A5017835879- Cancer therapeutics and mechanisms
- HIV/AIDS drug development and treatment
- Synthesis and biological activity
- HIV Research and Treatment
- Synthesis and pharmacology of benzodiazepine derivatives
- Biochemical and Molecular Research
- Cannabis and Cannabinoid Research
- Neuroscience and Neuropharmacology Research
- Alzheimer's disease research and treatments
- Bioactive Compounds and Antitumor Agents
- Cholinesterase and Neurodegenerative Diseases
- Chemical Synthesis and Analysis
- Nicotinic Acetylcholine Receptors Study
- Melanoma and MAPK Pathways
- Click Chemistry and Applications
- Free Radicals and Antioxidants
- Cancer-related Molecular Pathways
- Lipid Membrane Structure and Behavior
- Pharmacological Receptor Mechanisms and Effects
- Histone Deacetylase Inhibitors Research
- Biochemical effects in animals
- Computational Drug Discovery Methods
- Synthesis of Tetrazole Derivatives
- Protein Kinase Regulation and GTPase Signaling
- Receptor Mechanisms and Signaling
University of Salerno
2010-2025
Istituto di Genetica Molecolare
2009
Sigma Tau (Italy)
2005
University of Siena
1999-2005
University of Rome Tor Vergata
2005
Virginia Commonwealth University
2005
Trinity College Dublin
2002-2005
University of Naples Federico II
1998-2002
University of Calabria
2001
Federico II University Hospital
1999
N-Palmitoyl-ethanolamine (PEA) is an anti-inflammatory component of egg yolk that usually employed for the prevention respiratory apparatus virus infection and then frequently used its efficient analgesic effects in experimental models visceral, neuropathic, inflammatory diseases. Nevertheless, data use animal or human therapy are still scarce further studies needed. Herein, we report biological evaluation a small library N-palmitoyl-ethanolamine analogues derivatives, characterized by...
Effector caspases‐3, ‐6 and ‐7 are responsible for producing the morphological features associated with apoptosis, such as DNA fragmentation. The present study demonstrates that a member of novel series pyrrolo‐1,5‐benzoxazepines, PBOX‐6, induces apoptosis in MCF‐7 cells, which lack caspase‐3. Apoptosis was accompanied by fragmentation activation caspase‐7, but not caspases‐3 ‐6. Inhibition caspase‐7 activity reduced extent induced, indicating is involved mechanism PBOX‐6 cells. This...
New potent, selective monoacylglycerol lipase (MAGL) inhibitors based on the azetidin-2-one scaffold ((±)-5a–v, (±)-6a–j, and (±)-7a–d) were developed as irreversible ligands, demonstrated by enzymatic crystallographic studies for (±)-5d, (±)-5l, (±)-5r. X-ray analyses combined with extensive computational allowed us to clarify binding mode of compounds. 5v was identified MAGL when compared other serine hydrolases. Solubility, in vitro metabolic stability, cytotoxicity, absence mutagenicity...
Abstract In the last few years, severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) has been cause of a worldwide pandemic, highlighting need for novel antiviral agents. The main protease (M pro ) SARS‐CoV‐2 was immediately identified as crucial enzyme viral replication and validated drug target. Here, we present design synthesis peptidomimetic M covalent inhibitors characterized by quinoline‐based P 3 moieties. Structure–activity relationships (SARs) were also investigated at 1 ,...
Quinoxalinylethylpyridylthioureas (QXPTs) represent a new class of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 6-FQXPT (6). Docking studies based on the three-dimensional structure RT prompted synthesis novel heteroarylethylpyridylthioureas which were tested as anti-HIV agents. Several compounds proved to be potent broad-spectrum enzyme and significantly inhibited HIV-1 replication in vitro. Their potency...
We have recently developed five novel pyrrolo-1,5-benzoxazepines as proapoptotic agents. Their JNK-dependent induction of apoptosis in tumor cells suggested their potential anticancer The core structure the apoptotic agent 6 was investigated, and SARs were expanded with design synthesis several analogues. To define mechanism new compounds localization drug target, two analogues designed synthesized to delineate events leading JNK activation. cell-penetrating compound 16 induced cells, while...
