DNA and BSA binding, anticancer and antimicrobial properties of Co(II), Co(II/III), Cu(II) and Ag(I) complexes of arylhydrazones of barbituric acid

Two new cocrystalline compounds, (Hen)(H2L2)$2/3H2O (2) and (Him)(H3L3)$2H2O (8), were prepared by the reaction of 5-(2-(4-chlorophenyl)hydrazono)pyrimidine-2,4,6(1H,3H,5H)-trione (H3L2) and the sodium salt of 2-(2-(2,4,6-trioxotetrahydropyrimidin-5(2H)-ylidene)hydrazinyl)benzenesulfonic acid (H4L3), [Na(H3L3)(m-H2O)(H2O)2]2 (1) with protonated ethylenediamine (Hen) and imidazole (Him), respectively. By using 5-(2-(2-hydroxyphenyl)hydrazono)pyrimidine-2,4,6(1H,3H,5H)-trione (H4L1) and 1, several known CuII, CoII, CoII/III and new AgI complexes, [Cu(H2L1)(H2O)(im)]$3H2O (3), [Co(H2O)6]- [Co(H2L1)2]2$8H2O (4), [Co(H2L3)(im)3] (5), [Cu(H2L3)(im)2]$H2O (6), [Ag(H2O)(m-H3L3)]n (7) and [Co(H2O)6]- [H3L3]2$8H2O (9), were also prepared in order to study their DNA and BSA binding, anticancer and antimicrobial properties. The complexes are able to interact with DNA and BSA with high binding constant values. In particular, complex 4 strongly intercalates DNA and binds BSA. The antimicrobial activity of all compounds, determined against a panel of reference bacterial and fungal strains, indicates that only 2 and 7 possess antimicrobial activity. The same compounds 2 and 7 show a pronounced antiproliferative activity against the human tumor cell lines A375, MDA-MB 231 and HCT116

Novel Silver Complexes as Additives for Innovative Composite Materials with Permanent Antimicrobial Activity

In summary, most of the experimental work of my PhD thesis has been devoted to develop novel silver complexes with suitable physico-chemical properties for their employment as additives in antimicrobial composite materials with persistent activity. Among the most relevant results, the silver coordination polymers seem to be the most effective for their application as additives, due to their high and broad spectrum antimicrobial activity. Such activity is persistent in time, likely because of a contact mechanism of toxicity against bacteria, due to exposed silver centers within the polynuclear chain, which are able to attract the negatively charged cell membranes of bacteria altering their membrane potential and provoking their death. In any case, the release of silver ions from the composite material seems very limited or absent, thanks to the insolubility of such silver coordination polymers in almost all solvents and water, an essential feature for their application as additives for plastics. Future developments of this research will be directed to optimize the homogeneity of the composites’ surfaces by changing the substituents in the HQR proligands with the aim of increasing their hydrophobicity and solubility in the polymeric matrices

Silver(I) Acylpyrazolonate Complexes embedded in High Density Polyethylene or in polyvinyl chloride with Potent Antibacterial Activity

Composite plastics, containing silver(I) acylpyrazolonate complexes embedded in high density polyethylene or polyvinyl chloride, display potent antibacterial activity by contact, without silver ions release

Novel polyethylene-embedded silver(I) acylpirazolonate complexes with potent antibacterial activity.

Novel polyethylene-embedded silver(I) acylpirazolonate complexes with potent antibacterial activity

Synthesis and Characterization of New Ruthenium(II) Arene Acylpyrazolone Complexes

Arene ruthenium(II) complexes have been widely studied in the recent years, and their chemistry has been extensively studied for arenes such as benzene and para-cymene. They have found applications in catalysis, supramolecular assemblies, molecular devices.1 Moreover, they have shown antiviral, antibiotic and anticancer activities.2 Recently, mononuclear Ru-acylpyrazolone complexes have been shown to exhibit interesting in vitro activity in some cancer cells.3 On the basis of the our previous work,4 we extend our investigation to the interaction of several acylpyrazolones ligands with (arene)ruthenium(II)dichloride acceptors and PTA (1,3,5-triaza-7-phosphaadamantane)(Figure 1). Their structures have been confirmed by analytical and spectral data. X-ray diffraction studies and their biological activity are under investigation

Bioactivity of Curcuminoids in Half-Sandwich Ru(II), Rh(III) and Ir(III) Complexes: benefits from cooking to medicine

Curcumin has been used for centuries in Asia as a spice, natural colouring and traditional medicine owing to its anti-inflammatory, antioxidant and antitumoral effects [1]. An alternative strategy to improve the properties of curcumin, without the need to modify the drug, is its incorporation into metal complexes [2]. Ruthenium compounds have emerged in recent years as promising alternatives to platinum drugs by displaying specific activities against different cancers, favorable toxicity and clearance properties [3]. Recently, also metal complexes based on Rhodium and Iridium have arisen as fascinating potential alternative metallodrugs [4]. In the present work we exploit the coordination chemistry of Ru(II) arene and pentamethylcyclopentadienyl Rh(III) and Ir(III) complexes with curcumin [5] and bisdemethoxycurcumin as co-ligands and full characterization of relative RAPTA type complexes with 1,3,5-triaza-7-phosphaadamantane ligand (PTA) [6]. Hydrolysis studies were carried out under pseudopharmacological conditions to evaluate their aqueous chemistry. The antiproliferative effects in two human ovarian cancer cell lines (A2780 and A2780cisR) and non-tumorigenic human embryonic kidney cells (HEK293) will be reported

EUCHEME, EUropean CHemists for Energy, Materials and Environment. Intensive Programme (IP) Lifelong Learning Programme Erasmus

The main objective of the course is to provide a comprehensive and balanced overview of the most important aspects of different subjects (energy and materials production, fine chemicals, environment) related to organometallic chemistry, catalysis, advanced materials, green and environmental chemistry, bridging the gap between the need of advanced training and the actual offer in this fields

Synthesis, Characterization and Bioactivity of Novel Pentamethylcyclopentadienyl Rh(III) and Ir(III) Complexes Containing Dibenzoylmethane

Organometallic complexes play a key role in medicinal chemistry, especially in the development of anticancer therapies [1]. Among this class of inorganic compounds Rhodium and Iridium complexes are recently attracting an increasing interest in treatment of cancer since they possess several features that make them appealing alternative metallodrugs [2]. Dibenzoylmethane is a natural β-diketone that can be found in small amount in licorice roots. It possesses biological activity against different kind of cancer such as skin, prostate, lung and mammary tumors, lymphomas and leukemia [3]. Pentamethylcyclopentadienyl Rh(III) and Ir(III) complexes bearing dibenzoylmethane and their respective derivatives with PTA (1,3,5-triaza-7- phosphaadamantane) have been synthetized and fully characterized. Preliminary results on their biological and biochemical activity will also be reported