Showing papers in "Metal-based Drugs in 2002"
TL;DR: The antibacterial and antifungal activity of zinc(II) carboxylates with composition Zn(RCOO)2•nH2O is studied against bacterial strains Staphylococcus aureus, Escherichia coli and yeast Candida albicans.
Abstract: The antibacterial and antifungal activity of zinc(II) carboxylates with composition Zn(RCOO)2•nH2O(R =H-, CH3-, CH3CH2CH2-, (CH3)2CH-, XCH2-, X=Cl, Br, I, n=0 or 2), [ZnX2(Nia+CH2COO-)2](Nia=nicotinamide, X=Cl, Br, I) and [Zn(XCH2COO)2(Caf)2]•2H2O (Car=caffeine, X=Cl, Br) is studied against bacterial strains Staphylococcus aureus, Escherichia coli and yeast Candida albicans. The structural types are assigned to the prepared compounds and the influence of (i) carboxylate chain length, (ii) substitution of hydrogen atom of carboxylate by halogen and (iii) presence of N-donor organic ligands on the biological activity is discussed.
55 citations
TL;DR: The antibacterial potency of the Schiff base increased upon chelation/complexation, having the same metal ion but different anions opening up a novel approach in finding new ways to fight against antibiotic resistant strains.
Abstract: A condensation reaction of 2-amino-1,3,4-thiadiazole with 2-pyrrolecarboxaldehyde to form tridentate NNN donor Schiff base has been performed. The prepared Schiff base was further used for the formation of metal complexes having stoichiometry [M(L)(2)]X(n), where M=Cu(II) or Zn(II), L=N-(2-pyrrolylmethylene)-2-amino-1,3,4-thiadiazole, X=SO(4) (2-), NO(3) (-), C(2)O(4) (2-) or CH(3)CO(2-) and n=1 or 2. The new compounds described here have been characterized by their physical, spectral and analytical data, and have been screened against several bacterial strains such as Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The antibacterial potency of the Schiff base increased upon chelation/complexation, having the same metal ion (cation) but different anions opening up a novel approach in finding new ways to fight against antibiotic resistant strains.
28 citations
TL;DR: The Schiff-base and its complexes have been screened for antibacterial activity against bacterial strains e.g., Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.
Abstract: Co(II) and Ni(II) complexes with a Schiff base, N-(2-furanylmethylene)-2-aminothiadiazole have been prepared and characterized by their physical, spectral and analytical data. The synthesized Schiff-bases act as tridentate ligands during the complexation reaction with Co(II) and Ni(II. metal ions. They possess the composition [ M ( L ) 2 ] X n (where M=Co(II) or Ni(II), L=, X= NO 3 − , SO 4 2 − , C 2 O 4 2 − or CH 3 CO 2 − and n=1 or 2) and show an octahedral geometry. In order to evaluate the effect of anions upon chelation, the Schiff-base and its complexes have been screened for antibacterial activity against bacterial strains e.g., Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.
26 citations
TL;DR: A series of diorganotin dicarboxylates synthesized by the reaction of dimethyltin oxide with germanium substituted propionic acid in 1:2 molar ratio in toluene have been found to have potential activity against bacteria.
Abstract: A series of diorganotin dicarboxylates of the general formula (CH3)2Sn(OCOCHR3CHR2GeR1)2 where R1=(C6H5)3 , (P-CH3C6H4)3 , N(CH2CH2O)3 , R2=C6H5 , H, CH3 , P-CH3OC6H4 , P-ClC6H4 , P-CH3C6H4 , R3=CH3 and H, have been synthesized by the reaction of dimethyltin oxide with germanium substituted propionic acid in 1:2 molar ratio in toluene. The H2O formed was removed azeotropically using a Dean and Stark apparatus. All the compounds have been characterized by IR, multinuclear (H1 , C13 , S119n ) NMR, mass and Mossbauer spectroscopies. All compounds were found to have potential activity against bacteria.
