Metal-Based Drugs最新文献

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The in vitro antitumour activity of novel, mitochondrial-interactive, gold-based lipophilic cations. 新型线粒体相互作用的金基亲脂性阳离子的体外抗肿瘤活性。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/864653
Sherika Mahepal, Richard Bowen, Messai Adenew Mamo, Marcus Layh, Constance Elizabeth Jansen van Rensburg
{"title":"The in vitro antitumour activity of novel, mitochondrial-interactive, gold-based lipophilic cations.","authors":"Sherika Mahepal,&nbsp;Richard Bowen,&nbsp;Messai Adenew Mamo,&nbsp;Marcus Layh,&nbsp;Constance Elizabeth Jansen van Rensburg","doi":"10.1155/2008/864653","DOIUrl":"https://doi.org/10.1155/2008/864653","url":null,"abstract":"<p><p>In this study we compared the effects of two previously described antimitochondrial gold complexes, that is, [A] [Au(dppe)(2)]Cl and [B] [Au(d4pype)(2)]Cl with two novel lipophilic cations, that is, [C] [Au(dpmaaH(2))(dpmaaSnMe(2))]Cl and [D] [Au(dpmaaSnMe(2))(2)]Cl as antimitochondrial agents. The results of this study indicate that [C] and [D] have intermediate partition coefficients and exhibited a selective uptake by cells. They exhibited a higher selectivity for the various cell lines than [A] but were more cytotoxic than [B]. There is a significant correlation between the cytotoxic potential of [A], [B], [C], and [D] and their octanol/water partition coefficients in both MCF-7 (breast cancer) and MCF-12A (nonmalignant breast) cells, whereas their cytotoxic potential and ability to induce the release of cytochrome c correlated only in the case of the MCF-12A cells. Complexes [C] and [D] are promising new chemotherapeutic drugs. These compounds target the mitochondrial membranes of certain cancer cells exploiting the differences between the mitochondrial membrane potential of these cells and normal cells. Although the concentrations of these compounds necessary to eradicate cancer cells are very high, the results provide a basis for the synthesis of a new family of compounds with intermediate partition coefficients compared to [A] and [B] but with increased activity against cancer cells.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":" ","pages":"864653"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/864653","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27373031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 10
Phthalocyanine-based molecularly imprinted polymers as nucleoside receptors. 酞菁基分子印迹聚合物作为核苷受体。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/281843
Luigia Longo, Giuseppe Vasapollo
{"title":"Phthalocyanine-based molecularly imprinted polymers as nucleoside receptors.","authors":"Luigia Longo,&nbsp;Giuseppe Vasapollo","doi":"10.1155/2008/281843","DOIUrl":"https://doi.org/10.1155/2008/281843","url":null,"abstract":"<p><p>A molecularly imprinted polymer (MIP) for tri-O-acetyladenosine (TOAA), PPM(TOAA), was prepared by the combined use of methacrylic acid (MAA) and Zn(II)tetra(4'-methacryloxyphenoxy) phthalocyanine as functional monomers. This MIP exhibited a higher binding ability for TOAA compared to the MIP prepared using only MAA, PM(TOAA), in batch rebinding tests. Scatchard analysis gave a higher association constant of PPM(TOAA) for TOAA (2.96x104 M-1) than that of PM(TOAA) (1.48x104 M-1). The MIP prepared using only the zinc-phthalocyanine, PP(TOAA), did not show any binding capacity for TOAA. This means that the phthalocyanine in the MIP contributes to higher affinities, although it barely interacts with TOAA. Since selectivity for this kind of MIPs is more important than binding affinity, the binding of TOAA and a structurally related compound, tri-O-acetyluridine (TOAU), on the polymers was investigated. Both PPM(TOAA) and PM(TOAA) exhibited binding affinities for TOAA while they did not show any binding capacity for TOAU.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":" ","pages":"281843"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/281843","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27276468","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 14
