Analysis of organic polymorphs. A review

Vanadium compounds in medicine.

Coordination chemistry of vanadium in metallopharmaceutical candidate compounds

Radiometals possess an exceptional breadth of decay properties and have been applied to medicine with great success for several decades. The majority of current clinical use involves diagnostic procedures, which use either positron-emission tomography (PET) or single-photon imaging to detect anatomic abnormalities that are difficult to visualize using conventional imaging techniques (e.g., MRI and X-ray). The potential of therapeutic radiometals has more recently been realized and relies on ionizing radiation to induce irreversible DNA damage, resulting in cell death. In both cases, radiopharmaceutical development has been largely geared toward the field of oncology; thus, selective tumor targeting is often essential for efficacious drug use. To this end, the rational design of four-component radiopharmaceuticals has become popularized. This Review introduces fundamental concepts of drug design and applications, with particular emphasis on bifunctional chelators (BFCs), which ensure secure consolidation of the radiometal and targeting vector and are integral for optimal drug performance. Also presented are detailed accounts of production, chelation chemistry, and biological use of selected main group and rare earth radiometals.

Radioactive Main Group and Rare Earth Metals for Imaging and Therapy

The acid–base properties of two bifunctional 3-hydroxy-4-pyridinone ligands and their chelating capacity towards Zn2+, an essential bio-metal cation, were investigated in NaCl aqueous solutions by potentiometric, UV-Vis spectrophotometric, and 1H NMR spectroscopic titrations, carried out at 0.15 ≤ I/mol −1 ≤ 1.00 and 288.15 ≤ T/K ≤ 310.15. A study at I = 0.15 mol L−1 and T = 298.15 K was also performed for other three Zn2+/Lz− systems, with ligands belonging to the same family of compounds. The processing of experimental data allowed the determination of protonation and stability constants, which showed accordance with the data obtained from the different analytical techniques used, and with those reported in the literature for the same class of compounds. ESI-MS spectrometric measurements provided support for the formation of the different Zn2+/ligand species, while computational molecular simulations allowed information to be gained on the metal–ligand coordination. The dependence on ionic strength and the temperature of equilibrium constants were investigated by means of the extended Debye–Huckel model, the classical specific ion interaction theory, and the van’t Hoff equations, respectively.

Speciation Studies of Bifunctional 3-Hydroxy-4-Pyridinone Ligands in the Presence of Zn2+ at Different Ionic Strengths and Temperatures.

Preparation d'une serie de complexes avec les acides pyromeconique, kojique et chlorokojique et le maltol. Donnees RMN de 27 Al

Neutral water-soluble post-transition-metal chelate complexes of medical interest: aluminum and gallium tris(3-hydroxy-4-pyronates)

Les deux composes du titre cristallisent dans le systeme rhomboedrique, groupe d'espace P3 et leur structure est affinee jusqu'a R=0,045 pour le complexe d'aluminium et R=0,047 pour le complexe de gallium

Aluminum and gallium compounds of 3-hydroxy-4-pyridinones: synthesis, characterization, and crystallography of biologically active complexes with unusual hydrogen bonding

A series of 3-hydroxy-2-methyl-4(1H)-pyridinones has been prepared with the substituents H, CH3, n-C6H11, and CH2CH2NH2 at the ring N. The dipyridinone 1,6-bis(3-hydroxy-2-methyl-4(1H)-pyridinon-1-...

Physical and structural studies of N-substituted-3-hydroxy-2-methyl-4(1H)-pyridinones

A series of 3-hydroxy-2-methyl-4-pyridinones and their complexes with aluminium(III) have been characterized by potentiometric (glass electrode) titration. The equilibria have been examined at 25.0±0.1˚C and at ionic strengths of μ=0.15 and 0.6 M (NaCl). The pyridinones have a variety of substituents at the ring nitrogen atom (H, CH 3 , C 2 H 5 , and n-C 6 H 13

The complexation of aluminum with N-substituted 3-hydroxy-4-pyridinones

A series of complexes of several 3-hydroxy-2-methyl-4-pyridinones with gallium(III) and indium(III) have been characterized by potentiometric (glass electrode) titration. The effective formation constants of the various ligands for Ga 3+ at physiological pH are close to 10 31 . As a practical application of these data, comparative metal binding in a simple blood plasma model is simulated. This result is incorporated into the design of biodistribution experiments in mice using these ligands, their n-C 6 H 13 analogue, and l-mimosine

William O. Nelson

Papers

Neutral water-soluble post-transition-metal chelate complexes of medical interest: aluminum and gallium tris(3-hydroxy-4-pyronates)

Aluminum and gallium compounds of 3-hydroxy-4-pyridinones: synthesis, characterization, and crystallography of biologically active complexes with unusual hydrogen bonding

Physical and structural studies of N-substituted-3-hydroxy-2-methyl-4(1H)-pyridinones

The complexation of aluminum with N-substituted 3-hydroxy-4-pyridinones

Solution chemistry of gallium and indium 3-hydroxy-4-pyridinone complexes in vitro and in vivo