22 citations
TL;DR: Flow cytometry analysis has shown that each platinum(II) complex induced apoptosis in MCF7 cells, and the level of apoptosis correlated with cytotoxicity level for the range concentrations.
Abstract: The platinum (II)complexes, cis-[PtCl(2)(CH(3)SCH(2)CH(2)SCH(3))] (Pt1), cis-[PtCl(2)(dmso)(2)] (dmso is dimethylsulfoxide; Pt2) and cis-[PtCl(2)(NH(3))(2)] (cisplatin), and taxol (T) have been tested at different equimolar concentrations. Cells were exposed to complexes for 2 h and left to recover in fresh medium for 24, 48 or 72 h. Growth inhibition was measured by tetrazolium WST1 assay Analyses of the cell cycle, and apoptosis were performed by flow cytometry, at the same exposure times. The IC50 value of each platinum(II) complex as well as combination index (CI; platinum(II) complex + taxol) for various cytotoxicity levels were determined by median effects analysis.MCF7 cells were found to be sensitive to both Pt1 and Pt2 complexe These cisplatin analogues influenced the cell growth more effectively as compared to cisplatin. Cytotoxic effect was concentration and time-dependent. Profound growth inhibitory effect was observed for Pt1 complex, across all its concentrations at all recovery periods. A plateau effect was achieved three days after treatment at Pt1 concentrations
19 citations
TL;DR: Light microscopic study of the treated tumour mass demonstrated that certain cellular degradation, such as disappearance of mitotic figures, loss in cellular compactness, distortion of nucleus and disruption of cytoplasmic boundaries, takes place in the tumour region of complex treated mice.
Abstract: Thiiobenzyhdrazide (Htbh) and its Cu(II) complexes, [Cu(Htbh)2Cl2] and [Cu(tbh)2] were synthesized and characterized by various physicochemical studies. In vivo and in vitro antitumour activity of Htbh, [Cu(Htbh)2Cl2] and [Cu(tbh)2] has been tested. LD50 values were calculated for all the three compounds. It was observed that the antitumour effect of [Cu(Htbh)2Cl2] is maximum. Light microscopic study of the treated tumour mass demonstrated that certain cellular degradation, such as disappearance of mitotic figures, loss in cellular compactness, distortion of nucleus and disruption of cytoplasmic boundaries, takes place in the tumour region of complex treated mice. Further, tumour bearing mice administered with Cu(II) complexes showed reversal of tumour growth associated induction of apoptosis in lymphocytes.
17 citations
TL;DR: The results suggest a structure-activity relationship in that the 2-isomeric species are more active, particularly against the non-small cell lung cancer and renal cancer cell lines, results that may indicate some selectivity in their cytotoxic profile.
Abstract: The results of cytotoxicity trials against a panel of seven human cell lines for a series of triorganophosphinegold(I) 3- and 4-mercaptobenzoates are reported. While the new compounds show moderate to high toxicity, their potencies are inferior to those reported previously for their isomeric 2- mercaptobenzoate derivatives. The results therefore suggest a structure-activity relationship in that the 2-isomeric species are more active, particularly against the non-small cell lung cancer and renal cancer cell lines, results that may indicate some selectivity in their cytotoxic profile.
13 citations
TL;DR: The testicular sperm density andtesticular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs have been examined and discussed.
Abstract: Some antifertility inhibitors of 18 to 24-membered tetraazamacrocyclic complexes of iron(II) and manganese(II) have been synthesised by the template condensation using 1,3-phenylenediamine with malonic acid, succinic acid, glutaric acid and adipic acid. The reaction proceed smoothly to completion. The complexes were characterized by elemental analyses, molecular weight determinations, infrared, electronic, magnetic moment, mossbaur and mass spectral studies. The elemental analyses are consistent with the formation of the complexes [M(N4Ln)Cl2] (M = Fe(lI) or Mn(II)). All these complexes are stable and monomeric in nature as indicated by the molecular weight determinations. The spectral studies confirm the octahedral geometry around the central metal atom. The complexes have been screened in vitro against a number of fungi and bacteria to assess their growth inhibiting potential. The testicular sperm density and testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trials and biochemical parameters of reproductive organs have been examined and discussed.
