scholarly journals X-Ray Structure and In Vitro Anti-Tumoural Activity of the Dimeric Bis[(2-Phenyl-1,2-Dicarba-Closo-Dodecaborane-1-Carboxylato)-Di-n-Butyltin] Oxide

1997 ◽  
Vol 4 (2) ◽  
pp. 75-80 ◽  
Author(s):  
Edward R. T. Tiekink ◽  
Marcel Gielen ◽  
Abdeslam Bouhdid ◽  
Rudolph Willem ◽  
Vladimir I. Bregadze ◽  
...  
Keyword(s):  
Cell Lines ◽  
Carboxylate Ligand ◽  
X Ray Diffraction ◽  
X Ray ◽  
Anti Tumour Activity ◽  
Common Motif ◽  
The Common ◽  
Tumour Activity ◽  
Oxygen Atoms

X-ray diffraction studies reveal the structure of {[(2-C6H5-1,2-C2B10H10-1-COO)Bu2Sn]2O}2, 1, to conform to the common motif found for {[(R′COO)R2Sn]2O}2 compounds. The dimer features a central Bu4Sn2O2 unit (two-fold symmetry) with the two Bu2Sn groups being linked via bridging oxygen atoms, each of which also carries an exocyclic Bu2Sn moiety. The two pairs of exo- and endo-cyclic tin atoms are each linked via an almost symmetrically bridging carboxylate ligand and the two remaining ligands coordinate an exocyclic tin atom only, in the monodentate mode. The in vitro anti-tumour activity of 1, determined against a variety of cell lines, is compared with those of the corresponding 2-methylcarboranylacetate, derivative 2, and with clinically used compounds.

scholarly journals Preparation and Anti-Tumour Activity of Some Arylbismuth(III) Oxine Complexes

1998 ◽  
Vol 5 (5) ◽  
pp. 295-304 ◽  
Author(s):  
Katharine A. Smith ◽  
Glen B. Deacon ◽  
W. Roy Jackson ◽  
Edward R. T. Tiekink ◽  
Silvina Rainone ◽  
...  
Keyword(s):  
Phenyl Group ◽  
Significant Activity ◽  
X Ray ◽  
Crystallographic Study ◽  
Anti Tumour Activity ◽  
In Vivo Testing ◽  
Tumour Activity ◽  
Better Than

New arylbismuth(lll) oxinates, PhBi(MeOx)2, (p-MeC6H4)Bi(Ox)2, (p-MeC6H4)Bi(MeOx)2, (p-ClC6H4)Bi(Ox)2, and (p-ClC6H4)Bi(MeOx)2 (Ox− = quinolin-8-olate and MeOx−=2-methylquinolin-8-olate) have been prepared by reaction of the appropriate diarylbismuth chlorides with Na(Ox) or Na(MeOx) in the presence of 15-crown-5. An X-ray crystallographic study has shown PhBi(MeOx)2 to be a five coordinate monomer with distorted square pyramidal stereochemistry. Chelating MeOx ligands have a cisoid arrangement in the square plane and the phenyl group is apical. The lattice is stabilised by significant π-π interactions between centrosymmetric molecules. A range of these complexes has been shown to have high in vitro biological activity (comparable with or better than cisplatin) against L1210 leukaemia, the corresponding cisplatin resistant line, and a human ovarian cell line, SKOV-3. However, initial in vivo testing against a solid mouse plasmacytoma (PC6) and P388 leukaemia has not revealed significant activity.

scholarly journals Synthesis, Structure of Nitrogen-Containing Phosphinogold(I) Ferrocenes. In vitro Activity against Bladder and Colon Carcinoma Cell Lines

1995 ◽  
Vol 2 (6) ◽  
pp. 311-326 ◽  
Author(s):  
Manuella Viotte ◽  
Bernard Gautheron ◽  
Marek M. Kubicki ◽  
Ilya E. Nifant'ev ◽  
Simon P. Fricker
Keyword(s):  
Carcinoma Cell ◽  
In Vitro Activity ◽  
X Ray ◽  
Carcinoma Cell Lines ◽  
Anti Tumour Activity ◽  
Tetramethylammonium Bromide ◽  
Tumour Activity ◽  
Nitrogen Phosphorus ◽  
Good Agreement

