phenCl_3·3H_2O(RE:La~(3+)、Eu~(3+)、Sm~(3+)、Nd~(3+);Met=L-蛋氨酸;phen=邻菲咯啉).抗菌活性的研究表明,与配体相比,稀土三元配合物对大肠杆菌(Escherichia coli)和金黄色葡萄球菌(Staphylococcus aureus)均具有更强的抑菌能力.     

Synthesis, characterization and antitumour activity of metal complexes of 5-carboxy-2-thiouracil

Metal complexes of 5-carboxy-2-thiouracil with Mn(ll), Co(ll), Ni(ll), Cu(ll), Zn(ll) and Cd(ll) ions were synthesized, characterized, and subjected to a screening system for evaluation of antitumour activity against Sarcoma-180 (S-180) tumour cells. The complexes were characterized by elemental analysis, infrared, electronic spectra, room temperature magnetic measurements and powder X-ray diffraction. The antitumour activity results indicate that some complexes have antitumour activity both in vivo and in vitro against S-180 tumour cells.     

Synthesis and antitumor activity of N

摘要：以STX-0119为先导化合物基于生物电子等排原理设计并合成25个N"-苯亚甲基-2-(3-吡啶基)喹啉-4-酰肼衍生物（产率：20.4-42.6%），通过1H NMR、MS、13C NMR确证了产物结构，采用MTT和台盼蓝法以以人乳腺癌MCF-7细胞、人肺癌A549细胞、人慢性粒细胞白血病K562细胞、人急性B淋巴细胞白血病RS4:11细胞为测试细胞株评价了目标化合物的体外抗肿瘤活性。目标化合物Ⅶr表现出最强的抗A549细胞增殖活性（IC50 = 7.42 ± 0.83 μmol/L），目标化合物Ⅶq表现出最强的抗RS4:11细胞增殖活性（IC50 = 2.4 ± 0.17 μmol/L）目标化合物Ⅶl不仅表现出最强的抗MCF-7细胞增殖活性（IC50 = 4.91 ± 0.33 μmol/L），而且也表现出最强抗K562细胞增殖活性（IC50 = 1.24 ± 0.19 μmol/L），分子对接结果显示其发挥抗肿瘤的作用可能与STAT3通路有关，值得进一步深入研究。 关键词：喹啉；酰肼；合成；抗肿瘤；生物电子等排     

一种吡嗪基三唑配合物的合成与表征

利用水热法,基于3-(3-氧苯基)-5-(2-吡嗪基)-1,2,4-三唑(opt)和硝酸镍合成一种新型配位聚合物[Ni(opt)2(H2O)2]n。通过X射线单晶衍射、热重分析、红外光谱和元素分析对该配合物进行了表征,并分析了其光谱及结构特征。晶体结构分析表明,该配合物属于单斜晶系、P21/n空间群。其中,a=0.849 54(16)nm,b=0.729 95(7)nm,c=1.831 3(2)nm,α=90.00°,β=93.412(12)°,γ=90.00°,V=1.133 6(3)nm3,Z=2。中心金属镍原子分别与2个opt中的4个氮原子和2个水分子的氧原子配位,形成六配位的变形八面体构型。     

Pro-oxidant activity of nickel (II) pyridoxal complexes. Synthesis,characterization and peroxidase activity assays

The synthesis of Ni (II) complexes with pro-oxidant applications has demonstrated many advantages, such as accelerated reactions, solution stability and with high selectivity reactions. In this work we describe the synthesis, characterization and structural analysis of nickel ([(Ni)(C₃₀H₂₈N₄O₄S₂)]);([(Ni)(C₃₁H₃₀N₄O₄S₂)]) and ([(Ni)(C₃₃H₃₇N₄O₄S₂)]·DMF — complex 3) complexes with ligands obtained from the condensation of pyridoxal and aryl-thiol amines and their application as a pro-oxidant in the reaction of the phenol-aminoantipyrine adduct. The complexes show variation in carbon spacers between pyridoxal molecules: ethane, propane and butane. It was found that the spacer two carbons containing the most significant as the pro-oxidant activity.     