12 citations
TL;DR: Some manganese(II) complexes derived from different sulphadrugs and heterocyclic ketones have been prepared and it is suggested that the ligands act in a monobasic, bidentate manner coordinating through nitrogen atom.
Abstract: Some manganese(II) complexes derived from different sulphadrugs and heterocyclic ketones have been prepared. These complexes have been characterized on the basis of elemental analyses, molecular weight determinations, conductivity measurements, infrared, ESR and magnetic measurements. The spectral data suggest that the ligands act in a monobasic, bidentate manner coordinating through nitrogen atom. A high spin tetrahedral geometry around this metal has been proposed on the basis of magnetic and spectral studies. The isolated products are coloured solids, soluble in DMSO, DMF and MeOH. All the complexes are monomeric in nature as indicated by their molecular weight determinations and conductivity measurements in dry DMF show them to be non-electrolytes. All the ligands and their corresponding complexes have been screened for their fungicidal, bactericidal and nematicidal activities.
12 citations
TL;DR: Ten newly synthesized organophosphorus derivatives containing substituted chalcones and substitution chalcone semicarbazones were tested for their antifungal efficacy against sugarcane pathogens and the screening results were correlated with structural features of the tested compounds.
Abstract: Ten newly synthesized organophosphorus derivatives containing substituted chalcones and substituted chalcone semicarbazones were tested for their antifungal efficacy against Colletotrichum falcatum, Fusarium oxysporum, Curvularia pallescens (all sugarcane pathogens). The O,O-diethylphosphate derivatives containing 2-chlorochalcone and 2-chlorochalcone semicarbazone exhibited 70-85% mycelial inhibition against all the test fungi at 1000 ppm. The screening results were correlated with structural features of the tested compounds.
11 citations
TL;DR: Although many SOD: model compounds have been reported, their structures are quite different from those of the native enzyme, their potential for therapeutic usefulness and proposed for clinical uses are limited.
Abstract: Superoxide dismutase (SOD) is the scavenger of superoxide anion (O2−) and functions as a protector of living bodies. Study of a model compound of SOD is important when searching for the relationship between functions and structures of enzymes. Furthermore, SOD model compounds have potential for therapeutic usefulness. Although many SOD: model compounds have been reported, their structures are quite different from those of the native enzyme. Cu,Zn-SOD has been proposed for clinical uses. Unfortunately, many problems such as half-lifetime and antigenicity have not been overcome even though several copper(II) complexes are known to show SOD activity. Active oxygen species such as superoxide (O2−) from various components of the cellular electron transport chains, and provided during the respiratory burst of phagocytic cells, have been implicated both in the aging process and in degenerative diseases, including arthritis and cancer. Therefore, the biological system posseses the protective mechanisms against active species.
TL;DR: In this article, the Schiff base, N-(2-thienylmethylene)-2-aminothiadiazole has been prepared and characterized by their physical, spectral and analytical data.
Abstract: Co(II) and Ni(II) complexes Schiff base, N-(2-thienylmethylene)-2-aminothiadiazole have been prepared and characterized by their physical, spectral and analytical data. The title Schiff-base acts as NNS donor tridentate during the complexation reaction with these metal ions having a composition, [M(L)(2)]X(n) where M=Co(II) or Ni(II), L=, X=NO(3) (-), SO(4) (2-), C(2)O(4) (2-) or CH(3)CO(2) (-) and n=1 or 2 and show an octahedral geometry. In order to evaluate the effect anions upon chelation, the Schiff-base and its new complexes have been screened for their antibacterial activity against bacterial strains e.g., Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.
