RESUMO
Inorganic medicinal compounds represent a unique and versatile source of potential therapeutics in many diseases and, more recently, in neurodegeneration. Herein we investigated the effects of two η6-arene Ru(II) complexes on the self-aggregation processes of several amyloidogenic peptides endowed with different kinetics and primary sequences. The Ru(II) complexes exhibit, around the metal ion, two chlorides, one NHC = N-heterocyclic carbene, with a glucosyl and a methyl substituent and separately a hexamethylbenzene, which is named Ru1, and one benzene, named Ru2. Both complexes were demonstrated to bind monomeric amyloids suppressing aggregation as evidenced in thioflavin T (ThT) binding assays and autofluorescence experiments. Electrospray ionization mass spectrometry (ESI-MS) indicated the formation of direct adducts between amyloid and metal complexes, which determined the marked conformational variation of peptides and a rescue of cellular viability in SH-SY5Y cells. The complex Ru2 was demonstrated to be a more potent inhibitor of amyloid aggregation compared to Ru1 likely because of the less hindrance of the arene moiety. The presented data strongly support the in vitro ability of η6-arene Ru(II) complexes to suppress amyloid aggregation, providing insights into their potential application as novel therapeutics in neurodegenerative diseases.
Assuntos
Complexos de Coordenação , Agregados Proteicos , Rutênio , Humanos , Complexos de Coordenação/farmacologia , Complexos de Coordenação/química , Complexos de Coordenação/síntese química , Rutênio/química , Rutênio/farmacologia , Agregados Proteicos/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Amiloide/antagonistas & inibidores , Amiloide/metabolismo , Amiloide/química , Linhagem Celular Tumoral , Estrutura MolecularRESUMO
This article presents a thorough investigation into the synthesis of trimethylolpropane triacrylate (TMPTA) via the esterification reaction of trimethylolpropane (TMP) with acrylic acid using Amberlite™ 120 IR (H+), Amberlyst® 15, and Dowex™ 50WX8 resins as heterogeneous catalysts. Preliminary comparative tests explored the impact of air flow on water removal during the reaction and different acid-to-alcohol molar ratios (3:1, 6:1, or 9:1 mol:mol). The findings revealed that introducing air significantly enhances TMPTA yield and -OH group conversion, particularly at a 6:1 acid-to-alcohol molar ratio. Based on cost considerations, Amberlite™ 120 IR (H+) was selected as the preferred catalyst for further optimization. This included evaluating the effect of catalyst loading (10%, 5.0%, and 2.5% w/wtot) and assessing the impact of a pre-drying process on resin efficiency. The study concluded that optimal conditions did not necessitate drying, requiring 120 °C, a catalyst loading of 10% w/wtot, a 4 h reaction time, an acid:alcohol ratio of 6:1 mol:mol, the presence of MEHQ (0.1% mol/molAA), and air bubbling at 6 ± 1 Nl/h. Catalyst recycling was effectively implemented with a slight reduction in catalytic activity over consecutive runs. Furthermore, the study explored a scaled-up system with a mechanical stirrer, demonstrating the potential for multi-hundred grams scale-up. Considerations for optimizing the air flow stripping system are also highlighted. In summary, this study provides valuable insights into designing and optimizing the esterification process for TMPTA synthesis, laying the foundation for potential industrial applications.
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Platinum complexes are ubiquitous in chemistry and largely used as catalysts or as precursors in drug chemistry, thus a deep knowledge of their electronic properties may help in planning new synthetic strategies or exploring new potential applications. Herein, the electronic structure of many octahedral platinum complexes is drastically revised especially when they feature electronegative elements such as halogens and chalcogens. The investigation revealed that in most cases the five d platinum orbitals are invariably full, thus the empty antibonding orbitals, usually localized on the metal, are mainly centered on the ligands, suggesting a questionable assignment of formal oxidation state IV. The analysis supports the occurrence of the inverted ligand field theory in all cases with the only exceptions of the Pt-F and Pt-O bonding. The trends for the molecular complexes are mirrored also by the density of states plots of extended structures featuring octahedral platinum moieties in association with chalcogens atoms. Finally, the oxidative addition of a Se-Cl linkage to a square platinum complex to achieve an octahedral moiety has been revised in the framework of the inverted ligand field.
