Showing papers in "Metal-based Drugs in 2001"
TL;DR: The complexed Schiff bases have shown to be more antibacterial against one more bacterial species as compared to uncomplexed Schiff-bases.
Abstract: Some novel transition metal [Co(II), Cu(II), Ni(II) and Zn(II)] complexes of substituted pyridine Schiff-bases have been prepared and characterized by physical, spectral and analytical data. The synthesized Schiff-bases act as deprotonated tridentate for the complexation reaction with Co(II), Ni(II) and Zn(II) ions. The new compounds, possessing the general formula [M(L)(2)] where [M=Co(II), Cu(II), Ni(II) and Zn(II) and HL=HL(1), HL(2), HL(3) and HL(4)] show an octahedral geometry. In order to evaluate the effect of metal ions upon chelation, the Schiff bases and their complexes have been screened for antibacterial activity against the strains such as Escherichia coli,Staphylococcus aureus, and Pseudomonas aeruginosa. The complexed Schiff bases have shown to be more antibacterial against one more bacterial species as compared to uncomplexed Schiff-bases.
111 citations
TL;DR: The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.
Abstract: We synthesized a novel anticancer agents based on mixed chelate copper (II) complexes, named Casiopeinas® has of general formula [Cu(N-N)(N-O)H2O]NO3 (where, N-N = diimines as 1,10- phenanthroline, 2,2-bipyridine, or substituted and N-O=aminoeidate or [Cu(N-N)(O-O)H2O]NO3 (where NN= diimines as 10-phenanthroline, 2,2-bipyridine or substituted Casiopeinas I, II, IV, V, VI, VII VIII and O-O=acetylacetonate, salicylaldehidate Casiopinas III). We evaluated the in vitro antitumor activity using a human cancer cell panel and some nurine cancer cells. Eleven Casiopeinas are evaluated in order to acquire some structure-activity correlations and some monodentated Casiopeinas analogues; cisplatinum was used as control drug. The 50% growth inhibition observed is, in all cases reach with concentrations of Casiopeina's 10 or 100 times lower than cisplatinum. In a previous work we reported the induction of apoptosis by Casiopeina II. The results indicate that Casiopeinass are a promising new anticancer drug candidates to be developed further toward clinical trials.
71 citations
TL;DR: NAMI-A is active against metastases also by the oral route, suggesting the use of this way to treat tumour bearing hosts for long periods.
Abstract: NAMI-A, imidazolium trans-imidazoledimethylsulfoxidetetrachlororuthenate, is a ruthenium based compounds capable of inhibiting the growth of lung metastases of solid tumours in a number of experimental conditions.The aim of this study was to investigate the potential use of NAMI-A by the oral route to treat lung metastases of MCa mammary carcinoma in the CBA mouse. treatment of mice, carrying intramuscular tumours in advanced stage of growth, for 11 consecutive days caused a significant reduction of the weight of lung metastases over the range of doses from 150 to 600 mg/kg/day. No sign of toxicity was observed at the histological analysis in the gut epithelium or in the kidney parenchyma, and NAMI-A concentration in the kidney was more than 10-fold lower than after intraperitoneal treatments. NAMI-A is thus active against metastases also by the oral route, suggesting the use of this way to treat tumour bearing hosts for long periods.
42 citations
TL;DR: Antioxidant properties of three Curcumin derivatives in which the 1,3-diketone system is appended with nitrogen and sulfur donors and their copper conjugates are examined for the first time.
Abstract: Antioxidant properties of three Curcumin derivatives in which the 1,3-diketone system is appended with nitrogen and sulfur donors and their copper conjugates are examined for the first time. Metal conjugation seems to offer distinct advantages in radical scavenging activities of curcumin compounds.
36 citations
TL;DR: The antibacterial potency of these Schiff bases increased upon chelation/complexation, against the tested bacterial species, opening new aproaches in the fight against antibiotic resistant strains.
Abstract: Schiff bases were obtained by condensation of 2-amino-l,3,4-thiadiazole with 5-substituted-salicylaldehydes which were further used to obtain complexes of the type [M(L)2]Cl2, where M=Co(II), Cu(II), Ni(II) or Zn(II). The new compounds described here have been characterized by physical, spectral and analytical data, and have been screened for antibacterial activity against several bacterial strains such as Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The antibacterial potency of these Schiff bases increased upon chelation/complexation, against the tested bacterial species, opening new aproaches in the fight against antibiotic resistant strains.
