A5012577015- Cancer-related gene regulation
- Epigenetics and DNA Methylation
- RNA modifications and cancer
- Microfluidic and Capillary Electrophoresis Applications
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Catalytic Reactions
- Innovative Microfluidic and Catalytic Techniques Innovation
- Monoclonal and Polyclonal Antibodies Research
- Chemical Synthesis and Analysis
- Advanced Data Storage Technologies
- RNA regulation and disease
- Adenosine and Purinergic Signaling
- Synthesis and Characterization of Heterocyclic Compounds
- Genomics and Rare Diseases
- Genomics and Chromatin Dynamics
- Semiconductor materials and devices
- Quinazolinone synthesis and applications
University of Salerno
2014-2022
Istituto di Farmacologia Traslazionale
2014
Since the discovery of compound BIX01294 over 10 years ago, only a very limited number nonquinazoline inhibitors H3K9-specific methyltransferases G9a and G9a-like protein (GLP) have been reported. Herein, we report identification novel chemotype for G9a/GLP inhibitors, based on underinvestigated 2-alkyl-5-amino- 2-aryl-5-amino-substituted 3H-benzo[e][1,4]diazepine scaffold. Our research efforts resulted in 12a (EML741), which not maintained high vitro cellular potency its quinazoline...
Protein arginine methyltransferases (PRMTs) are important therapeutic targets, playing a crucial role in the regulation of many cellular processes and being linked to diseases. Yet, there is still much be understood regarding their functions biological pathways which they involved, as well on structural requirements that could drive development selective modulators PRMT activity. Here we report deconstruction-reconstruction approach that, starting from series type I inhibitors previously...
A continuous-flow strategy to achieve the benzodiazepine privileged structure.
Abstract An improved continuous‐flow synthetic method for the synthesis of benzodiazepinone derivatives (IV) is developed.
Abstract Review: [34 refs.