A5010189561- Synthesis and biological activity
- Synthesis and Biological Evaluation
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactions of Organic Compounds
- PARP inhibition in cancer therapy
- DNA Repair Mechanisms
- Asymmetric Synthesis and Catalysis
- Bioactive Compounds and Antitumor Agents
- Computational Drug Discovery Methods
- Cancer, Hypoxia, and Metabolism
- Sirtuins and Resveratrol in Medicine
- Chemical Synthesis and Analysis
- Click Chemistry and Applications
- Trypanosoma species research and implications
- Neuroscience and Neuropharmacology Research
- Alkaloids: synthesis and pharmacology
- Biochemical and Molecular Research
- Synthesis and pharmacology of benzodiazepine derivatives
- Organophosphorus compounds synthesis
- Neurotransmitter Receptor Influence on Behavior
- Analytical Chemistry and Chromatography
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Synthesis of heterocyclic compounds
- Plant-based Medicinal Research
- HIV/AIDS drug development and treatment
University of Bologna
2016-2025
Italian Institute of Technology
2009-2024
Scuola Internazionale Superiore di Studi Avanzati
2009
University of Ferrara
1994-2006
Sigma Tau (Italy)
2005
University of Palermo
1997-2003
Georgetown University
1996-1999
Jacksonville College
1992-1994
Mayo Clinic in Florida
1992-1994
WinnMed
1992-1994
Resveratrol 1 (3,4',5-trihydroxy-trans-stilbene), a phytoalexin present in grapes and other food products, has recently been suggested as potential cancer chemopreventive agent based on its striking inhibitory effects cellular events associated with initiation, promotion, progression. This triphenolic stilbene also displayed vitro growth inhibition number of human cell lines. In this context, series cis- trans-stilbene-based resveratrols were prepared the aim discovering new lead compounds...
One of the most prominent alterations in cancer cells is their strict dependence on glycolytic pathway for ATP generation. This observation led to evaluation glycolysis inhibitors as potential anticancer agents. The inhibition lactate dehydrogenase (LDH) a promising way inhibit tumor cell glucose metabolism without affecting energetic balance normal tissues. However, success this approach depends chiefly availability that display good selectivity. We identified compound (galloflavin, CAS...
We report the identification of multitarget anti-Alzheimer compounds designed by combining a naphthoquinone function and tacrine fragment. In vitro, 15 displayed excellent acetylcholinesterase (AChE) inhibitory potencies interesting capabilities to block amyloid-β (Aβ) aggregation. The X-ray analysis one those in complex with AChE allowed rationalizing outstanding activity data (IC50 = 0.72 nM). Two showed negligible toxicity immortalized mouse cortical neurons Neuro2A primary rat cerebellar...
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...
Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) six-membered ring (pyridine benzene). compounds evaluated for their effects on tubulin assembly and cytotoxic apoptotic activities. Five (18b, 20a, 21a, 34b, 35b) demonstrated an attractive profile cytotoxicity (IC50 < 1 μM) apoptosis-inducing activity but poor antitubulin activity. isoxazoline derivatives 18b, potent...
With the aim of enhancing structural complexity and diversity an existing collection bi- terphenyl compounds, we synthesized hybrid molecules comprising spirocyclic ketones (a complexity-bearing core) bi/terphenyls (privileged fragments). Compounds 1, 3, 4, 6 showed well-defined activity on apoptosis differentiation, making them potential leads for development as new anticancer agents chemical probes to study signaling networks in neoplastic cells.
Synthetic lethality is an innovative framework for discovering novel anticancer drug candidates. One example the use of PARP inhibitors (PARPi) in oncology patients with BRCA mutations. Here, we exploit a new paradigm based on possibility triggering synthetic using only small organic molecules (dubbed "fully small-molecule-induced lethality"). We exploited this to target pancreatic cancer, one major unmet needs oncology. discovered dihydroquinolone pyrazoline-based molecule (35d) that...
A convenient procedure to effect the Wittig and Horner−Wadsworth−Emmons reactions employs guanidine TBD MTBD as base-promoters; mild reaction conditions, high efficiency, facile isolation of final products make present methodology, at least in some cases, a practical alternative known procedures.
In a search for retinoic acid (RA) receptor ligands endowed with potent apoptotic activity, series of novel arotinoids were prepared. Because the stereochemistry C9-alkenyl portion natural 9-cis-RA and olefinic moiety previously synthesized isoxazole retinoid 4 seems to have particular importance their analogues restricted or, vice versa, larger flexibility in this region designed The new compounds evaluated vitro ability activate receptors differentiation-inducing activity. Cytotoxic...
To further explore the SAR of resveratrol-related trans-stilbene derivatives, here we describe synthesis (a) a series 3,5-dimethoxy analogues in which variety substituents were introduced at positions 2', 3', 4', and 5' stilbene scaffold (b) second group derivatives (2-phenylnaphthalenes terphenyls) that incorporate phenyl ring as bioisosteric replacement alkenyl bridge. We thoroughly characterized all new compounds with respect to their apoptosis-inducing activity effects on cell cycle. One...