TL;DR: Brine shrimp lethality of a new series of 16 to 26-membered macrocycles of iron(II) containing tetraaza groups and prepared by the template condensation reaction of diacarboxylic acids with 2,6-diaminopyridine and diethylenetriamine in 1:2:2 molar ratios have been studied.
Abstract: Brine shrimp lethality of a new series of 16 to 26-membered macrocycles of iron(II) containing tetraaza groups and prepared by the template condensation reaction of diacarboxylic acids (malonic, succinic, glutaric or adipic) with 2,6-diaminopyridine and diethylenetriamine in 1:2:2 molar ratios have been studied. Structures and bonding of the macrocyclic complexes have been proposed based on elemental analyses, IR, electronic, X-ray and mass spectral studies. An octahedral geometry for these complexes has been proposed as the binding sites are the nitrogen atoms of the macrocycles. The formation of the complexes as [Fe(Ln)Cl2] has been established on the basis of the chemical composition. The complexes have also been screened against several microbes.
TL;DR: The S-derivatives of N-methylimidazolyl, benzoxazoly l and 1,3,4-triazolyL thiols selectively lowered the low density lipoprotein (LDL) level in mice with the high cholesterol diet in nutrition.
Abstract: Silacyclic derivatives of heteroaromatic sulfides have been prepared by using phase transfer catalytic (PTC) system thiol / silacyclopropyl iodide / solid K2CO3 / 18-crown-6 / toluene. The target sulfides were isolated in yields up to 70 %. The S-derivatives of N-methylimidazolyl, benzoxazolyl and 1,3,4-triazolyl thiols selectively lowered the low density lipoprotein (LDL) level in mice with the high cholesterol diet in nutrition.
TL;DR: The mechanism of the formation of complexes in solution is discussed as well as their possible role in aluminum toxicity.
Abstract: Toxic effects due to high aluminum body loads were observed in a number of conditions following ingestion of Al-containing antacids. Bio-availability of aluminum depends not only on the solubility of the ingested salt but also on the physico-chemical properties of the soluble Al complexes formed in body fluids. Amino acids may, upon interaction with Al-salts, form absorbable Al-complexes. Hence, complex formation equilibria between Al3+ and either, L- histidine or L-tyrosine were studied by glass electrode potentiometric (0.1 mol/L LiCl ionic medium, 298 K), proton NMR and uv spectrophotometric measurements. Non linear least squares treatment of the potentiometric data indicates that in the concentration ranges: 0.5≤CA1≤2.0 ; 1.0≤CHis≤10.0; 2.5≤PH≤6.5, in Al3+ + His solutions, the following complexes (with log overall stability constants given in parenthesis) are formed: Al(HHis)3+(12.21±0.08); Al(His)2+, (7.25±0.08); and Al(HHis)His2+, (20.3±0.1). In Al3+ + Tyr solutions in the concentration range 1.0≤CTyr≤3.0 mmol/L and ligand to metal concentration ratio from 2:1 to 3:1, in the pH interval from 3.0 to 6.5 the formation of the following complexes was detected: Al(HTyr)2+, (12.72±0.09); Al(Tyr)2+, (10.16±0.03) and Al(OH)2Tyr , (2.70±0.05). Proton NMR data indicate that in Al(His)2+ complex histidine acts as a monodentate ligand but its bidentate coordination is possible with carboxylate oxygen and imidazole 1-nitrogen as donors. In Al(HTyr)3+ complex tyrosine is a monodentate ligand with carboxylate oxygen as donor. The mechanism of the formation of complexes in solution is discussed as well as their possible role in aluminum toxicity.