32 citations
TL;DR: Pd-THBD has been found to exhibit an antileukemic activity of the HL-60 line cells matching that of an arbitrary criterion and copper(II) complex has been determined.
Abstract: Complexes of 2-(4-thiazolyi)benzimidazole (thiabendazole, THBD) with Co(II), Ni(II), Cu(ll) of general formula ML2(NO3)2 H2O and complexes of Pd(II) and Pt(II) of general formula ML2Cl2 H2O have been obtained and characterized by elemental analyses, IR and far IR spectroscopy and magnetic measurements. The X-ray crystal structure of the copper(II) complex has been determined. The in vitro cell proliferation inhibitory activity of these compounds was examined against human cancer cell lines A 549 (lung carcinoma), HCV-29 T (urinary bladder carcinoma), MCF-7 (breast cancer), T47D (breast cancer), MES-SA (uterine carcinoma) and HL-60 (promyelocytic leukemia). Pt-THBD has been found to exhibit an antileukemic activity of the HL-60 line cells matching that of an arbitrary criterion.
20 citations
TL;DR: Three new isolated complexes with isomeric ligands markedly affect the growth of the parasites and none of them shows cytotoxicity against macrophage of the J774.2 line at the heaviest dosages used.
Abstract: The synthesis and characterization of two Pt(II) Complexes with the isomeric ligands 4,5-dihydro-5-oxo- [1,2,4]triazolo-[ 1,5-a]pyrimidine (5HtpO) and 4,7-dihydro-7-oxo-[ 1,2,4]-triazolo-[ 1,5-a]pyrimidine (7HtpO) are described, as well as a Ru(III) complex with 7HtpO. The crystal structure of cis-[PtCl2(7HtpO)2].2H2O has been solved by X-ray diffraction analysis. In vitro activity of the new isolated complexes against the epimastigote form of T. cruzi, procyclic form of T. b. brucei and promastigote form of L. donnovani and P. characias has also been studied. The three complexes markedly affect the growth of the parasites and none of them shows cytotoxicity against macrophage of the J774.2 line at the heaviest dosages used.
20 citations
TL;DR: It is found that the three major products of guanine oxidation are formed by independent reaction routes, and the oxidized guanidinohydantoin and the proposed spiro compound 3 derivatives are not precursors of imidazolone lesion (Iz).
Abstract: In order to better define the mechanism and the products of guanine oxidation within DNA, we investigated the details of the mechanism of guanine oxidation by a metalloporphyrin, Mn-TMPyP, associated to KHSO5 on oligonucleotides. We found that the three major products of guanine oxidation are formed by independent reaction routes. The oxidized guanidinohydantoin (1) and the proposed spiro compound 3 derivatives are not precursors of imidazolone lesion (Iz). These guanine lesions as well as their degradation products, may account for non-detected guanine oxidation products on oxidatively damaged DNA.
19 citations
TL;DR: Some ruthenium(III) complexes with aryl-azo 2,4-pentanedione as co-ligands (L1H - L3H2) have been synthesized and characterized spectroscopically IR, 1H NMR, UV/Vis, ESR, conductimetric and FAB-mass data.
Abstract: Some ruthenium(III) complexes with aryl-azo 2,4-pentanedione as co-ligands (LH1-LH3) have been synthesized and characterized spectroscopically IR, H1 NMR, UV/Vis, ESR, conductimetric) along with elemental analysis and FAB-mass data. Their luminescent and redox properties have been studied. The antibacterial, anti-HIV and antitmnour activities have also been reported.
18 citations
TL;DR: Interaction studies of these complexes with CT-DNA revealed their high affinity for DNA and the possibility of noncovalent interactions between ancillary ligands and nucleobases by van der Waals contacts and H-bridges.