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This study describes new platinum(II) cationic five-coordinate complexes (1-R,R') of the formula [PtR(NHC)(dmphen)(ethene)]CF3SO3 (dmphen = 2,9-dimethyl-1,10-phenanthroline), containing in their axial positions an alkyl group R (methyl or octyl) and an imidazole-based NHC-carbene ligand with a substituent R' of variable length (methyl or octyl) on one nitrogen atom. The Pt-carbene bond is stable both in DMSO and in aqueous solvents. In DMSO, a gradual substitution of dmphen and ethene is observed, with the formation of a square planar solvated species. Octanol/water partitioning studies have revealed the order of hydrophobicity of the complexes (1-Oct,Me > 1-Oct,Oct > 1-Me,Oct > 1-Me,Me). Their biological activity was investigated against two pairs of cancer and non-cancer cell lines. The tested drugs were internalized in cancer cells and able to activate the apoptotic pathway. The reactivity of 1-Me,Me with DNA and protein model systems was also studied using UV-vis absorption spectroscopy, fluorescence, and X-ray crystallography. The compound binds DNA and interacts in various ways with the model protein lysozyme. Remarkably, structural data revealed that the complex can bind lysozyme via non-covalent interactions, retaining its five-coordinate geometry.
Assuntos
Antineoplásicos , Muramidase , Antineoplásicos/farmacologia , Antineoplásicos/química , Cristalografia por Raios X , Dimetil Sulfóxido , DNA , Interações Hidrofóbicas e Hidrofílicas , Compostos de Platina/química , Compostos de Platina/farmacologiaRESUMO
Neurodegenerative diseases are often caused by uncontrolled amyloid aggregation. Hence, many drug discovery processes are oriented to evaluate new compounds that are able to modulate self-recognition mechanisms. Herein, two related glycoconjugate pentacoordinate Pt(II) complexes were analyzed in their capacity to affect the self-aggregation processes of two amyloidogenic fragments, Aß21-40 and Aß25-35, of the C-terminal region of the ß-amyloid (Aß) peptide, the major component of Alzheimer's disease (AD) neuronal plaques. The most water-soluble complex, 1Ptdep, is able to bind both fragments and to deeply influence the morphology of peptide aggregates. Thioflavin T (ThT) binding assays, electrospray ionization mass spectrometry (ESI-MS), and ultraviolet-visible (UV-vis) absorption spectroscopy indicated that 1Ptdep shows different kinetics and mechanisms of inhibition toward the two sequences and demonstrated that the peptide aggregation inhibition is associated with a direct coordinative bond of the compound metal center to the peptides. These data support the in vitro ability of pentacoordinate Pt(II) complexes to inhibit the formation of amyloid aggregates and pave the way for the application of this class of compounds as potential neurotherapeutics.
Assuntos
Peptídeos beta-AmiloidesRESUMO
The catalytic properties of a simple iron-containing MOF based on fumaric acid, MIL-88A, were investigated in the ketalization of ethyl levulinate with glycerol. The corresponding product is a component of current interest as a renewable building block for many uses. Under the following conditions (solventless, 120 °C, stoichiometric ratio, 1% cat.), the reaction proceeds with good yields (85%), and the catalyst can be recovered and recycled without loss of activity, despite some changes in the crystalline lattice and morphology. Moreover, the residual iron content in the product is in the order of units of ppm (≤2), which demonstrates the robustness of the MOF under the reaction conditions.
