A5081705830- Histone Deacetylase Inhibitors Research
- Synthetic Organic Chemistry Methods
- Electrostatic Discharge in Electronics
- Click Chemistry and Applications
- Synthesis and pharmacology of benzodiazepine derivatives
- Cardiac electrophysiology and arrhythmias
- Alkaloids: synthesis and pharmacology
- Cancer Treatment and Pharmacology
- Plant-based Medicinal Research
- Cardiac pacing and defibrillation studies
- Berberine and alkaloids research
- Protein Degradation and Inhibitors
University of Bologna
2012-2014
Berberine (1) is an alkaloid used widely in the treatment of several diseases. However, its physicochemical properties, pharmacokinetics, and metabolism remain unclear, conflicting data have been reported. In this study, main properties 1 metabolites were evaluated, including lipophilicity, solubility, pKa, albumin binding. A sensitive HPLC-ESIMS/MS method was developed validated to identify human plasma. This quantify their levels plasma healthy volunteers hypercholesterolemic patients...
Molecular knowledge of hERG blocking liability can offer the possibility optimizing lead compounds in a way that eliminates potentially lethal side effects. In this study, we computationally designed, synthesized, and tested small series "minimally structured" molecules. Some these were remarkably potent against (6, IC50 = 2.4 nM), allowing us to identify minimal structural requirements for liability.
Given our interest in finding potential antitumor agents and view of the multifactorial mechanistic nature cancer, present work, taking advantage multifunctional ligands approach, new chimeric molecules were designed synthesized by combining single chemical entities structural features SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained us endowed antiproliferative pro-apoptotic activity. The characterized respect to their...