Abstract: The complexes [Ru([9]aneS3)(dppz)Cl]Cl 1 and [Ru([12]aneS4)(dppz)]Cl2,2 ([9]aneS3 = 1,4,7- trithiaciclononane and [12]aneS4 = 1,4,7,10-tetrathiaciclododecane) were synthesised and fully characterised . These complexes belong to a small family of dipyridophenazine complexes with non-polypyridyl ancillary ligands . Interaction studies of these complexes with CT-DNA (UV/Vis titrations, steady-state emission and thermal denaturation) revealed their high affinity for DNA . Intercalation constants determined by UV/Vis titrations are of the same order of magnitude (106) as other dppz metallointercalators, namely [Ru(II)(bpy)2dppz]S2
17 citations
TL;DR: The result suggest that circumvention of ciplatin resistance by trans-[PtCl2(N,N-dimethylamine)(isopropylamine)] in A2780cisR cells might be related with the ability of this drug to induce apoptosis.
Abstract: Trans-[PtCl2(N,N-dimethylamine)(isopropylamine)] is a novel trans-platinum compound that shows cytotoxic activity in several cisplatin resistant cell lines. The aim of this paper was to analyse, by means of molecular cell biology techniques and total reflection X-ray fluorescence (TXRF), the cytotoxic activity, the induction of apoptosis, the cellular uptake and the DNA binding of trans-[PtCl2(N,N-dimethylamine)(isopropylamine)] in the cisplatin resistant cell line A2780cisR. The results show that this drug is more cytotoxic and induces a higher amount of apoptotic cells than cisplatin in A2780cisR cells. However, the intracellular accumulation and extent of binding to DNA of trans-[PtCl2(N,N-dimethylamine)( isopropylamine)] is lower than that of cis-DDP. Moreover, trans-[PtCl2(N,N-dimethylamine)(isopropylaminae)] is partially inactivated by intracellular levels of glulathione. The result suggest that circumvention of ciplatin resistance by trans-[PtCl2(N,N-dimethylamine)(isopropylamine)] in A2780cisR cells might be related with the ability of this drug to induce apoptosis.
TL;DR: The stepwise preparation and the characterization of new unsymmetrical monoanionic Ru(III) dinuclear compounds are reported and the chemical behavior of compounds 1-4 in physiological solution is described.
Abstract: In this paper we report the stepwise preparation and the characterization of new unsymmetrical monoanionic Ru(III) dinuclear compounds, [NH(4)][{trans-RuCl(4)(Me(2)SO-S)}(mu-L){mer-RuCl(3)(Me(2)SO-S)(Me(2)SO-O)}] (L = pyz (1), pym (2)). By a similar synthetic approach we also prepared new mixed-valence Ru(III)/Ru(II) dinuclear compounds of formula [NH(4)][{trans-RuCl(4)(Me(2)SO-S)}(mu-pyz){cis,cis,cis-RuCl(2)(Me(2)SO-S)(2)(CO)}] (L = pyrazine (pyz, 3), pyrimidine (pym, 4)). Moreover, we describe the chemical behavior of compounds 1-4 in physiological solution, also after complete reduction (with ascorbic acid) to the corresponding Ru(II)/Ru(II) species. Overall, the chemical behavior of 1 and 2 after reduction resembles that of the corresponding dianionic and neutral dinuclear species, [{trans-RuCl(3)(Me(2)SO-S)}(2)(mu-L)](2-)and [{mer-RuCl(3)(Me(2)SO-S)(Me(2)SO-O)}(2) (mu-L)]. On the other hand, the mixed-valence dinuclear compounds 3 and 4, owing to the great inertness of the cis,cis,cis-RuCl(2)(Me(2)SO-S)(2)(CO)(1/2mu-L) fragment, behave substantially like the mononuclear species [trans-RuCl(4)(Me(2)SO-S)(L)](-) in which the terminally bonded L ligand can be considered as bearing a bulky substituent on the other N atom.
TL;DR: Biological investigations have demonstrated that germyl derivatives of trifluoroacetylfuran are more toxic than the silicon analogues.
Abstract: A series of silyl, germyl and alkyl substituted trifluoroacetylfurans has been synthesized under Friedel-Crafts electrophilic acylation conditions Biological investigations have demonstrated that germyl derivatives of trifluoroacetylfuran are more toxic than the silicon analogues 5-Triethylgermyl-2-trifluoroacetylfuran was the most toxic compound (LD50, 112 mg kg-1, ip for white mice), 200 times more toxic than the silicon analogue 5-t-Butyl- and 5-trimethylsilyl-2-trifluroacetylfuran prolong the duration of ethanol anaesthesia by 220 and 140% 5-Triethylgermyl-2-trifluroacetylfuran exibited high anesthetic activity in hexobarbital test (prolonged the duration by 137%) Some of compounds influenced muscle tone and locomotor coordination parameters 5-Triethylgermyl-2-trifluomacetylfuran exibited analgesic activity (ED50, 09 mg kg-1)
TL;DR: Thetesticular sperm density, testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trails and biochemical parameters of reproductive organs have been examined and discussed.