The gold salt [(tht)AuCl] was reacted with [1-N,N-dimethylaminométhyl-2-diphenylphosphino]ferrocene (1) forming the bimetallic derivative 4. The reaction of methyl iodide and tetramethylammonium bromide on the chloride 4 produced the ammonium salt 5 and the bromide 6 respectively. New aminophosphines 2 and 3, which represent two of the rare phosphorylated metallocenes containing P(III)-N bond have also been coordinated to gold(I) to form 7 and 8. The presence of the ethoxy group in 7 provides evidence for the lability of one nitrogen-phosphorus bond. The X-ray structure of compounds 4 and 7 have been established. Both crystallize in space group P21/c, monoclinic, with a = 11.095(2) Å, b = 12.030(3) Å, c = 17.763(4) Å, β= 94.02(2)∘, Z = 4 for 4 and a = 14.863(3) Å, b = 8.036(5)Å, c = 18.062(5)Å, β =101.64(1)°, Z = 4 for 7. A197u Mössbauer data are in good agreement with those for other linear P-Au-Cl containing complexes. The compounds were evaluated for in vitro anti-tumour activity against two human tumours. Differential cytotoxicity was observed with activity comparable to cisplatin, with the exception of one compound which was significantly more cytotoxic.

A Novel Heat Shock Protein (HSP) 90 Inhibitor KW-2478 shows Activity in B-Cell Malignancies in Vitro and in Vivo.

Blood ◽  
2008 ◽  
Vol 112 (11) ◽  
pp. 1625-1625
Author(s):  
Simone Juliger ◽  
Takayuki Nakashima ◽  
Lenushka Maharaj ◽  
Toshihiko Ishii ◽  
Hiroshi Nakagawa ◽  
...  
Keyword(s):  
Cell Growth ◽  
B Cell ◽  
Cell Lines ◽  
Cell Lymphoma ◽  
Hsp90 Inhibitor ◽  
Anti Tumour Activity ◽  
Client Proteins ◽  
Tumour Activity

Abstract Background : HSP90 plays an important role in chaperoning key proteins implicated in malignant disease and is a promising therapeutic target. We now report the in vitro and in vivo activity of a novel HSP90 inhibitor of non-ansamycin, non-purine analogue class, KW-2478, (Kyowa Hakko Kirin) in B-cell malignancies including multiple myeloma (MM), B-cell lymphoma (BCL) and mantle cell lymphoma (MCL) cells, and in primary tumour cells from MM and BCL patients. Procedures: The binding affinity of KW-2478 to HSP90 was examined using immobilised human HSP90a and a biotinylated HSP90 binding agent, radicicol (bRD). The effect of KW-2478 on cell viability, cell growth and apoptosis induction were evaluated in cell lines, with KW-2478 induced changes in major HSP90 client proteins studied by Western blotting analysis. The in vivo anti-tumour activity of KW-2478 was evaluated in a human MM xenograft mouse model,. Primary MM cells were studied using a co-culture system with the HS-5 bone marrow stromal cell line (BMSCs), while primary BCL samples were cultured on CHO cells stably transfected to produce CD40L. Results: KW-2478 inhibited the binding of bRD to HSP90α in concentration-dependent manner with an IC50 value of 3.8 nM. KW-2478 clearly inhibited cancer cell growth in all cell lines, with EC50 values from 101–252 nM in BCL, 81.4–91.4 nM in MCL and 120–622 nM in MM. The drug also exhibited potent growth inhibitory activity in primary CLL (n=3) and NHL (n=2) cells with EC50 values of 40–170 nM and 200–400 nM, respectively. In 2 of 4 human primary myeloma cells, KW-2478 at 2 μM inhibited cell growth by at least 50%. The presence of BMSCs did not affect drug activity against primary MM cells and importantly there was little or no effect on cell number or viability of normal BMSCs at up to 20 μM KW-2478. Exposure of MM and BCL cell lines to KW-2478 for 24 hours resulted in the degradation of HSP90 client proteins (IGF-1Rβ and Raf-1) and the induction of HSP70. KW-2478 also induced PARP cleavage and dephosphorylated Erk1/2 in NCI-H929 cells. Further studies in selected cell lines showed that exposure to 1 μM KW-2478 or lower resulted in the depletion of p53 and Akt proteins, a reduction in nuclear NFKB, and the cleavage of caspase-3. In the NCI-H929 xenograft model, KW-2478 (qd×5, i.v.) showed a statistically significant suppression of tumour growth at the doses of 25, 50, 100 and 200 mg/kg. Moreover, tumour regressions were observed at doses of 100 and 200 mg/kg, with a significant decrease in serum M protein concentration at doses of 50, 100 and 200 mg/kg. No severe KW-2478 toxicity was observed as assessed by treatment-related mortality and body weight change. Conclusions: The novel HSP90 inhibitor KW-2478 showed a potent anti-tumour activity both in vitro and in vivo, including activity in primary patient samples. The agent retained its activity in primary myeloma cells in the presence of BMSCs, suggesting that KW-2478 can overcome the protective effect of the bone marrow microenvironment. Additional pharmacokinetic and safety data support the further development of KW-2478 and the drug is currently undergoing clinical evaluation in a phase I trial.