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Estruturas Metalorgânicas , Catálise , Glicerol , Ferro/química , Estruturas Metalorgânicas/químicaRESUMO
A lignin fraction (LF) was extracted from the sea balls of Posidonia oceanica (egagropili) and extensively dialyzed and characterized by FT-IR and NMR analyses. LF resulted water soluble and exhibited a brownish-to-black color with the highest absorbance in the range of 250-400 nm, attributed to the chromophore functional groups present in the phenylpropane-based polymer. LF high-performance size exclusion chromatography analysis showed a highly represented (98.77%) species of 34.75 kDa molecular weight with a polydispersity index of 1.10 and an intrinsic viscosity of 0.15. Quantitative analysis of carbohydrates indicated that they represented 28.3% of the dry weight of the untreated egagropili fibers and 72.5% of that of LF. In particular, eight different monosaccharides were detected (fucose, arabinose, rhamnose, galactose, glucose, xylose, glucosamine and glucuronic acid), glucuronic acid (46.6%) and rhamnose (29.6%) being the most present monosaccharides in the LF. Almost all the phenol content of LF (113.85 ± 5.87 mg gallic acid eq/g of extract) was water soluble, whereas around 22% of it consisted of flavonoids and only 10% of the flavonoids consisted of anthocyanins. Therefore, LF isolated from egagropili lignocellulosic material could be defined as a water-soluble lignin/carbohydrate complex (LCC) formed by a phenol polymeric chain covalently bound to hemicellulose fragments. LCC exhibited a remarkable antioxidant activity that remained quite stable during 6 months and could be easily incorporated into a protein-based film and released from the latter overtime. These findings suggest egagropili LCC as a suitable candidate as an antioxidant additive for the reinforcement of packaging of foods with high susceptibility to be deteriorated in aerobic conditions.
Assuntos
Alismatales/química , Antioxidantes/química , Lignina/química , Monossacarídeos/química , Extratos Vegetais/química , Ácido Gálico/química , Glucosamina/química , Fenóis/química , Proteínas/química , ViscosidadeRESUMO
This article describes the synthesis, characterization, and biological activity of novel square-planar cationic platinum(II) complexes containing glucoconjugated triazole ligands and a comparison with the results obtained from the corresponding five-coordinate complexes bearing the same triazole ligands. Stability in solution, reactivity with DNA and small molecules of the new compounds were evaluated by NMR, fluorescence, and UV-vis absorption spectroscopy, together with their cytotoxic action against pairs of immortalized and tumorigenic cell lines. The results show that the square-planar species exhibit greater stability than the corresponding five-coordinate ones. Furthermore, although the square-planar complexes are less cytotoxic than the latter ones, they exhibit a certain selectivity. These results simultaneously demonstrate that overall stability is a fundamental prerequisite for preserving the performance of the agents and that coordinative saturation constitutes a point in favor of their biological action.
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Antineoplásicos/síntese química , Glucose/química , Compostos Organoplatínicos/síntese química , Triazóis/química , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Ligantes , Células MCF-7 , Estrutura Molecular , Compostos Organoplatínicos/química , Compostos Organoplatínicos/farmacologia , Espectroscopia de Prótons por Ressonância Magnética , RatosRESUMO
Octahedral Pt(IV) complexes (2Pt-R) containing a glycoconjugate carbene ligand were prepared and fully characterized. These complexes are structural analogues to the trigonal bipyramidal Pt(II) species (1Pt-R) recently described. Thus, an unprecedented direct comparison between the biological properties of Pt compounds with different oxidation states and almost indistinguishable structural features was performed. The stability profile of the novel Pt(IV) compounds in reference solvents was determined and compared to that of the analogous Pt(II) complexes. The uptake and antiproliferative activities of 2Pt-R and 1Pt-R were evaluated on the same panel of cell lines. DNA and protein binding properties were assessed using human serum albumin, the model protein hen egg white lysozyme, and double stranded DNA model systems by a variety of experimental techniques, including UV-vis absorption spectroscopy, fluorescence, circular dichroism, and electrospray ionization mass spectrometry. Although the compounds present similar structures, their in-solution stability, cellular uptake, and DNA binding properties are diverse. These differences may represent the basis of their different cytotoxicity and biological activity.
Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Glicoconjugados/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/metabolismo , Bovinos , Linhagem Celular Tumoral , Galinhas , Complexos de Coordenação/síntese química , Complexos de Coordenação/metabolismo , DNA/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Glicoconjugados/síntese química , Glicoconjugados/metabolismo , Humanos , Ligantes , Camundongos , Estrutura Molecular , Muramidase/metabolismo , Platina/química , Ligação Proteica , Albumina Sérica Humana/metabolismoRESUMO
The design of novel metal complexes with N-heterocyclic carbene (NHC) ligands that display biological activity is an active research field in organometallic chemistry. One of the possible approaches consists of the use of NHC ligands functionalized with a carbohydrate moiety. Two novel Au(I)-Au(I) dinuclear complexes were synthesized; they present a neutral structure with one bridging diNHC ligand, having one or both heterocyclic rings decorated with a carbohydrate functionality. With the symmetric diNHC ligand, the dicationic dinuclear complex bearing two bridging diNHC ligands was also synthesized. The study was completed by analyzing the antiproliferative properties of these complexes, which were compared to the activity displayed by similar mononuclear Au(I) complexes and by the analogous bimetallic Au(I)-Au(I) complex not functionalized with carbohydrates.