Abstract: Synthesis, characterization and antimicrobial activities of an interesting class of biologically potent macrocyclic complexes have been carried out. All the complexes have been evaluated for their antimicrobial effects on different species of pathogenic fungi and bacteria. The testicular sperm density, testicular sperm morphology, sperm motility, density of cauda epididymal spermatozoa and fertility in mating trails and biochemical parameters of reproductive organs have been examined and discussed. The resulting biologically active [M(Ma L n )( R 2 )] Cl 2 and [Pb(Ma L n )( R 2 ) X 2 ] (where, M = P d II or P t II and X = Cl or N O 3 ) type of complexes have been synthesized by the reactions of macrocyclic ligands (Ma L n ) with metal salts and different diamines in 1:1:1 molar ratio in methanol. Initially the complexes were characterized by elemental analyses, molecular weight determinations and conductivity measurements. The mode of bonding was established on the basis of IR, H 1 NMR, C 13 NMR, Pt 195 NMR, Pb 207 NMR, XRD and electronic spectral studies. The macrocyclic ligand coordinates through the four azomethine nitrogen atoms which are bridged by benzil moieties. IR spectra suggest that the pyridine nitrogen is not coordinating. The palladium and platinum complexes exhibit tetracoordinated square-planar geometry, whereas a hexacoordinated octahedral geometry is suggested for lead complexes.
TL;DR: The synthesis and the evaluation of the pharmacological activity of new organosilicon and organogermanium compounds such as sila- and germadithioacetals derived from N-substituted naphthylimidazolne are reported.
Abstract: A number of organosilicon and organogermanium derivatives and some related compounds including the N-substituted. 2-[1-naphthylmethyl]-2-imidazoline and 2-[1-(1-naphthyl)ethyl]-2-imidazoline have been prepared and the toxicity of some compounds have been determined in mice. In this paper we report the synthesis and the evaluation of the pharmacological activity of new organosilicon and organogermanium, compounds such as sila- and germadithioacetals derived from N-substituted naphthylimidazolne.
TL;DR: It has been found that 2-{[dimethyl (β-triethylgermylethyl)-silylmethyl]thio}-1-methylimidazole and 2-(β-triphenylsilyleal) silyl-methyl}benzothiazole are the most active cholesterol level lowering and vasodilating agents.
Abstract: Silicon and germanium containing heteroaromatic sulfides have been prepared using phase transfer catalytic (PTC) system thiol / Si or Ge containing alkyl halide / solid KOH / 18- crown-6 / toluene The target sulfides were isolated in yields up to 92 % It has been found that 2-{[dimethyl (β-triethylgermylethyl)-silylmethyl]thio}-1-methylimidazole and 2-{[dimethyl(β-triphenylsilylethyl) silyl-methyl]thio}benzothiazole are the most active cholesterol level lowering and vasodilating agents
TL;DR: A square planar copper complex of derivatized NSAID drug, Ketoprofen thiosemicarbazone, is characterized by elemental analysis, spectroscopy, electrochemistry and magnetic susceptibility studies which exhibits dose-dependent and enhanced antiproliferative effects on human breast cancer cell line T47D rich in progesterone receptors.
Abstract: A square planar copper complex of derivatized NSAID drug (Ketoprofen thiosemicarbazone [3-benzoyl- α -methyl benzene acetic acid thiosemicarbazone]), is characterized by elemental analysis, spectroscopy, electrochemistry and magnetic susceptibility studies which exhibits dose-dependent and enhanced antiproliferative effects on human breast cancer cell line T47D rich in progesterone receptors.
TL;DR: Six new compounds [(CpTi)X, Cp=ϋ∇-c∇H∇, X=Ge, Ga, B) have been prepared and their Keggin structures determined by elementary analysis, IR, UV, ∞H NMR and ∞∀∊WNMR spectrometry.