scholarly journals Triphenyltin Ortho-Aminophenyl- and 2-Pyridyl-Thiolates: Synthesis and In Vitro Antitumour Activity

1996 ◽  
Vol 3 (2) ◽  
pp. 75-78 ◽  
Author(s):  
Marcel Gielen ◽  
Abdeslam Bouhdid ◽  
Edward R. T. Tiekink ◽  
Dick de Vos ◽  
Rudolph Willem
Keyword(s):  
Cell Lines ◽  
Antitumour Activity ◽  
Spectroscopic Characterization ◽  
X Ray Diffraction ◽  
Tetrahedral Geometry ◽  
X Ray ◽  
Distorted Tetrahedral Geometry ◽  
Monodentate Coordination

The synthesis, spectroscopic characterization and in vitro antitumour activity of two triorganotin compounds, triphenyltin ortho-aminophenylthiolate (1) and triphenyltin 2-pyridylthiolate, compound (2) are reported. The structure of 1 is confirmed by X-ray diffraction, with the tin atom in a distorted tetrahedral geometry because of monodentate coordination, as a thiolate (Sn-S 2.431(2) Å), of the ortho-aminophenylthiolate ligand. The in vitro antitumour activities of 1 and 2, against a number of cell lines, are comparable to those exhibited by methotrexate and doxorubicin, and higher than those of carboplatin and cisplatin.

Host–Guest Inclusion System of Scutellarin with Polyamine-β-Cyclodextrin: Preparation, Characterisation, and Anti-cancer Activity

2015 ◽  
Vol 68 (6) ◽  
pp. 946 ◽  
Author(s):  
Xue Ma ◽  
Bo Yang ◽  
Yulin Zhao ◽  
Hudie Xie ◽  
Xiaoshun Gong
Keyword(s):  
Inclusion Complexation ◽  
Two Dimensional ◽  
X Ray Diffraction ◽  
Amino Groups ◽  
X Ray ◽  
Anti Tumour Activity ◽  
Anti Cancer ◽  
Tumour Activity ◽  
Cancer Activity ◽  
Scanning Electron

The inclusion complexation behaviours of scutellarin (SCU) with four polyamine-modified β-cyclodextrins (NH2-βCD, EN-βCD, DETA-βCD, and TETA-βCD; EN = ethylenediamine; DETA = diethylenetriamine; TETA = triethylenetetramine) have been investigated in both solution and solid state by photoluminescence spectroscopy, 1H and two-dimensional NMR spectroscopy, thermogravimetric analysis, X-ray diffraction, and scanning electron microscopy. The results showed that, with the increase in the number of amino groups, the hosts polyamine-modified β-cyclodextrins (NH2-βCD, EN-βCD, DETA-βCD, TETA-βCD) were able to solubilise SCU to higher levels than native β-CD (9.0 mg mL–1) up to 15.8, 20.4, 44.6, 50.7 mg mL–1 (calculated as SCU), respectively. Besides, the anti-tumour activity of SCU obviously increased after formation of the inclusion complexes. The SCU/CD complexes will be potentially useful for the design of a novel formulation of SCU for clinical treatment.

Novel Thiazine Substituted 9-Anilinoacridines: Synthesis, Antitumour Activity and Structure Activity Relationships

2019 ◽  
Vol 19 (11) ◽  
pp. 1350-1358 ◽  
Author(s):  
R. Kalirajan ◽  
K. Gaurav ◽  
A. Pandiselvi ◽  
B. Gowramma ◽  
S. Sankar
Keyword(s):  
Cell Lines ◽  
Anticancer Agents ◽  
Antitumor Agents ◽  
Antitumour Activity ◽  
Human Tumor ◽  
Cytotoxic Activities ◽  
Anti Tumour Activity ◽  
Tumour Activity

