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1.
RSC Adv ; 8(59): 34162-34167, 2018 Sep 28.
Article in English | MEDLINE | ID: mdl-35548818

ABSTRACT

Diagnostic nanomedicine constantly requires the development of novel contrast agents with intrinsic imaging capabilities. Phosphorescent Ir(iii)-complexes represent good candidates when delivered through polymeric nanoparticles. In this work, we propose a biocompatible nanoparticle made from an intrinsically phosphorescent copolymer, synthesized directly with an imaging tag present on its backbone. Polymeric nanoparticles can be obtained with the exact amount of phosphorescent moieties needed to maximize their output signal. Complete characterization and ex vivo studies confirmed that this nanosystem is suitable as a future diagnostic tool.

2.
Eur J Med Chem ; 117: 1-7, 2016 Jul 19.
Article in English | MEDLINE | ID: mdl-27081742

ABSTRACT

In this paper a straightforward synthesis of a novel pyrazole derivative is reported. Prominent feature of this synthetic process is a 1,3-Dipolar Cycloaddition of a suitable nitrile imine with an activated α,ß-unsaturated lactam to afford directly and regioselectively the corresponding ring-fused pyrazole. Having obtained the central core of the synthetic target, a double stepwise functionalization with a "side chain" characterized by a terminal cyclic aliphatic amine was carried out. This molecular structure was designed to interact strongly with typical biological residues, and indeed it showed potent anticancer capability: in vitro cytotoxicity test on five different cancer cell lines showed interesting IC50 values in the range of 15-60 µM for exposure time of 24-72 h, thus resulting comparable with commercially available and nowadays therapeutically exploited anticancer compounds, such as 5-FU and NVP-BEZ235.


Subject(s)
Antineoplastic Agents/chemical synthesis , Pyrazoles/chemical synthesis , Amino Acids, Cyclic/chemistry , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cycloaddition Reaction , Drug Design , Humans , Imines/chemistry , Lactams/chemistry , Nitriles/chemistry , Pyrazoles/pharmacology
4.
Nanotechnology ; 25(2): 025101, 2014 Jan 17.
Article in English | MEDLINE | ID: mdl-24334365

ABSTRACT

Metal oxide nanoparticles, hybridized with various polymeric chemicals, represent a novel and breakthrough application in drug delivery, hyperthermia treatment and imaging techniques. Radiolabeling of these nanoformulations can result in new and attractive dual-imaging agents as well as provide accurate in vivo information on their biodistribution profile. In this paper a comparison study has been made between two of the most promising hybrid core-shell nanosystems, bearing either magnetite (Fe3O4) or cobalt ferrite (CoFe2O4) cores, regarding their magnetic, radiolabeling, hyperthermic and biodistribution properties. While hyperthermic properties were found to be affected by the metal-core type, the radiolabeling ability and the in vivo fate of the nanoformulations seem to depend critically on the size and the shell composition.


Subject(s)
Cobalt/chemistry , Ferric Compounds/chemistry , Ferrosoferric Oxide/chemistry , Magnetite Nanoparticles/chemistry , Animals , Cobalt/pharmacokinetics , Drug Delivery Systems , Female , Ferric Compounds/pharmacokinetics , Ferrosoferric Oxide/pharmacokinetics , History, 16th Century , Humans , Hyperthermia, Induced , Isotope Labeling , Magnetic Phenomena , Mice , Radiopharmaceuticals , Tissue Distribution
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