Assuntos
Antineoplásicos , Proliferação de Células/efeitos dos fármacos , Ouro/química , Compostos Heterocíclicos , Neoplasias/tratamento farmacológico , Compostos Organoáuricos , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Células 3T3 BALB , Linhagem Celular Tumoral , Compostos Heterocíclicos/síntese química , Compostos Heterocíclicos/química , Compostos Heterocíclicos/farmacologia , Humanos , Camundongos , Neoplasias/metabolismo , Neoplasias/patologia , Compostos Organoáuricos/síntese química , Compostos Organoáuricos/química , Compostos Organoáuricos/farmacologiaRESUMO
The RuIII-based prodrug AziRu efficiently binds to proteins, but the mechanism of its release is still disputed. Herein, in order to test the hypothesis of a reduction-mediated Ru release from proteins, a Raman-assisted crystallographic study on AziRu binding to a model protein (hen egg white lysozyme), in two different oxidation states, RuII and RuIII, was carried out. Our results indicate Ru reduction, but the Ru release upon reduction is dependent on the reducing agent. To better understand this process, a pH-dependent, spectroelectrochemical surface-enhanced Raman scattering (SERS) study was performed also on AziRu-functionalized Au electrodes as a surrogate and simplest model system of RuII- and RuIII-based drugs. This SERS study provided a p Ka of 6.0 ± 0.4 for aquated AziRu in the RuIII state, which falls in the watershed range of pH values separating most cancer environments from their physiological counterparts. These experiments also indicate a dramatic shift of the redox potential E0 by >600 mV of aquated AziRu toward more positive potentials upon acidification, suggesting a selective AziRu reduction in cancer lumen but not in healthy ones. It is expected that the nature of the ligands (e.g., pyridine vs imidazole, present in well-known RuIII complex NAMI-A) will modulate the p Ka and E0, without affecting the underlying reaction mechanism.
Assuntos
Muramidase/química , Pró-Fármacos/química , Rutênio/química , Sítios de Ligação , Concentração de Íons de Hidrogênio , Estrutura Molecular , Muramidase/metabolismo , Pró-Fármacos/síntese químicaRESUMO
Stable five-coordinate Pt(II) complexes have been highlighted as a promising and original platform for the development of new cytotoxic drugs. Their interaction with proteins has been scarcely studied. Here, the reactivity of the five-coordinate Pt(II) compound [Pt(I)(Me) (dmphen)(olefin)] (Me = methyl, dmphen = 2,9-dimethyl-1,10-phenanthroline, olefin = dimethylfumarate) with the model proteins hen egg white lysozyme (HEWL) and bovine pancreatic ribonuclease (RNase A) has been investigated by X-ray crystallography and electrospray ionization mass spectrometry. The X-ray structures of the adducts of RNase A and HEWL with [Pt(I)(Me)(dmphen)(olefin)] are not of very high quality, but overall data indicate that, upon reaction with RNase A, the compound coordinates the side chain of His105 upon releasing the iodide ligand, but retains the pentacoordination. On the contrary, upon reaction with HEWL, the trigonal bi-pyramidal Pt geometry is lost, the iodide and the olefin ligands are released, and the metal center coordinates the side chain of His15 probably adopting a nearly square-planar geometry. This work underlines the importance of the combined use of crystallographic and mass spectrometry techniques to characterize, in detail, the proteinâ»metallodrug recognition process. Our findings also suggest that five-coordinate Pt(II) complexes can act either retaining their uncommon structure or functioning as prodrugs, i.e., releasing square-planar platinum complexes as bioactive species.