Background: 9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9- anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. Methods: In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characterized by physical and spectral data and their cytotoxic activities against DLA cell lines were evaluated. Results: Among those compounds, 4b, c, e, g, i, j, k, m, o, p, q, r exhibited significant short term in vitro cytotoxic activity against Daltons lymphoma ascites (DLA) cells with CTC50 value of 0.18 to 0.31μM. The compounds 4b, c, e, g, i, j, k, m, o, p, q, r are also exhibited significant long term in vitro anti-tumour activity against human tumor cell lines, HEp-2 (laryngeal epithelial carcinoma) by Sulforhodamine B assay with CTC50 value of 0.20 to 0.39μM. The compounds 4b, i, j exhibited significant in vivo antitumor activity with % Increase in Life Span (ILS) 48-82%. Conclusion: Results obtained in this study clearly demonstrated that many of the thiazine substituted 9- anilinoacridines exert interesting anti-tumour activity. The compounds 4b, i, j have significant anti-tumour activity and useful drugs after further refinement. The above derivatives will encourage to design future antitumor agents with high therapeutic potentials.

scholarly journals Synthesis and evaluation of protein-based biopolymer in production of silver nanoparticles as bioactive compound versus carbohydrates-based biopolymers

2020 ◽  
Vol 7 (10) ◽  
pp. 200928
Author(s):  
Altaf H. Basta ◽  
Vivian F. Lotfy ◽  
Khaled Mahmoud ◽  
Nayera A. M. Abdelwahed
Keyword(s):  
Silver Nanoparticles ◽  
Cell Line ◽  
Cell Lines ◽  
Active Agent ◽  
Antimicrobial Activities ◽  
Compound Versus ◽  
Normal Retina ◽  
Anti Tumour Activity ◽  
Tumour Activity

This overall process deals with evaluating the performance of silver nanoparticles, synthesized from sodium caseinate (SC) as green biological active agent, in comparison with widely produced from carboxymethyl cellulose, other carbohydrates (oxidized nanocellulose fibres (OC) and starch (St)). The TGA, FTIR and TEM, as well as its antimicrobial activities toward pathogenic Gram-positive and Gram-negative bacteria in addition to the yeast strain Candida albicans NRRL Y-477 were examined. In addition, with regard to their anti-tumour activity, the evaluation was studied via many cancer cell lines against RPE1 (normal retina cell line). The results revealed that the SC–Ag(I) and CMC–Ag(I) complexes were formed in six- and five-membered chelate rings, respectively, as nanoparticles, while linear chelation structure was formed in case of OC–Ag(I) and St–Ag(I) complexes. The complexation of SC with Ag(I) ions was recommended as promising stable and antimicrobial agent, with lower free Ag(I) ions and particle size than other Ag-complexes. Moreover, it provided anti-tumour activity of most tested cell lines ( in vitro ), with the following sequence HCT116 > PC3 > HePG 2 > MCF-7 > A549 with IC 50 and IC 90 values of 25.8 and 54.73 µg ml −1 , 45.1 and 66.7 µg ml −1 , 64.3 and 110.7 µgml −1 , 71.4 and 114.8 µgml −1 and 80.1 and 127.7 µgml −1 , respectively. The promising effect of SC–Ag complex was also clear from its selective index versus RPE1 (normal retina cell line).

scholarly journals In vitro targeting and selective killing of mcf-7 and colo320dm cells by 5-fluorouracil anchored to carboxylated SWCNTs and MWCNTs

2021 ◽  
Vol 32 (6) ◽  
Author(s):  
Rutuja V. Kamble ◽  
Somnath D. Bhinge ◽  
Shrinivas K. Mohite ◽  
Dheeraj S. Randive ◽  
Mangesh A. Bhutkar
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Functional Group ◽  
Drug Loading ◽  
Loading Capacity ◽  
X Ray Diffraction ◽  
X Ray ◽  
Swcnts And Mwcnts ◽  
Mcf 7

AbstractThe intention of the present work was to synthesize the f-MWCNT and f-SWCNT terminated with proper functional group, loading of 5-Flurouracil and to perform cytotoxic activity. Functionalization of MWCNTs and SWCNTs was achieved through the acid treatment (H2SO4 + HNO3). 5-flurouracil was loaded into the prepared functionalized CNTs, thereafter; in vitro drug loading capacity and % drug release were calculated. Also the prepared f-CNTs, 5-flurouracil loaded CNTs were distinguished by using SEM, TGA, DSC, X-ray diffraction, Raman and FTIR spectroscopy. MCF-7 and COLO320DM cells were treated with selected concentrations of 5-FU loaded f-MWCNTs and f-SWCNTs to estimate the cytotoxic activity. It was observed that 5-FU loaded f-SWCNTs showed good activity against selected cell lines than others. Moreover, apoptosis percentage was reported to be 84.46 ± 4.3515 and 92.78 ± 2.6549 for 5-FU loaded f-SWCNTs against MCF-7 and COLO320DM cells respectively. It is evident from the results that the prepared drug loaded CNTs have comparable antitumor activity in cancer cell lines.