Nuclear Factor-kappa B as a Resistance Factor to Platinum-Based Antineoplasic Drugs. 核因子κ B对含铂类抗肿瘤药物的耐药作用。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/576104
Vilma Maldonado Lagunas, Jorge Meléndez-Zajgla
{"title":"Nuclear Factor-kappa B as a Resistance Factor to Platinum-Based Antineoplasic Drugs.","authors":"Vilma Maldonado Lagunas,&nbsp;Jorge Meléndez-Zajgla","doi":"10.1155/2008/576104","DOIUrl":"https://doi.org/10.1155/2008/576104","url":null,"abstract":"<p><p>Platinum drugs continue to be major chemotherapy drugs for cancer treatment. Nevertheless, acquired or intrinsic resistance to these compounds is common in human tumors. One important mechanism for this resistance is the avoidance of cells entering the apoptotic pathway. Nuclear factor-kappa B (NF-kappa B, NF-kappaB) is a pleiotropic transcription factor key in determining the death threshold of human cells. This factor is important in the final response of cells to platinum drugs, as exemplified by in vitro and in vivo models showing that inhibition of NF-kappaB sensitizes cancer cells to the effects of these drugs. New approaches focusing on the inhibition of NF-kappaB could help to minimize or even eliminate intrinsic or acquired resistance to platinum drugs.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"576104"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/576104","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374387","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 23
Identification of Proteins Related to Nickel Homeostasis in Helicobater pylori by Immobilized Metal Affinity Chromatography and Two-Dimensional Gel Electrophoresis. 固定化金属亲和色谱和二维凝胶电泳鉴定幽门螺杆菌中镍稳态相关蛋白。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/289490
Xuesong Sun, Ruiguang Ge, Jen-Fu Chiu, Hongzhe Sun, Qing-Yu He
{"title":"Identification of Proteins Related to Nickel Homeostasis in Helicobater pylori by Immobilized Metal Affinity Chromatography and Two-Dimensional Gel Electrophoresis.","authors":"Xuesong Sun,&nbsp;Ruiguang Ge,&nbsp;Jen-Fu Chiu,&nbsp;Hongzhe Sun,&nbsp;Qing-Yu He","doi":"10.1155/2008/289490","DOIUrl":"https://doi.org/10.1155/2008/289490","url":null,"abstract":"<p><p>Helicobacter pylori (H. pylori) is a widespread human pathogen causing peptic ulcers and chronic gastritis. Maintaining nickel homeostasis is crucial for the establishment of H. pylori infection in humans. We used immobilized-nickel affinity chromatography to isolate Ni-related proteins from H. pylori cell extracts. Two-dimensional gel electrophoresis and mass spectrometry were employed to separate and identify twenty two Ni-interacting proteins in H. pylori. These Ni-interacting proteins can be classified into several general functional categories, including cellular processes (HspA, HspB, TsaA, and NapA), enzymes (Urease, Fumarase, GuaB, Cad, PPase, and DmpI), membrane-associated proteins (OM jhp1427 and HpaA), iron storage protein (Pfr), and hypothetical proteins (HP0271, HP jhp0216, HP jhp0301, HP0721, HP0614, and HP jhp0118). The implication of these proteins in nickel homeostasis is discussed.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"289490"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/289490","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9367102","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 22
DNA Binding and Photocleavage Studies of Cobalt(III) Ethylenediamine Pyridine Complexes: [Co(en)2(py)2]3+ and [Co(en)2(mepy)2]3+. 钴(III)乙二胺吡啶配合物:[Co(en)2(py)2]3+和[Co(en)2(mepy)2]3+的DNA结合和光裂解研究。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/275084
Penumaka Nagababu, D Aravind Kumar, Kotha Laxma Reddy, K Ashwini Kumar, Md B Mustafa, Mynam Shilpa, S Satyanarayana