Unexpected cis-dioxido uranyl carboxylate compound: Synthesis,characterization and photocatalytic activity of uranyl-succinate complexes

Two new complexes formed by uranyl ions with succinic acid and 4,4′-dipyridine have been investigated. Interestingly, the uranium(VI) coordination polymers possess two types dioxido unit, a cis-dioxido bond angle with 115.421(2)°and a trans-dioxido bond angle with 178.421(2)°, respectively. The complexes were characterized by elemental analysis, IR and UV–vis spectroscopy and X-ray crystal diffraction. In addition, the properties of luminescence and photocatalytic analysis were also investigated. The result revealed that the two complexes show different photocatalytic activity in the decomposition of RhB under visible light and UV light irradiation.     

Hormone anchored metal complexes. 1. Synthesis, structure, spectroscopy and in vitro antitumor activity of testosterone acetate thiosemicarbazone and its metal complexes

Testosterone acetate thiosemicarbazone (TATSC, 17-beta-hydroxyandrost-4-one acetate thiosemicarbazone) was synthesized and characterized by single crystal X-ray structure determination. The copper and platinum complexes of this steroid derivative were synthesized and characterized by spectroscopy and electrochemiatry. The in vitro activity of these compounds against human breast cancer cell line MCF-7 was tested. The highest activity was found for the [Pt(TATSC)Cl(1)] followed by [Cu(TATSC)Cl(2)] and the ligand in compariosn with cisplatin.     

噻二唑硫醚双腙的合成及抗肿瘤活性

为研究杂环双腙类化合物的合成方法和抗肿瘤活性,用2-巯基-5-苯基-1,3,4-噻二唑与β-氯苯丙酮取代后与水合肼缩合得相应的单腙,然后再与芳香醛缩合得双腙目标物.7个新目标物的结构经元素分析和光谱数据确证,并用MTT实验法评价了它们的体外抗肿瘤活性.初步的药理结果表明,部分目标物对CHO、HL60、L1210 3种癌细胞株具有潜在的体外生长抑制活性.     

Novel bioactive copper and nickel polymeric complexes: Synthesis,characterization, antimicrobial activity,and DFT calculations

Polymeric complexes, especially metal-containing polymers, possess aggregated medical applications, especially as antibacterial and antifungal agents. This work describes a facile procedure for producing a series of novel copper and nickel complexes of poly(2-hydroxyphenyl methacrylamide) and poly(2-carboxyphenyl methacrylamide). The polymeric ligands were synthesized through a multistep procedure. Firstly, 4-formylphenyl methacrylate was constructed by acylating 4-hydroxybenzaldehyde with methacryloyl chloride. Then, polymerization of the as-prepared monomer to obtain poly(4-formylphenyl methacrylate) using benzoyl peroxide as an initiator. Thirdly, the polymeric ligands PL1 and PL2 were achieved via exchange reactions between poly(4-formylphenyl methacrylate) and o-aminophenol and anthranilic acid, respectively. Consequently, the two ligands were reacted with copper and nickel acetates to afford four target complexes (Cu-PL1, Ni-PL1, Cu-PL2, and Ni-PL2). By FT-IR, ¹HNMR, UV-visible, and TGA analyses, the structures of PL1, PL2, and their complexes were investigated. Furthermore, the geometries of PL1, PL2, and their complexes were reported through a molecular modeling to investigate some interesting parameters such as the bond length, bond angle, charge on the atoms, the HOMO and LUMO using the Material Studio program. The calculation results illustrated that octahedral geometries are proposed for the synthesized metal complexes. The reported antimicrobial efficiency showed a strong potency for most synthesized compounds against the selected microbes, especially compounds Cu-PL1 and Cu-PL2 which are more effective than the standard against Candida albicans.     

一种新型缩氨基硫脲及其金属配合物的合成、表征与生物活性研究

合成了1-(2-羟基-1-亚甲基)-4-苯基氨基硫脲配体(HL)及它们的铜、钴、镍金属配合物,通过核磁、元素分析、摩尔电导、红外光谱、紫外-可见光谱等测试对其进行了结构表征,并测试了该配体及其金属配合物对大肠杆菌、金黄色葡萄球菌、欧文氏草生杆菌的抑菌活性。     

Synthesis,characterization and sulfide oxidation activity of vanadyl Schiff base complexes anchored on MCM-41

Vanadyl Schiff base complexes covalently attached on the surface of MCM-41 have been synthesized by anchoring Schiff base and subsequent reaction with VO(acac)₂. XRD, nitrogen adsorption and desorption, UV-visible spectroscopy and FT-IR show that vanadyl Schiff base complexes were successfully anchored on the surface of MCM-41 and the mesopore ordering decreased after the anchoring. The so-prepared heterogeneous catalysts have showed high activity for sulfide oxidation.