TL;DR: In this paper, the interaction of Co(II, Ni(II), Cu( II), Zn( II) and Cd(II) metal ions with 5-fluorouracil (5FU) and histamine (Hm) separately (binary) and in the presence of each other (ternary) at 25 + 0.1 C temperature and a constant ionic strength of
Abstract: Solution studies were performed pH-metrically to study the interaction of Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) metal ions with 5-fluorouracil (5FU) and histamine (Hm) separately (binary) and in the presence of each other (ternary) at 25 + 0.1 C temperature and a constant ionic strength of 0.1 M NaNO3 in aqueous solution. The ternary complexes have been found to be more stable than the corresponding binary complexes as shown by the positive value of AlogK. The species distribution curves have been obtained using the computer programme BEST. On the basis of species distribution results, efforts were also made to prepare some mixed complexes of Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) ions by performing the reaction of their metal nitrates, 5FU and Hm in aqueous ethanol medium at suitable pH. The isolated solid complexes were characterized by different physico-chemical method in order to suggest the possible binding site of the ligands and the structure of the resultant complexes. All these complexes were checked for their antitumour activity by injecting in Dalton’s lymphoma (DL) and Sarcoma-180 (S-180) bearing C3H/He mice. The results indicate that some complexes have good antitumour activity both in vivo and in vitro.
TL;DR: 31P NMR and fluorescence spectroscopy was used to determine the resting [Mg2+]i in bovine chromaffin cells, a neuron-like cellular model, as well as confocal laser scanning microscopy to study the free Mg2 + spatial distribution in these cells.
Abstract: Magnesium is an essential element for all living systems. The quantification of free intracellular Mg(2+) concentration ([Mg(2+)](i)) is of utmost importance since changes in its basal value may be an indication of different pathologies due to abnormalities of Mg(2+) metabolism. In this work we used (31)P NMR and fluorescence spectroscopy to determine the resting [Mg(2+)](i) in bovine chromaffin cells, a neuron-like cellular model, as well as confocal laser scanning microscopy to study the free Mg(2+) spatial distribution in these cells. (31)P NMR spectroscopy did not prove to be effective for the determination of [Mg(2+)](i) in this particular case due to some special morphological and physiological properties of this cell type. A basal [Mg(2+)](i) value of 0.551 +/- 0.008 mM was found for these cells using fluorescence spectroscopy and the Mg(2+)-sensitive probe furaptra; this value falls in the concentration range reported in the literature for neurons from different sources. This technique proved to be an accurate and sensitive tool to determine the [Mg(2+)](i).lntraceilular free Mg(2+) seems to be essentially localized in the nucleus and around it, as shown by confocal microscopy with the Mg(2+)-sensitive probe Magnesium Green. It was not possible to derive any conclusion about free Mg(2+) localization inside the chromaffin granules and/or in the cytoplasm due to the lack of sufficient spatial resolution and to probe compartmentalization.
TL;DR: It could be concluded that the prepared Fe(II)- SFX complex may be recommended to the therapeutic experts for its possible use as a more potent antibiotic drug.
Abstract: The qualitative and quantitative analysis of an antibiotic drug, 5-amino-1 cyclopropyl-7 (cis-3, 5 dimethyl-1-piperazyl)-6,8- dihydro-1, 4 dihydro-4-oxo-3-quinoline carboxylic acid (Sparfloxacin, SFX) and its pharmaceutical formulation i.e.sparx-100 tablet, has been done using polarographic and amperometric methods. Complexation behavior of SFX with Fe(II), both in solid and liquid phases has been studied by elemental analysis, IR.-spectra and polarographic and amperometric methods. SFX produces a single cathodic reduction wave in 0.1 M ammonium tartrate (supporting electrolyte) at pH 6.0 ±0.1. The wave is diffusion controlled and wave height is proportional to the concentration of SFX. The complex is also reversibly reduced at the electrode surface with diffusion-controlled kinetics. The stoichiometry of the Fe(II)- SFX complex is 1:1. Antibacterial studies on the drug and its metal complex have been performed against different bacteria. The observed results revealed the complex to be more potent in its antibacterial activity as compared to the parent drug. On the basis of observed results it could be concluded that the prepared Fe(II)- SFX complex may be recommended to the therapeutic experts for its possible use as a more potent antibiotic drug.