Abstract: Six new compounds [(CpTi)XW11O39]n− (Cp=η5-C5H5, X=Ge, Ga, B) have been prepared and their Keggin structures determined by elementary analysis, IR, UV, H1 NMR and W183 NMR spectrometry The results show that the complexes retain Keggin structure The complexes exhibit antitumoral activity in vitro as shown by MTT experiment
TL;DR: It is observed that 2-hydroxy-1,4-naphthalenedione-l-oximes exhibit higher antifungal activity as compared to antibacterial activity.
Abstract: Erbium(III) complexes of 2-hydroxy-l,4-naphthalenedione-1-oxime and its C-3 substituted derivatives are synthesized and characterized by elemental analysis, thermogravimetric analysis, infrared spectroscopy, magnetic susceptibility measurements 2-hydroxy-1,4-naphthalenedione-1-oxime derivatives are analysed using H1 and C13 NMR spectroscopy. The molecular composition of the synthesized complexes is found to be [ML3(H2O)2]. The antimicrobial activity of these complexes is determined by well diffusion method against the target microorganisms- Staphylococcus aureus, Xanthomonas campestris, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. The antimicrobial activities of 2- hydroxy-1,4-naphthalenedione-1-oximes and their complexes are compared. It is observed that 2-hydroxy-1,4-naphthalenedione-l-oximes exhibit higher antifungal activity as compared to antibacterial activity. These activities are reduced upon complexation of these oximes with Erbium.
TL;DR: Reports of radioprotection, which involves treatment before irradiation, with calcium-channel blockers, acyl Melatonin homologs, and substituted anilines, as well as Curcumin, which is a chelating agent, are included to suggest additional approaches to combination treatments that may be useful in facilitating radiation recovery.
Abstract: Treatment with essential metalloelement (Cu, Fe, Mn, and Zn) chelates or combinations of them before and/or after radiation injury is a useful approach to overcoming radiation injury. No other agents are known to increase survival when they are used to treat after irradiation, in a radiorecovery treatment paradigm. These chelates may be useful in facilitating de novo syntheses of essential metalloelement-dependent enzymes required to repair radiation injury. Reports of radioprotection, which involves treatment before irradiation, with calcium-channel blockers, acyl Melatonin homologs, and substituted anilines, which may serve as chelating agents after biochemical modification in vivo, as well as Curcumin, which is a chelating agent, have been included in this review. These inclusions are intended to suggest additional approaches to combination treatments that may be useful in facilitating radiation recovery. These approaches to radioprotection and radiorecovery offer promise in facilitating recovery from radiation-induced injury experienced by patients undergoing radiotherapy for neoplastic disease and by individuals who experience environmental, occupational, or accidental exposure to ultraviolet, x-ray, or γ-ray radiation. Since there are no existing treatments of radiation-injury intended to facilitate tissue repair, studies of essential metalloelement chelates and combinations of them, as well as combinations of them with existing organic radioprotectants, seem worthwhile.
TL;DR: The compatibility of the substituted boranophosphates with common protecting groups is demonstrated and the α-borano triphosphates are good substrates for DNA polymerases and incorporation of boranophile into DNA causes an increase in the resistance to exo- and endonucleases.
Abstract: Tetraethyldicyanoborane pyrophosphate (2) and 3'-(diethylphosphite-cyanoborano)-5'-dimethoxytrityl.N4-benzoyl-deoxycytidine (3) have been synthesized in 70% and 76% yields, respectively. The compatibility of the substituted boranophosphates with common protecting groups is hereby demonstrated.
Boron containing biologically active compounds, such as nucleosides and nucleotides 1-6 and amino acids 7-9 are important due to their potential therapeutic activity, research and diagnostic applications. Many boron containing compounds have shown promising activity as anticancer, 10. 11. 12 antiinflammatory,13 and antiosteoporotic 13agents. Oligonucleotdes in which a non-bridging oxygen atom is replaced by a borane(BH3) group are a very important class of modified nucleic acids. 1. 3. 14-16 The BH3 group is isoelectronic with oxygen in natural oligonucleotides and isoelectronic and isostructural with the oligonucleotide methyl phosphonates, which are nuclease resistant. On the other hand, the α-borano triphosphates are good substrates for DNA polymerases and incorporation of boranophosphates into DNA causes an increase in the resistance to exo- and endonucleases 2. 17a as compared to non-modified DNA. There are also notable applications of the α-borano triphosphates in PCR sequencing 17a and nucleic acid detection 17b.