{"title":"DNA Binding and Photocleavage Studies of Cobalt(III) Ethylenediamine Pyridine Complexes: [Co(en)2(py)2]3+ and [Co(en)2(mepy)2]3+.","authors":"Penumaka Nagababu,&nbsp;D Aravind Kumar,&nbsp;Kotha Laxma Reddy,&nbsp;K Ashwini Kumar,&nbsp;Md B Mustafa,&nbsp;Mynam Shilpa,&nbsp;S Satyanarayana","doi":"10.1155/2008/275084","DOIUrl":"https://doi.org/10.1155/2008/275084","url":null,"abstract":"<p><p>Two novel cobalt(III) pyridine complexes (1)[Co(en)2(py)2]3+ and (2)[Co(en)2(mepy)2]3+ (en=ethylenediamine, py=pyridine, and mepy=methylpyridine) have been synthesized and characterized. The interaction of these complexes with calf thymus DNA was investigated by absorption, emission spectroscopy, viscosity measurements, DNA melting, and DNA photocleavage. Results suggest that the two complexes bind to DNA via groove mode and complex 2 binds more strongly to CT DNA than complex 1. Moreover, these Co(III) complexes have been found to promote the photocleavage of plasmid DNA pBR322 under irradiation at 365 nm, cytotoxicity results of complexes are also showing anticancer activity.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"275084"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/275084","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374512","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 16
Synthesis and Biological Analysis of Thiotetra(ethylene glycol) monomethyl Ether-Functionalized Porphyrazines: Cellular Uptake and Toxicity Studies. 硫四(乙二醇)单甲基醚功能化卟啉的合成和生物学分析:细胞摄取和毒性研究。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/391418
Sangwan Lee, Benjamin J Vesper, Hong Zong, Neal D Hammer, Kim M Elseth, Anthony G M Barrett, Brian M Hoffman, James A Radosevich
{"title":"Synthesis and Biological Analysis of Thiotetra(ethylene glycol) monomethyl Ether-Functionalized Porphyrazines: Cellular Uptake and Toxicity Studies.","authors":"Sangwan Lee,&nbsp;Benjamin J Vesper,&nbsp;Hong Zong,&nbsp;Neal D Hammer,&nbsp;Kim M Elseth,&nbsp;Anthony G M Barrett,&nbsp;Brian M Hoffman,&nbsp;James A Radosevich","doi":"10.1155/2008/391418","DOIUrl":"https://doi.org/10.1155/2008/391418","url":null,"abstract":"<p><p>The porphyrazines (pzs), a class of porphyrin analogues, are being investigated for their potential use as tumor imaging/therapeutic agents. We here examine six peripherally-functionalized M[pz(AnB4-n)] pzs with n=4, 3, or 2 (in a trans conformation) and M = H2 or Zn, where A is an [S((CH2)2O)4Me]2 unit and B is a fused beta,beta'-diisopropyloxybenzo group. Cell viability/proliferation assays and fluorescence microscopy were carried out in both tumor and normal cells. Dark toxicity studies disclosed that four of the compounds exhibited toxicity in both normal and tumor cells; one was nontoxic in both normal and tumor cells, and one was selectively toxic to normal cells. Additionally, three of the pzs showed enhanced photo-induced toxicity with these effects in some cases being observed at treatment concentrations of up to ten-fold lower than that needed for a response in Photofrin. All six compounds were preferentially absorbed by tumor cells, suggesting that they have potential as in vitro diagnostic agents and as aids in the isolation and purification of aberrant cells from pathological specimens. In particular, two promising diagnostic candidates have been identified as part of this work.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"391418"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/391418","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374514","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 17
Synthesis, structure, electrochemistry, and spectral characterization of bis-isatin thiocarbohydrazone metal complexes and their antitumor activity against ehrlich ascites carcinoma in swiss albino mice. 双isatin硫代碳腙金属配合物的合成、结构、电化学、光谱表征及其对瑞士白化小鼠埃利希腹水癌的抗肿瘤活性。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/362105
M P Sathisha, V K Revankar, K S R Pai