TL;DR: An attempt has been made to correlate the structural aspects of the compounds with their antiinflammatory and antifertility activities.
Abstract: Manganese(II) and iron(II) macrocyclic complexes of polyamide groups have been synthesized by the template codensation of diamines (2,6 diaminopyridine, 1,2 phenylenediamine and 1,3 phenylenediame) and triamine (diethylenetriamine) with phthalic acid in 1:2:2 molar ratios. On the basis of elemental analysis, IR, electronic, magnetic moment, Mossbauer, mass and X-ray spectral studies, octahedral structure has been assigned to [M(N4macn)Cl2] (M = Mn(II) and Fe(II), n = 1 to 4) complexes. The complexes have been screened in vitro against a number of fungi and bacteria to assess their growth inhibiting potential. An attempt has been made to correlate the structural aspects of the compounds with their antiinflammatory and antifertility activities.
TL;DR: Silicon containing pyridine and quinoline sulfides have been prepared using phase transfer catalytic system thiol/alkyl halide / solid KOH/18-crown-6 / toluene and the cytotoxicity of the synthesized compounds was studied.
Abstract: Silicon containing pyridine and quinoline sulfides have been prepared using phase transfer catalytic system thiol/alkyl halide / solid KOH/18-crown-6 / toluene. The target S-ethers were isolated in yields up to 81%. The cytotoxicity of the synthesized compounds was studied. Among pyridine sulfides S-[3-(1-methyl- 1-silacyclohexyl)propyl] derivatives 5e and 6e exhibit the highest cytotoxicity. Aliphatic silicon derivatives were considerably less active. 8-[(Trimethylsilylmethyl)thio]quinoline (8a) exhibits the highest activity among quinoline sulfides.
TL;DR: Overall, these antineoplastic agents caused reduction of DNA and protein replication, which would lead to killing of cancer cells.
Abstract: N 6 -Benzoyladenine-cyanoborane (2), and 6-triphenylphosphonylpurine-cyanoborane (3) were selected for investigation of cytotoxicity in murine and human tumor cell lines, effects on human HL-60 leukemic metabolism and DNA strand scission to determine the feasibility of these compounds as clinical antineoplastic agents. Compounds 2 and 3 both showed effective cytotoxicity based on ED50 values less than 4 μg/ml for L1210, P388, HL-60, Tmolt3, HUT-78, HeLa-S3 uterine, ileum HCT-8, and liver Hepe-2. Compound 2 had activity against ovary 1-A9, while compound 3 was only active against prostate PL and glioma UM. Neither compound was active against the growth of lung 549, breast MCF-7, osteosarcoma HSO, melanoma SK2, KB nasopharynx, and THP-1 acute monocytic leukemia. In mode of action studies in human leukemia HL-60 cells, both compounds demonstrated inhibition of DNA and protein syntheses after 60 min at 100 μM. These compounds inhibited RNA synthesis to a lesser extent. The utilization of the DNA template was suppressed by the compounds as determined by inhibition of the activities of DNA polymerase α, m-RNA polymerase, r-RNA polymerase and t-RNA polymerase, which would cause adequate inhibition of the synthesis of both DNA and RNA. Both compounds markedly inhibited dihydrofolate reductase activity, especially in compound 2. The compounds appeared to have caused cross-linking of the DNA strands after 24 hr at 100 μM in HL-60 cells, which was consistent with the observed increased in ct-DNA viscosity after 24 hr at 100 μM. The compounds had no inhibitory effects on DNA topoisomerase I and II activities or DNA-protein linked breaks. Neither compound interacted with the DNA molecule itself through alkylation of the nucleotide bases nor caused DNA interculation between base pairs. Overall, these antineoplastic agents caused reduction of DNA and protein replication, which would lead to killing of cancer cells.
TL;DR: Five coordinated novel complexes of Cu II and Ni II have been synthesized from benzil and 1,3- diaminopropane- Cu II / Ni II complex and characterized by elemental analysis, indicating strong binding of the complex to the calf thymus DNA.