TL;DR: Some ruthenium (II) polypyridyl complexes with a bis-chalcone (obtained by the condensation of 3-methyl-thiophene-2-carboxaldehyde and 4-acetyl pyridine) have been synthesized and characterized spectroscopically (IR, NMR, UV/Vis), conductimetric, elemental analysis and FAB mass data.
Abstract: Some ruthenium (II) polypyridyl complexes with a bis-chalcone (obtained by the condensation of 3-methyl-thiophene-2-carboxaldehyde and 4-acetyl pyridine) have been synthesized and characterized spectroscopically (IR, NMR, UV/Vis), conductimetric, elemental analysis and FAB mass data. Their luminescent, redox and Li(+) binding properties have been studied. The anti-HIV and antitumour activities have also been reported.
TL;DR: The Schiff bases and their complexes with different anions were tested for their antibacterial activity against bacterial species such as Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa andKlebsiella pneumonae.
Abstract: Acylhydrazine derived furanyl and thienyl Schiff bases and their Cu(II) complexes have been prepared and characterized on the basis of their physical, spectral and analytical data. The preferred enolic form of the Schiff base function as a tetradentate ligand during coordination to the metal ion yielding a square planar complex. The Schiff bases and their complexes with different anions were tested for their antibacterial activity against bacterial species such as Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa andKlebsiella pneumonae.
TL;DR: While the Gram-positive bacteria were all readily inhibited, Bacillus subtilis (+) appeared to the most susceptible among them towards the test compounds, and their inhibitory activity ranked in the order 2 > 3 >1.
Abstract: Bacterial screening employing the agar diffusion test on triphenyltin carboxylates containing various functional residues in the ester moiety revealed appreciable differences in their activities relative to triphenyltin acetate. Among these, [3-(Diethylphosphono)propionato] triphenyltin (1) and [N-cyclohexylcarbamoyl) glycinato] triphenyltin displayed activities comparable to tri-n-butyltin cinnamate (2) towards both Gram-positive and Gram-negative bacteria; the latter compound was the most active among the eleven triorganotin compounds tested, which included cyclopentyldiphenyltin hydroxide (3) and its methacrylate derivative. Applying the more quantitative plate count and optical density tests on compounds 1-3, it was shown that their inhibitory activity ranked in the order 2 > 3 >1. Significantly, 3 caused around 90% inhibition of both Eschechia coli (−) and Pseudomonas aeruginosa (−) when incubated for 24 h at 37±1℃ at the 10.0 μg/ mL concentration level. Compound 2 was less effective against P.aeruginosa than against E.coli. While the Gram-positive bacteria were all readily inhibited, Bacillus subtilis (+) appeared to the most susceptible among them towards the test compounds.
TL;DR: The synthesized and characterized new binary and ternary complexes of Pd(II) of formulae cis-(pen)2PdCl2 and cis,[(nucl) 2Pd( pen)2]Cl2, where nucl = guanosine, inosine, cytidine or penciclovir, and all the prepared complexes were markedly active against HSV-1 andHSV-2 strains.
Abstract: With the aim to improve and extend the antiviral activity of the antiherpic drug penciclovir, to a wider spectrum of viruses, we have synthesized and characterized new binary and ternary complexes of Pd(II) of formulae cis- ( pen ) 2 Pd Cl 2 and cis,[ ( nucl ) 2 Pd ( pen ) 2 ] Cl 2 , where nucl = guanosine, inosine, cytidine or penciclovir. The characterization was mainly based on IR and H 1 NMR spectroscopy, and the results showed that in all prepared complexes, penciclovir coordinates to the metal through N7. The far-i.r. spectrum of the complex cis- ( pen ) 2 Pd Cl 2 confirmed the cis- geometry around Pd(II). All the prepared complexes were markedly active against HSV-1 and HSV-2 strains, but not against thymidine kinase-deficient HSV-1 strains.
TL;DR: The preparation and characterization of two triorganophosphinegold(I) complexes containing the anion derived from thiobenzoic acid are described and the cytotoxicity of these complexes has been investigated against a variety of human cell lines.