{"title":"Synthesis, structure, electrochemistry, and spectral characterization of bis-isatin thiocarbohydrazone metal complexes and their antitumor activity against ehrlich ascites carcinoma in swiss albino mice.","authors":"M P Sathisha,&nbsp;V K Revankar,&nbsp;K S R Pai","doi":"10.1155/2008/362105","DOIUrl":"https://doi.org/10.1155/2008/362105","url":null,"abstract":"<p><p>The synthesis, structure, electrochemistry, and biological studies of Co(II), Ni(II), Cu(II), and Zn(II) complexes of thiocarbohydrazone ligand are described. The ligand is synthesized starting from thiocarbohydrazide and isatin. It is evident from the IR data that in all the complexes, only one part of the ligand is coordinated to the metal ion resulting mononuclear complexes. The ligand coordinates essentially through the carbonyl oxygen of the isatin fragment, the nitrogen atom of the azomethine group, and sulfur atom after deprotonation to give five membered rings. H1 NMR spectrum of the ligand shows only one set of signals for the aromatic protons, while the NH of isatin and NH of hydrazone give rise to two different singlets in the 11-14 ppm range. The formulations, [Cu(L)Cl].2H2O, [Cu(L)(CH3COO)].2H2O, [Ni(L)Cl], [Ni(L)(CH3COO)], [Co(L2)], and [Zn(L2)].2H2O are in accordance with elemental analyses, physical, and spectroscopic measurements. The complexes are soluble in organic solvents. Molar conductance values in DMF indicate the nonelectrolytic nature of the complexes. Copper complex displays quasireversible cyclic voltametric responses with Ep near -0.659 v and 0.504 v Vs Ag/AgCl at the scan rate of 0.1 V/s. Copper(II) complexes show a single line EPR signals. For the observed magnetic moment and electronic spectral data possible explanation has been discussed. From all the available data, the probable structures for the complexes have been proposed. The compounds synthesized in present study have shown promising cytotoxic activity when screened using the in vitro method and at the same time were shown to have good activity when tested using the Ehrlich ascites carcinoma (EAC) model. The antimicrobial screening showed that the cobalt complex possesses enhanced antimicrobial activity towards fungi.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"362105"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/362105","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9367109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 68
Kinetic and high-pressure mechanistic investigation of the aqua substitution in the trans-aquaoxotetracyano complexes of re(v) and tc(v): some implications for nuclear medicine. re(v)和tc(v)的反水氧四氰配合物中水取代的动力学和高压机理研究:对核医学的一些启示。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/745989
J Mattheus Botha, Andreas Roodt
{"title":"Kinetic and high-pressure mechanistic investigation of the aqua substitution in the trans-aquaoxotetracyano complexes of re(v) and tc(v): some implications for nuclear medicine.","authors":"J Mattheus Botha,&nbsp;Andreas Roodt","doi":"10.1155/2008/745989","DOIUrl":"https://doi.org/10.1155/2008/745989","url":null,"abstract":"<p><p>A kinetic study of the aqua substitution in the [TcO(OH(2))(CN)(4)](-) complex by different thiourea ligands (TU = thiourea, NMTU = N-methyl thiourea, NNDMTU = N, N'-dimethylthiourea) yielded second-order formation rate constants (25 degrees C) as follows [NNDMTU, NMTU, TU, respectively]: k(f) = 11.5 +/- 0.1, 11.38 +/- 0.04, and 7.4 +/- 0.1 M(-1)s(-1), with activation parameters: Delta H(#) (k(f) ) : 55 +/- 2, 42 +/- 3, 35 +/- 5 kJ mol(-1); DeltaS(#) (k(f) ) : - 40 +/- 8, - 84 +/- 11, - 110 +/- 17 J K(-1)mol(-1). A subsequent high-pressure investigation of the aqua substitution in the [ReO(OH(2))(CN)(4)](-) and [TcO(OH(2))(CN)(4)](-) complexes by selected entering ligands yielded DeltaV(#) (k(f) ) values as follows: Re(V): -1.7 +/- 0.3(NCS(-)), -22.1 +/- 0.9 (TU) and for Tc(V): -3.5 +/- 0.3(NCS(-)), -14 +/- 1 (NNDMTU), and -6.0 +/- 0.5 (TU) cm(3)mol (-1), respectively. These results point to an interchange associative mechanism for the negative NCS(-) as entering group but even a pure associative mechanism for the neutral thiourea ligands.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"745989"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/745989","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374388","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