Abstract: Five coordinated novel complexes of CuII and NiII have been synthesized from benzil and 1,3- diaminopropane-CuII/NiII complex and characterized by elemental analysis, i.r., n.m.r., e.p.r, molar conductance and u.v-vis, spectroscopy. The complexes are ionic in nature and exhibit pentaeoordinated geometry around the metal ion. The reaction kinetics of C25H36N5O2CuCl with calf thymus DNA was studied by u.v-vis, spectroscopy in aqueous medium. The complex after interaction with calf thymus DNA shows shift in the absorption spectrum and hypochromicity indicating an intercalative binding mode. The Kobs values have been calculated under pseudo-first order conditions. The redox behaviour of complex C25H36N5O2CuCl in the presence and in the absence of calf thymus DNA in the aqueous solution has been investigated by cyclic voltammetry. The cyclic voitammogram exhibits one quasi-reversible redox wave corresponding to CuII/CuI redox couple with E1/2 values of -0.377 and -0.237 V respectively at a scan rate of 0.1Vs-1 .On interaction with calf thymus DNA, the complex C25H36N5O2CuCl exhibits shifts in both Ep as well as in E1/2 values, indicating strong binding of the complex to the calf thymus DNA.
TL;DR: This solventless synthesis apart from eliminating organic solvent from workup step, also gave improved yield as compared to the conventional heating, with reaction time reduced from hours to minutes.
Abstract: A series of new barbituryl/thiobarbituryl substituted organomercurial derivatives 3a-i have been synthesised from pyrimidine derivatives 1a-c and arylmercuric chloride 2a-c over K2CO3 under microwave irradiations (MWI). This solventless synthesis apart from eliminating organic solvent from workup step, also gave improved yield as compared to the conventional heating, with reaction time reduced from hours to minutes. The prepared compounds were tested against A. niger and A. flavous for their antifungal activity and were found to posses good activity.
TL;DR: According to spectroscopic observations, the hybrid anions consist of a lacunary anion framework on which are grafted two equivalent or groups through P-O-W bridges.
Abstract: Organothiophosphoryl polyoxotungstates R 2 XW 11 O 39 n − , R 2 P 2 W 17 O 61 6 − , R 2 PW 9 O 34 5 − , (X = P, Si, Ge, B or Ga; R = PhP(S), C6H11P(S)) have been prepared from lacunary polyoxoanions and PhP(S) Cl 2 or C 6 H 11 P ( S ) Cl 2 . The products were characterized by elemental analysis, IR, P 31 and W 183 NMR spectroscopy. According to spectroscopic observations, the hybrid anions consist of a lacunary anion framework on which are grafted two equivalent C 6 H 5 P ( S ) or C 6 H 11 P ( S ) groups through P-O-W bridges. Some of the title compounds showed the antigerm activity.
TL;DR: The in vitro antitumour activity of ionic diphenyltin(IV) complexes 4 and 5 against seven tumoural cell lines of human origin is reported and the preparation and characterization of the novel compound 3 is mentioned too.
Abstract: The in vitro antifungal activity of compounds 1-3 ( { [ ( CH 3 ) 2 NCH 2 ] 2 C 6 H 3 } R 2 SnX ; (where X=Cl, R=n-Bu for 1, X=Br, R=n-Bu for 2 and x= PF 6 , R=n=Bu for 3)) was estimated with the help of a modified microdilution format of the M27-A guidelines and was compared with in vitro activity of their diphenyltin(IV) analogues 4 and 5 (where X=Br, R=Ph for 4 and X= PF 6 , R=Ph for 5), and of drugs currently in clinical use (ketoconazole, fluconazole and amphotericin B). It was found that in coordinating solvents the more soluble derivative 2 is less active than the phenyl one (4), and compounds 1 and 3 are even inactive.
