A5012577015- Cancer-related gene regulation
- Epigenetics and DNA Methylation
- RNA modifications and cancer
- Eicosanoids and Hypertension Pharmacology
- Innovative Microfluidic and Catalytic Techniques Innovation
- Synthesis and Catalytic Reactions
- Microfluidic and Capillary Electrophoresis Applications
- RNA regulation and disease
- Chemical Synthesis and Analysis
- Adenosine and Purinergic Signaling
- Genomics and Chromatin Dynamics
- Quinazolinone synthesis and applications
- Advanced Data Storage Technologies
- Synthesis and Characterization of Heterocyclic Compounds
- Semiconductor materials and devices
- Genomics and Rare Diseases
- Monoclonal and Polyclonal Antibodies Research
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.