Synthesis, structural, and biological studies of some schiff bases and their metal complexes. 一些席夫碱及其金属配合物的合成、结构和生物学研究。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/875410
A P Mishra, Monika Soni
{"title":"Synthesis, structural, and biological studies of some schiff bases and their metal complexes.","authors":"A P Mishra,&nbsp;Monika Soni","doi":"10.1155/2008/875410","DOIUrl":"https://doi.org/10.1155/2008/875410","url":null,"abstract":"<p><p>New bidentate or tridentate Schiff bases and their VO(II) and Co(II) complexes formed by the condensation of methyl isobutyl ketone with nicotinamide (mna)/2-amino-4-chlorophenol (map) and 2-hydroxy acetophenone with nicotinamide (han)/isoniazide (hai). Physicochemical characterization has been carried out to determine the structure of the complexes. The FAB mass and thermal data show degradation pattern of the complexes. XRD analysis reveals that all the studied complexes crystallize as tetragonal crystal system. Some of the complexes have been screened for their antimicrobial activity by the well diffusion technique using DMSO as solvent on different species of pathogenic bacteria/fungi, that is, E. coli, S. aureus, S. fecalis, A. niger, T. polysporum, and their antimicrobial potency have been discussed. It has been found that all the complexes are antimicrobially active and show higher activity than the free ligand. Metal chelation affects significantly the antimicrobial/bioactive behavior of the organic ligands.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"875410"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/875410","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374394","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 62
Synthesis and cytotoxicity studies of titanocene C analogues. 二茂钛C类似物的合成及细胞毒性研究。
Metal-Based Drugs Pub Date : 2008-01-01 DOI: 10.1155/2008/754358
Megan Hogan, James Claffey, Eoin Fitzpatrick, Thomas Hickey, Clara Pampillón, Matthias Tacke
{"title":"Synthesis and cytotoxicity studies of titanocene C analogues.","authors":"Megan Hogan,&nbsp;James Claffey,&nbsp;Eoin Fitzpatrick,&nbsp;Thomas Hickey,&nbsp;Clara Pampillón,&nbsp;Matthias Tacke","doi":"10.1155/2008/754358","DOIUrl":"https://doi.org/10.1155/2008/754358","url":null,"abstract":"<p><p>From the carbolithiation of 6-N,N-dimethylamino fulvene (3) and 2,4[bis(N,N-dimethylamino)methyl]-N-methylpyrrolyl lithium (2a), N-(N',N'-dimethylaminomethyl)benzimidazolyl lithium (2b), or p-(N,N-dimethylamino)methylphenyl lithium (2c), the corresponding lithium cyclopentadienide intermediate (4a-c) was formed. These three lithiated intermediates underwent a transmetallation reaction with TiCl(4') resulting in N,N-dimethylamino-functionalised titanocenes 5a-c. When these titanocenes were tested against a pig kidney epithelial cell line (LLC-PK), the IC50 values obtained were of 23, and 52 muM for titanocenes 5a and 5b, respectively. The most cytotoxic titanocene in this paper, 5c with an IC50 value of 13 muM, was found to be approximately two times less cytotoxic than its analogue Titanocene C (IC50=5.5 muM) and almost four times less cytotoxic than cisplatin, which showed an IC50 value of 3.3 muM when tested on the LLC-PK cell line.</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"2008 ","pages":"754358"},"PeriodicalIF":0.0,"publicationDate":"2008-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/2008/754358","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374513","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 6
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