A Gadolinium DO3A Amide m-Phenyl Boronic Acid MRI Probe for Targeted Imaging of Sialated Solid Tumors

We developed a new probe, Gd-DO3A-Am-PBA, for imaging tumors. Our results showed active targeting of Gd-DO3A-Am-PBA to sialic acid (SA) moieties, with increased cellular labeling in vitro and enhanced tumor accumulation and retention in vivo, compared to the commercial Gadovist. The effectiveness of our newly synthesized probe lies in its adequate retention phase, which is expected to provide a suitable time window for tumor diagnosis and a faster renal clearance, which will reduce toxicity risks when translated to clinics. Hence, this study can be extended to other tumor types that express SA on their surface. Targeting and MR imaging of any type of tumors can also be achieved by conjugating the newly synthesized contrast agent with specific antibodies. This study thus opens new avenues for drug delivery and tumor diagnosis via imaging.

Photo-responsive host–guest complexation directs dynamic covalent condensation of phenyl boronic acid and d-fructose

The photo-responsive host-guest interaction of an azo-based photoswitch with permethylated cyclodextrin is used to modulate the dynamic covalent interaction of a phenyl boronic acid and D-fructose by irradiation with light.

2-formyl phenyl boronic acid (2FPBA)-maleimide crosslinker: a versatile platform for cys-peptide – hydrazine conjugation and interplay

In this work we describe the preparation of a heterobifunctional 2-formyl phenyl boronic acid (2-FPBA)-maleimide crosslinker and explore its versatility in the preparation of various bioconjugates. We demonstrate the straightforward...

Microwave-Assisted Synthesis and Fluorescent Properties of 4-Phenyl-1,8-naphthalimide

4-Phenyl-1,8-naphthalimide was synthesized by imidation of commercially available 4-bromo-1,8-naphthalic anhydride, followed by Suzuki coupling with phenyl boronic acid, both under microwave heating. The microwave-assisted reactions were found to be faster and more efficient than reactions carried out by heating in oil-baths. While this compound was quite fluorescent in solvents such as chloroform, methanol and ethanol, it is virtually non-fluorescent in DMSO; however, upon the addition of water to DMSO solutions of this dye, fluorescence was restored, suggesting a tendency for aggregation-induced emission. The fluorescent properties of 4-phenyl-1,8-naphthalimide were found to be influenced by salt concentrations, likely as a result of hydrophobic effects. While this dye does not show binding to DNA, presence of bovine serum albumin leads to effective fluorescence quenching.