In this paper, the in vitro antitumour activity of ionic diphenyltin(IV) complexes 4 and 5 against seven tumoural cell lines of human origin is also reported. The preparation and characterization ( H 1 , C 13 and Sn 119 NMR spectroscopy and electrospray ionization mass spectrometry) of the novel compound 3 is mentioned too.
TL;DR: It has been observed that the addition of dexamethasone enhances the apoptosis index only in U937, a monocytic line with a glucocorticoid receptor bearing.
Abstract: Apoptosis induced by rhodium II amidate, rhodium II propionate, cisplatin and interactions with dexamethaxone were studied on some human leukemia cell lines Raji, Jurkat and U937. Apoptosis was studied by flow cytometry, agarose gel electrophoresis and morphological analysis. Rhodium II propionate induced apoptosis in all the three cell lines, Rhodium II amidate, in the lymphoid cell lines Jurkat and Raji, and cisplatin, only in the Jurkat, a T lymphoid cell line. It has also been observed that the addition of dexamethasone enhances the apoptosis index only in U937, a monocytic line with a glucocorticoid receptor bearing.
TL;DR: Some of the organo-iron ferrocene derivatives and arenocenium salts are promising to be used against Chagas' disease as a prophylactic agents.
Abstract: Eight organo-iron ferrocene derivatives and arenocenium salts were prepared and evaluated by “in vitro” assay against one strain of Trypanosoma cruzi (Y). Six of the eight organo-iron compounds assayed, piperazinium diferrocenoate 1, η 6 - ( o - xylene ) - η 5 -(cyclopentadienyl) Iron(II) hexafluorophosphate 3, η 6 -(mesitylene)- η 5 -(cyclopentadienyl) iron(II) hexafluorphosphate 5, η 6 -(durene)- η 5 -(cyclopentadienyl) iron(II) hexafluorphosphate 6, η 6 -( ρ -chlorotoluene)- η 5 -(cyclopentadienyl) Iron(II) hexafluorphosphate 7 and η 6 -(chlorobenzene)- η 5 -(cyclopentadienyl) iron(II) picrate 8 , were poorly active in the “in vitro” assays. Only two compounds 1,1'–(N-pyperidinocarbonyl) ferrocene 2 ( IC 50 = 2.4 μg/mL ) and η 6 - ( o - xylene ) - η 5 (cyclopentadienyl) iron(II) picrate 4 ( IC 50 = 12.08 μg/mL ) , were more active. Thus, some of the compounds are promising to be used against Chagas' disease as a prophylactic agents.
TL;DR: It is suggested that copper aspirinate possesses potential neuroprotective properties, the mechanism of which might be related to an increase of the activity of endogenous superoxide dismutase.
Abstract: The cerebroprotective effects of copper aspirinate [dimeric copper(II) bis(o-acetoxybenzoate)] were investigated in gerbils subjected to 10-min global cerebral ischemia followed b 60-min reperfusion. The results showed that intragastric copper aspirinate (7.5, 15.0 and 30.0 mg Kg(-1)) markedly promoted the recovery of the electroencephalogram amplitude, attenuated the increase of lipid peroxide content and the decrease of superoxide dismutase activity in the cortex during ischemia-reperfusion injury. It suggested that copper aspirinate possesses potential neuroprotective properties, the mechanism of which might be related to an increase of the activity of endogenous superoxide dismutase.
TL;DR: While the compound shows no activity against K-562 cells, there is evidence for some cytotoxicity against SK-OV-3, and its limited solubility restricts the useable concentration range.
Abstract: A simple method for the preparation of cis-dichloro(1,4,7-triazacyclononane)platinum(II), cis-Pt(tacn)Cl2 is presented, together with the results of screening the compound against the K-562 (leukemia) and SK-OV-3 (ovarian) human cancer cell lines. While the compound shows no activity against K-562 cells, there is evidence for some cytotoxicity against SK-OV-3. The compound is much less effective than cisplatin, and its limited solubility restricts the useable concentration range.