Assuntos
Complexos de Coordenação/metabolismo , Muramidase/metabolismo , Platina/química , Ribonuclease Pancreático/metabolismo , Animais , Sítios de Ligação , Bovinos , Complexos de Coordenação/química , Cristalografia por Raios X , Espectrometria de Massas , Modelos Moleculares , Muramidase/química , Ligação Proteica , Conformação Proteica , Ribonuclease Pancreático/químicaRESUMO
This article describes the synthesis and characterization of novel cationic five-coordinate Pt(II) complexes containing nitrogen sugar-based ligands. The cytotoxicity of the complexes was evaluated on different cell lines with the expectation that both the coordinative saturation and the sugar moiety cooperate to enhance their biological activity. In fact, the complexes resulted to be more active than cisplatin but still with little selectivity. They activate the apoptosis pathway. Binding of representative compounds with DNA was studied by ethidium bromide displacement assay and circular dichroism. Binding to model proteins was also investigated; the X-ray structure of the adduct formed in the reaction between a representative compound and the model protein bovine pancreatic ribonuclease was obtained. The structure discloses an unprecedented interaction between a five-coordinate Pt(II) moiety and a His side chain.
Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Glucosídeos/farmacologia , Platina/química , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Bovinos , Linhagem Celular Tumoral , Galinhas , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , DNA/química , Glucosídeos/síntese química , Glucosídeos/química , Histidina/química , Humanos , Substâncias Intercalantes/síntese química , Substâncias Intercalantes/química , Substâncias Intercalantes/farmacologia , Ligantes , Estrutura Molecular , Muramidase/química , Ratos , Ribonuclease Pancreático/químicaRESUMO
[Cp*Ir(R-pica)Cl] (Cp*=pentamethylcyclopentadienyl anion, pica=2-picolineamidate) complexes bearing carbohydrate substituents on the amide nitrogen atom (R=methyl-ß-D-gluco-pyranosid-2-yl, 1; methyl-3,4,6-tri-O-acetyl-ß-D-glucopyranosid-2-yl, 2) were tested as catalysts for formic acid dehydrogenation in water. TOFMAX values over 12000â h-1 and 50000â h-1 were achieved at 333â K for 1 and 2, respectively, with TON values over 35000 for both catalysts. Comparison with the simpler cyclohexyl-substituted analogue (3) indicated that glucosyl-based complexes are much better performing under the same experimental conditions (TOFMAX=5144â h-1, TON=5000 at pHâ 2.5 for 3) owing to a lower tendency to isomerize to the less active k2-N,O isomer upon protonation. The 5-fold increase in TOFMAX observed for 2 with respect to 1 is reasonably due to an optimal steric protection by the acetyl substituent, which may prevent unproductive inner-sphere reactivity. These results showcase a powerful strategy for the inhibition of the common deactivation pathways of [Cp*Ir(R-pica)X] catalysts for FA dehydrogenation, paving the way for the development of better performing hydrogen storage systems.
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In this work, the properties of a novel electrolyte based on the combination of bio-based Æ´-valerolactone (GVL) solvent with lithium bis(oxalato)borate (LiBOB) salt and its use for lithium-ion capacitors (LICs) are presented. It is shown that the 1 m LiBOB in GVL electrolyte displays good transport properties, high thermal stability, and the ability to prevent anodic dissolution. Its impact on the performance of both battery-type and capacitive-type electrodes is evaluated. In this regard, special attention is paid to the filming properties associated with LiBOB and GVL decomposition at the electrode surfaces. To the best of the authors' knowledge, the full-cell devices assembled in this study are the first example of a fluorine-free LIC. These devices exhibit a favorable energy-to-power ratio, delivering 80 Wh kg-1 AM at 10 000 W kg-1 AM along with excellent cycling stability, retaining 80% of the initial capacitance after 25 000 cycles. Furthermore, post-mortem analysis of the LIC electrodes is conducted to gain deeper insights into the degradation mechanisms within the device.
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In the title adduct, C15H10N4·2C10H10N2, the pyrimidine ring is nearly co-planar with the heteroatomic perimidine ring, as indicated dihedral angle between their mean planes of 3.21â (11)°. The di-aminona-phthalene mol-ecules are slightly twisted [dihedral angles = 4.2â (2) and 3.0â (2)°] because of the steric encumbrance of NH2 groups. The perimidine and di-aminona-phthalene mol-ecules are linked by N-Hâ¯N hydrogen bonds, forming an R (4) 4(12) graph-set motif across an inversion center. In the crystal, alternating layers of the perimidine and di-aminona-phthalene mol-ecules are formed along [100]. In the perimidine layer, mol-ecules are π-π stacked along the c-axis direction with an inter-plane separation of approximately 3.4â Å.