Two three-dimensional receptor interaction models for EAAT substrates and nontransportable inhibitors have been developed, new glutamate (Glu) aspartate (Asp) analogues synthesized. The 1a 3 represent novel lead compounds the development of inhibitors, selective EAATs over iGluRs, as possible neuroprotective agents useful to minimize progression chronic or acute neurodegenerative diseases. role played by protonatable amine function in with has discussed.
Citrus fruits are one of the principal used to produce juices. Over years, these have been recognized as new health-promoting agents. In this work, food wastes derived from autochthonous citrus Southern Italy, named Limone di Rocca Imperiale, Arancia Rossa Moro, and Bionda Tardivo Trebisacce, were analyzed. After fresh-squeezing juice, peel pomace employed obtain six different extracts using an ultrasound-assisted method in a hydroalcoholic solvent. The analyzed terms qualitative...
Extra virgin olive oil (EVOO) is the typical source of fats in Mediterranean diet. While fatty acids are essential for EVOO nutraceutical properties, multiple biological activities also due to presence polyphenols. In this work, autochthonous Tuscany EVOOs were chemically characterized and selected samples extracted obtain hydroalcoholic phytocomplexes, which assayed establish their anti-inflammatory vasorelaxant properties. The polar extracts via 1H-NMR UHPLC-HRMS investigate chemical...
Aiming to simultaneously modulate the endocannabinoid system (ECS) functions and epigenetic machinery, we selected fatty acid amide hydrolase (FAAH) histone deacetylase (HDAC) enzymes as desired targets develop potential neuroprotective multitarget-directed ligands (MTDLs), expecting achieve an additive or synergistic therapeutic effect in oxidative stress-related conditions. We herein report design, synthesis, biological evaluation of first-in-class FAAH-HDAC multitarget inhibitors. A...
Inherited retinal diseases, which include retinitis pigmentosa, are a family of genetic disorders characterized by gradual rod-cone degeneration and vision loss, without effective pharmacological treatments. Experimental approaches aim to delay disease progression, supporting cones' survival, crucial for human vision. Histone deacetylases (HDACs) mediate the activation epigenetic nonepigenetic pathways that modulate cone in RP mouse models. We developed new HDAC inhibitors (5a–p), typified...
Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures HIV-1 RT prompted synthesis novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target highly conserved amino acid residues within β12-β13 hairpin, namely primer grip, proved be very potent against most common...
The mitogen-activated protein (MAP) kinase family is activated in response to a wide variety of external stress signals such as UV irradiation, heat shock, and many chemotherapeutic drugs leads the induction apoptosis. A novel series pyrrolo-1,5-benzoxazepines have been shown potently induce apoptosis chronic myelogenous leukemia (CML) cells, which are resistant agents. In this study we delineated part mechanism by representative compound known PBOX-6 induces We investigated whether...
Pyrrolobenzoxazepinone (PBO) derivatives represent a new class of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase (RT) inhibitors (NNRTs) whose prototype is (+/-)-6-ethyl-6-phenylpyrrolo[2,1-d][1,5]benzoxazepin-7(6H)- one (6). Docking studies based on the three-dimensional structure RT prompted synthesis and biological evaluation novel analogues 6 featuring meta-substituted phenyl or 2-thienyl ring at C-6 pyridine system in place fused-benzene to yield...
The novel tetrasubstituted pyrrole derivatives 8g, 8h, and 8i showed selective cytotoxicity against M14 melanoma cells at low micromolar concentration. Structure-activity relationships (SARs) indicated the presence of three aromatic substituents on core as necessary for biological activity. Computational studies strongly suggest that peculiar 3D orientation these is able to reproduce hydrophobic side chains in LxxLL-like protein recognition motifs. Biological results altered p53 expression...
Abstract Cinnamic acid and its derivatives represent attractive building blocks for the development of pharmacological tools. A series piperoniloyl cinnamoyl‐based amides ( 6‐9 a‐f ) have been synthesized assayed against a wide panel colorectal cancer (CRC) cells, with aim finding promising anticancer agents. Among all twenty‐four molecules, 7a , 7e‐f 9c 9f displayed best antiproliferative activity. The induced G1 cell cycle arrest increase in apoptotic death was seen FACS analysis western...