New trends in platinum and palladium complexes as antineoplastic agents

The discovery of cisplatin (cis-Pt(NH3)2Cl2) as an antineoplastic agent has focused attention on the rational design of metal complexes that can be potentially used in cancer chemotherapy. Today, the pharmaceutical industry invests more than $1 billion each year in the development of new metal-based drugs to improve biological activities, in terms of cellular selectivity, therapeutic efficiency and minimization of side effects. Chemotherapies based on transition metals play a key role in cancer treatment, and among them platinum and palladium are the most fruitful. This article reviews the main recent advances in the design and synthesis of platinum- and palladium-based drugs, their structural features and biological studies of them. The rationale for the choice of the ligand, related to leaving groups, the geometry of the complex and the oxidation state of the metal ion, is discussed. An overview of the main biological techniques and approaches for testing the interaction of these molecules with the biological environment, mainly DNA, to validate the effect is also provided

A Metal-Based Receptor for Selective Coordination and Fluorescent Sensing of Chloride

A scorpionate Zn2+ complex, constituted by a macrocyclic pyridinophane core attached to a pendant arm containing a fluorescent pyridyl-oxadiazole-phenyl unit (PyPD), has been shown to selectively recognize chloride anions, giving rise to changes in fluorescence emission that are clearly visible under a 365 nm UV lamp. This recognition event has been studied by means of absorption, fluorescence, and NMR spectroscopy, and it involves the intramolecular displacement of the PyPD unit by chloride anions. Moreover, since the chromophore is not removed from the system after the recognition event, the fluorescence can readily be restored by elimination of the bound chloride anion

Synthesis and biological characterization of a new fluorescent probe for vesicular trafficking based on polyazamacrocycle derivative

The fluorescent probes represent an important tool in the biological study, in fact characterization of cellular structures and organelles are an important tool-target for understanding the mechanisms regulating most biological processes. Recently, a series of polyamino-macrocycles based on 1,4,7,10-tetraazacyclododecane was synthesized, bearing one or two NBD units (AJ2NBD·4HCl) useful as sensors for metal cations and halides able to target and to detect apolar environment, as lipid membranes. In this paper, we firstly illustrate the chemical synthesis of the AJ2NBD probe, its electronic absorption spectra and its behavior regarding pH of the environment. Lack of any cellular toxicity and an efficient labelling on fresh, living cells was demonstrated, allowing the use of AJ2NBD in biological studies. In particular, this green fluorescent probe may represent a potential dye for the compartments involved in the endosomal/autophagic pathway. This research's field should benefit from the use of AJ2NBD as a vesicular tracer, however, to ensure the precise nature of vesicles/vacuoles traced by this new probe, other more specific tests are needed

Pharmaceutical composition of [(3-​hydroxy-​4 -​pyron-​2-​yl) methyl] -​amine derivatives and DNA demethylating agents and their use as anti-​neoplastic drugs

The present invention concerns pharmaceutical compositions comprising compounds with general formula I or polyalkyl-bis- maltolic molecules and in particular derivatives of [(3-hydroxy-4- pyron-2-yl)methyl]-amine in combination with DNA demethylating agents as anti-neoplastic drugs. In particular, for the preparation of a medicament for the treatment of neoplastic pathologies

RADIONUCLIDES FOR BIOMEDICAL USES: AN APPLICATION PROPOSAL WITH 64Cu

In this proposal has been developed a prototype of radiopharmaceutical based on the radioactive isotope 64Cu, designed for theranostic applications in medical field. This radiopharmaceutical was designed analysing previous results and considering the fundamental characteristics that it must has. A radiopharmaceutical based on 64Cu, since is consisting of this radionuclide, could be used in a diagnostic field (PET and SPECT): that because the radioisotope copper-64 shows medium-long half life (12,7 h), interesting decay (β+ and β− emitter) without abundant gamma emission and it can be produced quickly in large quantities. After the radiopharmaceutical administration, the radioisotope will emit radiations that will be taken over by special tools named tomographers and elaborated to obtain an image of the organism spacetime distribution of the radiolabelled substance; in addition, the emitting particles could be of aid in therapy when the radioisotope is opportunely distributed

Derivative of [(3-hydroxy-4-pyron-2-yl)-methyl]-amine and use thereof as anti-neoplastic drugs

The present invention relates to compounds heaving general formula (I), i.e. poly-alkyl-bis-maltolic molecules and in particular to derivates of [(3-hydroxy-4-pyron-2-yl)methyl]-amine and pharmaceutically accetable salts thereof, and to the use thereof as anti-neoplastic drugs, in particular, for a preparation of a medicament for the treatment of neoplastic disease

Pharmaceutical composition of [(3-​hydroxy-​4 -​pyron-​2-​yl) methyl] -​amine derivatives and DNA demethylating agents and their use as anti-​neoplastic drugs

The present invention concerns pharmaceutical compositions comprising compounds with general formula I or polyalkyl-bis- maltolic molecules and in particular derivatives of [(3-hydroxy-4- pyron-2-yl)methyl]-amine in combination with DNA demethylating agents as anti-neoplastic drugs. In particular, for the preparation of a medicament for the treatment of neoplastic pathologies

Chimica. Principi generali con esercizi

Un libro realizzato come testo per il primo corso di chimica presente nei vari Corsi di Laurea del nostro sistema universitario. Sono trattati i principi generali alla base della chimica che devono essere bagaglio imprescindibile per uno studente che affronta un qualsiasi percorso di laurea scientifica dal futuro chimico al biologo, dal geologo al biotecnologo, dal nutrizionista al medico, dall’ingegnere al farmacista, dall’agronomo al fisico e così via. Ad integrazione di questi principi, e per facilitare la verifica da parte dello studente della comprensione degli argomenti trattati, sono stati inseriti alla fine di ogni capitolo sia un paragrafo concernente gli obiettivi minimi che dovrebbero essere acquisiti sia una serie di domande di autovalutazione con le quali lo studente può valutare il proprio grado di preparazione. Nel libro è inclusa la stechiometria, cioè quel ramo della chimica che si occupa delle relazioni quantitative nelle trasformazioni chimiche, necessaria per una corretta comprensione di molti degli argomenti trattati e per la loro applicazione reale. Questa è stata sviluppata inserendo, nei capitoli interessati, un’ampia casistica per la risoluzione guidata degli esercizi e una serie di esercizi non risolti per i quali sono state riportate le soluzioni a fine testo. La presenza della parte stechiometrica permette al libro di essere adottato come testo unico in qualsiasi primo corso di chimica di livello universitario