Aryl diazonium salts are versatile building blocks in organic synthesis In light of the ever-increasing importance of aryl diazonium salts spanning most disciplines of the chemical sciences, we review the recent development of aryl diazonium chemistry over the past seven years (2013-2020) Special emphasis is put on various new transformations involving the generation of radical intermediates via thermal, photochemical, and electrochemical means Recent advances in the development of transition metal-catalyzed reactions using aryl diazonium salts are also reviewed Together, these newly developed transformations significantly expand the synthetic chemist's repertoire of aromatic carbon-carbon and carbon-heteroatom bond forming methods using aryl diazonium precursors, providing powerful tools for the synthesis and modification of complex molecular scaffolds

Recent Development of Aryl Diazonium Chemistry for the Derivatization of Aromatic Compounds

Nanomaterial-based drug delivery systems (NBDDS) are widely used to improve the safety and therapeutic efficacy of encapsulated drugs due to their unique physicochemical and biological properties. By combining therapeutic drugs with nanoparticles using rational targeting pathways, nano-targeted delivery systems were created to overcome the main drawbacks of conventional drug treatment, including insufficient stability and solubility, lack of transmembrane transport, short circulation time, and undesirable toxic effects. Herein, we reviewed the recent developments in different targeting design strategies and therapeutic approaches employing various nanomaterial-based systems. We also discussed the challenges and perspectives of smart systems in precisely targeting different intravascular and extravascular diseases.

Advances in nanomaterial-based targeted drug delivery systems

Over the last two decades, the development of chemical biology and the need for more defined protein conjugates have fostered active research on new bioconjugation techniques. In particular, a wide range of biorthogonal labelling strategies have been reported to functionalise the phenol side chain of tyrosines (Tyr). Tyr occur at medium frequency and are partially buried at the protein surface, offering interesting opportunities for site-selective labelling of the most reactive residues. Tyr-targeting has proved effective for designing a wide range of important biomolecules including antibody-drug conjugates, fluorescent or radioactive protein probes, glycovaccines, protein aggregates, and PEG conjugates. Innovative methods have also been reported for site-specific labelling with ligand-directed anchors and for the specific affinity capture of proteins. This review will present and discuss these promising alternatives to the conventional labelling of the nucleophilic lysine and cysteine residues.

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Tyrosine Conjugation Methods for Protein Labelling

Radiolabeled nanomaterials for biomedical applications: radiopharmacy in the era of nanotechnology

Cancer is one of the leading causes of death worldwide. The development of cancer-specific diagnostic agents and anticancer toxins would improve patient survival. The current and standard types of medical care for cancer patients, including surgery, radiotherapy, and chemotherapy, are not able to treat all cancers. A new treatment strategy utilizing tumor targeting peptides to selectively deliver drugs or applicable active agents to solid tumors is becoming a promising approach. In this review, we discuss the different tumor-homing peptides discovered through combinatorial library screening, as well as native active peptides. The different structure–function relationship data that have been used to improve the peptide’s activity and conjugation strategies are highlighted.

Peptide-Based Strategies for Targeted Tumor Treatment and Imaging.

Polymeric micellar nanoparticles represent versatile and biocompatible platforms for targeted drug delivery. However, tracking their biodistribution, stability, and clearance profile in vivo is challenging. The goal of this study was to prepare surface-modified micelles with peptide GE11 for targeting the epidermal growth factor receptor (EGFR). In vitro fluorescence studies demonstrated significantly higher internalization of GE11 micelles into EGFR-expressing HCT116 colon cancer cells versus EGFR-negative SW620 cells. Azo coupling chemistry of tyrosine residues in the peptide backbone with aryl diazonium salts was used to label the micelles with radionuclide 64Cu for positron emission tomography (PET) imaging. In vivo analysis of 64Cu-labeled micelles showed prolonged blood circulation and predominant hepatobiliary clearance. The biodistribution profile of EGFR-targeting GE11 micelles was compared with nontargeting HW12 micelles in HCT116 tumor-bearing mice. PET revealed increasing tumor-to-muscle ratios for both micelles over 48 h. Accumulation of GE11-containing micelles in HCT116 tumors was higher compared to HW12-decorated micelles. Our data suggest that the efficacy of image-guided therapies with micellar nanoparticles could be enhanced by active targeting, as demonstrated with cancer biomarker EGFR.

Synthesis and Analysis of 64Cu-Labeled GE11-Modified Polymeric Micellar Nanoparticles for EGFR-Targeted Molecular Imaging in a Colorectal Cancer Model

Tyrosine is an attractive target for chemo- and site-selective protein modification. The particular chemical nature of tyrosine residues allows bioconjugation chemistry with reactive aryl diazonium...

Radiometal-Containing Aryl Diazonium Salts for Chemoselective Bioconjugation of Tyrosine Residues.

Radiolabeling of small molecules and peptides with therapeutic radionuclide Cu-67 for theranostic applications

Optimizing 203Pb cyclotron production and availability: The ideal SPECT imaging theranostic partner for 212Pb targeted alpha therapy

64Cu-labeled panitumumab for PET imaging of EGFR+ non-small cell lung cancer: Subcutaneous and metastatic mouse models

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