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In this work, γ-valerolactone (GVL), a green solvent based on largely available biomass (carbohydrates), highly biodegradable, and with low eco-toxicological profile, was used as electrolyte component in energy storage devices. This solvent allowed the realization of electrolytes with good transport properties and high thermal stability, which could be successfully applied in electrical double layer capacitors (EDLCs). GVL-based EDLCs could operate at 2.7-2.9â V and displayed good performance in term of capacitance, cycling stability, as well as specific energy and power. The results of this study indicate that the use of solvent obtained from largely available natural sources is a feasible strategy for the realization of sustainable and safe electrolytes for EDLCs.
Assuntos
Eletrólitos , Lactonas , Solventes , CarboidratosRESUMO
Neurodegenerative diseases are often characterized by the formation of aggregates of amyloidogenic peptides and proteins, facilitating the formation of neurofibrillary plaques. In this study, we investigate a series of Ru-complexes sharing three-legged piano-stool structures based on the arene ring and glucosylated carbene ligands. The ability of these complexes to bind amyloid His-peptides was evaluated by ESI-MS, and their effects on the aggregation process were investigated through ThT and Tyr fluorescence emission. The complexes were demonstrated to bind the amyloidogenic peptides even with different mechanisms and kinetics depending on the chemical nature of the ligands around the Ru(II) ion. TEM analysis detected the disaggregation of typical fibers caused by the presence of Ru-compounds. Overall, our results show that the Ru-complexes can modulate the aggregation of His-amyloids and can be conceived as good lead compounds in the field of novel anti-aggregating agents in neurodegeneration.
Assuntos
Antineoplásicos , Complexos de Coordenação , Rutênio , Estrutura Molecular , Antineoplásicos/química , Rutênio/farmacologia , Rutênio/química , Histidina , Ligantes , Peptídeos , Proteínas Amiloidogênicas , Complexos de Coordenação/químicaRESUMO
New neutral carbene complexes of gold(I) [Au(Im-Me)X] (X = Cl, Au1; X = Br, Au2; X = I, Au3) have been synthesized and fully characterized by different techniques, including NMR and UV-vis absorption spectroscopy and single crystal X-ray diffraction. The carbene ligand Im-Me is decorated with a glucoside fragment via a triazole linker, obtainable through a click chemistry reaction. The compounds retain the Au-NHC fragment in aqueous solvents, and an equilibrium between the neutral halo- and the cationic di-carbene form [Au(Im-Me)2]+ is observed, whose extent follows the trend Au1 < Au2 < Au3. Cytotoxicity studies on two cancer and two non-tumorigenic cell lines reflect the solution behavior, as a certain difference among the complexes was disclosed, with the iodo complex Au3 being more active and selective. The compounds interact with both DNA and protein model systems. The X-ray structure of the adduct formed upon the reaction of Au1 with bovine pancreatic ribonuclease (RNase A) reveals Au binding at the side chain of His105 of both protein molecules A and B of the asymmetric unit. The binding of gold atoms at both the nitrogen atoms of the imidazole ring of His15 and at the N-terminal tail has been found in the adduct formed with hen egg white lysozyme.
Assuntos
DNA , Ouro , Animais , Bovinos , Glicoconjugados/farmacologia , Ouro/química , Ligantes , Metano/análogos & derivados , Modelos MolecularesRESUMO
Three novel inosine-based dinuclear platinum complexes have been synthesized via a solid-phase strategy. In these compounds, the metal is linked both to the N-7 of the purine nucleus and to the terminal amine group of a hexylamine side chain installed on N-1. Cis- or trans- diamine as well as ethylenediamine ligands are coordinated to platinum along with a chloride. The synthesised complexes were tested against four different human tumor cell lines. One of these complexes proved to be more cytotoxic than cisplatin against the MCF7 cancer cell line in a short-term exposure assay.