Abstract: The preparation and characterization of two triorganophosphinegold(I) complexes containing the anion derived from thiobenzoic acid are described. The cytotoxicity of these complexes has been investigated along with that of triphenylphosphinegold(I) mercaptopurinate, a known anti-tumor compound, against a variety of human cell lines. The complexes showed moderate to high cytotoxicity (ID50 250 – 2500 ng/ml).
TL;DR: Six new N-substituted di- and tributyltin 2-aminoethanethiolates (cysteaminates) have been prepared and characterised by 1H, 13C and 119Sn NMR spectroscopy and their activity is comparable with that of some antifungal drugs commonly used in the clinical use like ketoconazole.
Abstract: Six new N-substituted di- and tributyltin 2-aminoethanethiolates (cysteaminates) have been prepared and characterised by 1H, 13C and 119Sn NMR spectroscopy. All these compounds exhibit a good in vitro antifungal effect against selected types of human pathogenic fungi (Candida albicans, Candida krusei, Candida tropicalis, Candida glabrata, Trichosporon beigelii, Aspergillus fumigatus, Absidia corymbifera, Trichophyton mentagrophytes) and their activity is comparable with that of some antifungal drugs commonly used in the clinical use like ketoconazole. The structure-activity relationships in these compounds are discussed.
TL;DR: The results suggested that copper aspirinate inhibited platelet-neutrophil adhesion and resulted in a more potent antithrombotic activity.
Abstract: Antithrombotic effect of the copper-aspirin complex (dimeric copper(II) bis(o-acetoxybenzoate) was evaluated in the model of venous thrombosis; its effects on platelet-neutrophil adhesion were investigated by use of rosette assay. The results showed that the intragastrically administered copper-aspirin complex (5, 7, and 10 mg kg(-1)) dose-dependently lowered the wet and dry thrombus weight; it significantly decreased the binding of arachidonic acid-activated platelets to neutrophils with an IC(50) value of 41.5 mumol L(-1). The results suggested that copper aspirinate inhibited platelet-neutrophil adhesion and resulted in a more potent antithrombotic activity.
TL;DR: The cytotoxicity of four Co(III) complexes of arginine on nontumour MDBK cells and on two cell lines derived from transplantable tumors, LSCC-SF(Mc29) and LSR-SF (SR), was evaluated comparative!y.
Abstract: The cytotoxicity of four Co(III) complexes of arginine on nontumour MDBK cells and on two cell lines derived from transplantable tumors, LSCC-SF(Mc29) and LSR-SF (SR), was evaluated comparative!y. Based on the cytotoxic concentration required to inhibit cell surveillance by 50% ( CC 50 ) it was found that: (i) the cytotoxicity of complexes tested increases when the concentration decreased; (ii) the cell surveillance depends on both complex and cell specificities. The complex specificity was illustrated by the order 1 > 4 > 2 ≥ 3 . The cell specific response was demonstrated by the fact that LSCC-SG (Mc29) cells were up to 60 times more sensitive to 1 while LSR-SF (SR) cells were up to 1000 times more sensitive to 2 as compared to MDBK cells. Furthermore, with the prolongation of action on nontumour cells the cytotoxicity of 4 decreased up to 300 times while for both tumour cells it was independent on the duration of action.
TL;DR: Here, the influence of the inert ligands of the platinum(II) complex and of the nucleotide residues in the vicinity of the adduct on the rearrangement reaction is studied and the relevance of platinated oligonucleotides as potent and specific drugs is discussed.
Abstract: When an oligonucleotide containing a 1,3-(G,G)-transplatin cross-link at a GNG site (N represents a C, T, A or U residue) is paired with its complementary strand, the intrastrand adduct rearranges into an interstrand cross-link, resulting in the covalent attachment of both strands. Here, we have studied the influence of the inert ligands of the platinum(II) complex and of the nucleotide residues in the vicinity of the adduct on the rearrangement reaction. Dramatic effects on the linkage isomerization rate could be 37℃. The results are analyzed in relation with the mechanism of rearrangement of the 1,3-intrastrand adducts into interstrand cross-links. The relevance of platinated oligonucleotides as potent and specific drugs is discussed.