scholarly journals Pyrene Carboxylate Ligand Based Coordination Polymers for Microwave-Assisted Solvent-Free Cyanosilylation of Aldehydes

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1101
Author(s):  
Anirban Karmakar ◽  
Anup Paul ◽  
Elia Pantanetti Sabatini ◽  
M. Fátima C. Guedes da Silva ◽  
Armando J. L. Pombeiro
Keyword(s):  
Coordination Polymer ◽  
Single Crystal ◽  
Coordination Polymers ◽  
Metal Ion ◽  
Solvent Free ◽  
Lewis Acidity ◽  
Carboxylate Ligand ◽  
X Ray Diffraction ◽  
X Ray ◽  
Microwave Assisted

The new coordination polymers (CPs) [Zn(μ-1κO1:1κO2-L)(H2O)2]n·n(H2O) (1) and [Cd(μ4-1κO1O2:2κN:3,4κO3-L)(H2O)]n·n(H2O) (2) are reported, being prepared by the solvothermal reactions of 5-{(pyren-4-ylmethyl)amino}isophthalic acid (H2L) with Zn(NO3)2.6H2O or Cd(NO3)2.4H2O, respectively. They were synthesized in a basic ethanolic medium or a DMF:H2O mixture, respectively. These compounds were characterized by single-crystal X-ray diffraction, FTIR spectroscopy, thermogravimetric and elemental analysis. The single-crystal X-ray diffraction analysis revealed that compound 1 is a one dimensional linear coordination polymer, whereas 2 presents a two dimensional network. In both compounds, the coordinating ligand (L2−) is twisted due to the rotation of the pyrene ring around the CH2-NH bond. In compound 1, the Zn(II) metal ion has a tetrahedral geometry, whereas, in 2, the dinuclear [Cd2(COO)2] moiety acts as a secondary building unit and the Cd(II) ion possesses a distorted octahedral geometry. Recently, several CPs have been explored for the cyanosilylation reaction under conventional conditions, but microwave-assisted cyanosilylation of aldehydes catalyzed by CPs has not yet been well studied. Thus, we have tested the solvent-free microwave-assisted cyanosilylation reactions of different aldehydes, with trimethylsilyl cyanide, using our synthesized compounds, which behave as highly active heterogeneous catalysts. The coordination polymer 1 is more effective than 2, conceivably due to the higher Lewis acidity of the Zn(II) than the Cd(II) center and to a higher accessibility of the metal centers in the former framework. We have also checked the heterogeneity and recyclability of these coordination polymers, showing that they remain active at least after four recyclings.

A study on using expanded perlite with hydroxyapatite: Reinforced bio-composites

2021 ◽  
pp. 095441192199656
Author(s):  
Erdoğan Karip ◽  
Mehtap Muratoğlu
Keyword(s):  
Body Fluid ◽  
Xrd Analysis ◽  
Cold Isostatic Pressing ◽  
Expanded Perlite ◽  
X Ray Diffraction ◽  
Pressing Method ◽  
X Ray ◽  
Infra Red ◽  
Ft Ir

People are exposed to different kinds of diseases or various accidents in life. Hydroxyapatite (HA) has been widely employed for bone treatment applications. In this study, HA was extracted from sheep bones. Bio-composites were doped with 1, 5, and 10 wt.% of expanded perlite and 5 wt.% of ZrO2–MgO-P2O5. The bio-composites were prepared by the cold isostatic pressing method (250 MPa) and sintered at 900°C for 1 h. In order to evaluate the characteristics of the bio-composites, microhardness, density, X-ray diffraction (XRD), Fourier transform infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM), and energy dispersive spectroscopy (EDS) analyses were carried out on them. Additionally, the specimens whose characteristics were determined were kept in synthetic body fluid (SBF), and their in vitro behavior was examined. As a result, it was observed that microhardness increased as both the weight and the grain size of the expanded perlite were increased. Calcium silicate, tri-calcium phosphate, and hydroxyapatite were observed in the XRD analysis of all samples, and the formation of apatite structures was increased by addition of ZrO2–MgO–P2O5.

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