Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway

• Paul M. Hershberger,
• Satyamaheshwar Peddibhotla,
• E. Hampton Sessions,
• Daniela B. Divlianska,
• Ricardo G. Correa,
• Anthony B. Pinkerton,
• John C. Reed and
• Gregory P. Roth

Beilstein J. Org. Chem. 2013, 9, 900–907, doi:10.3762/bjoc.9.103

• transduction in reporter cell lines containing either low or overexpressed NOD2 proteins. Probes 13 and 17 were also selective over the non-NOD-stimulated NF-κB pathways (TNF-α, doxorubicin and PMA/ionomycin) in these reporter assays. Both of the probes, and their close analogues as discovered through SAR

Cyclodextrin-based nanosponges as drug carriers

• Francesco Trotta,
• Marco Zanetti and
• Roberta Cavalli

Beilstein J. Org. Chem. 2012, 8, 2091–2099, doi:10.3762/bjoc.8.235

• interactions between molecules with different lipophilicities and structures. The ability of cyclodextrin nanosponges to encapsulate drugs has been studied in depth for both hydrophilic and lipophilic molecules, including dexamethasone, flurbiprofen, doxorubicin, itraconazole, resveratrol, paclitaxel, 5

• nanosponges [37], reaching a percentage of less than 10% after 130 minutes. A similar result was obtained with the incorporation of doxorubicin in nanosponges. In in vitro tests, doxorubicin was released very slowly at pH 1.2 (about 1% after 120 minutes) and the percentage increased with pH values

• . Doxorubicin release of about 29% was obtained at pH 7.4. This behaviour could suggest that the nanosponge formulation is able to protect the drug from the gastric environment, allowing delivery in the intestinal tract. Vavia prepared nelfinavir mesylate loaded nanosponges to enhance the solubility of the drug

Syntheses and applications of furanyl-functionalised 2,2’:6’,2’’-terpyridines

• Jérôme Husson and
• Michael Knorr

Beilstein J. Org. Chem. 2012, 8, 379–389, doi:10.3762/bjoc.8.41

• -substituted terpyridines in biomedical sciences Furanyl-terpyridines were probed in biomedical sciences as cytotoxic molecules. Compounds 12 and 13 were tested as anticancer agents against seven different cell lines [4]. Their activities were compared to that of doxorubicin, which is a currently used

• anticancer agent. Additionally, their cytotoxicity against normal cells was evaluated (Table 3). As can be seen from Table 3, these furanyl-functionalised terpyridines display, in many cases, better cytotoxicity than doxorubicin. Unfortunately, they are also more toxic toward normal cells (RPTEC). Note that

• -functionalised tpys as potential biomolecule-labelling agents. Synthetic sequence envisioned for biomolecules labelling by click-chemistry. Influence of solvent on U/S ratio. Complexes obtained by direct oxidation of furanyl-functionalised tpys. GI50 (μg/ml) for terpyridines 12 and 13 compared to doxorubicin