SILVESTRI Romano

Professore ordinario
Settore Scientifico-Disciplinare: 
CHIM/08
Informazioni personali
Curriculum vitae (it): 
Curriculum vitae (en): 
Didattica
Aree di afferenza: 
- Area Farmaceutica
- Corso di Laurea in Farmacia
- Corso di Laurea in Scienze Farmaceutiche Applicate
- Scuola di Specializzazione in Farmacia Ospedaliera
Ricevimento studenti: 

Mercoled,ì dalle ore 14 alle 17

Ricerca
Aree di interesse: 

The research projects are mainly focused on the drug design and synthesis of new biologically active chemical entities in the areas of antitumor, antiviral or SNC drugs. The drug design is based on molecular models performed by either the internal unit or external research groups. New procedures for the microwave-assisted synthesis and the highly automated purification of relevant pharmaceutical molecules are also developed.

Tubulin polymeriztion inhibitors Carbonic anhydrase inhibitors Chronic myelogenous leukemia agents HIV-1 non-nucleoside reverse transcriptase inhibitors Monoamine oxidase inhibitors  
Finanziamenti: 
2010, PRIN, Italian MIUR, PI 2013,, PRIN, Italian MIUR, PI 2017, PRIN, Italian MIUR, PI 2009, Istitute Pasteur Italy, PI 2012, Istitute Pasteur Italy, PI 2011, FIRB, Italian, RU Coordinator 2014, A.C.R.A.F. SpA, Italy, PI 2016,  A.C.R.A.F. SpA, Italy, PI 2012, European Institute of Oncology, Italy, PI  

Pubblicazioni scientifiche

Anno: 2021
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
CXCR4 antagonism sensitizes cancer cells to novel indole-based MDM2/4 inhibitors in glioblastoma multiforme European Journal of Pharmacology 2021 Sci_Dir
CXCR4 antagonism sensitizes cancer cells to novel indole-based MDM2/4 inhibitors in glioblastoma multiforme European Journal of Pharmacology 2021 Sci_Dir
Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia European Journal of Medicinal Chemistry 2021 Sci_Dir
RS4651 suppresses lung fibroblast activation via the TGF-β1/SMAD signalling pathway European Journal of Pharmacology 2021 Sci_Dir
Anno: 2020
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Design, Synthesis and Discovery of N,N’-Carbazoyl-aryl-urea Inhibitors of Zika NS5 Methyltransferase and Virus Replication ChemMedChem 2020 Sci_Dir
Discovery of New 1,1′-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors ACS Medicinal Chemistry Letters 2020 Sci_Dir
Discovery of Zika Virus NS2B/NS3 Inhibitors That Prevent Mice from Life-Threatening Infection and Brain Damage ACS Medicinal Chemistry Letters 2020 Sci_Dir
HDAC inhibition induces expression of scaffolding proteins critical for tumor progression in pediatric glioma: Focus on EBP50 and IRSp53 Neuro-Oncology 2020 Sci_Dir
Modeling Epac1 interactions with the allosteric inhibitor AM-001 by co-solvent molecular dynamics Journal of Computer-Aided Molecular Design 2020 Sci_Dir
Mutational analysis of the essential lipopolysaccharide-transport protein LptH of Pseudomonas aeruginosa to uncover critical oligomerization sites Scientific Reports 2020 Sci_Dir
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains European Journal of Medicinal Chemistry 2020 Sci_Dir
Selenotriapine – An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity, low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors Arabian Journal of Chemistry 2020 Sci_Dir
Sulfonamide Inhibitors of β-Catenin Signaling as Anticancer Agents with Different Output on c-MYC ChemMedChem 2020 Sci_Dir
Targeting the Interaction between the SH3 Domain of Grb2 and Gab2 Cells 2020 Sci_Dir
Anno: 2019
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents ACS Medicinal Chemistry Letters 2019 Sci_Dir
Identification of a pharmacological inhibitor of Epac1 that protects the heart against acute and chronic models of cardiac stress Cardiovascular Research 2019 Sci_Dir
Nox2-mediated platelet activation by glycoprotein (GP) VI: Effect of rivaroxaban alone and in combination with aspirin Biochemical Pharmacology 2019 Sci_Dir
Small molecule inhibitors of KDM5 histone demethylases increase the radiosensitivity of breast cancer cells overexpressing JARID1B Molecules 2019 Sci_Dir
Structure-activity relationship studies and in vitro and in vivo anticancer activity of novel 3-aroyl-1,4-diarylpyrroles against solid tumors and hematological malignancies European Journal of Medicinal Chemistry 2019 Sci_Dir
Switching on the activity of 1,5-diaryl-pyrrole derivatives against drug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies European Journal of Medicinal Chemistry 2019 Sci_Dir
Towards modern anticancer agents that interact with tubulin European Journal of Pharmaceutical Sciences 2019 Sci_Dir
Anno: 2018
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
A high-throughput screening of a chemical compound library in ovarian cancer stem cells Combinatorial Chemistry and High Throughput Screening 2018 Sci_Dir
A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist Biochemistry 2018 Sci_Dir
Arginine- and lysine-rich peptides: Synthesis, characterization and antimicrobial activity Letters in Drug Design and Discovery 2018 Sci_Dir
Arginine- and lysine-rich peptides: Synthesis; characterization and antimicrobial activity Letters in Drug Design and Discovery 2018 Sci_Dir
Bax Activation Blocks Self-Renewal and Induces Apoptosis of Human Glioblastoma Stem Cells ACS Chemical Neuroscience 2018 Sci_Dir
Indolylarylsulfones, a fascinating story of highly potent human immunodeficiency virus type 1 non-nucleoside reverse transcriptase inhibitors Antiviral Chemistry and Chemotherapy 2018 Sci_Dir
New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors European Journal of Medicinal Chemistry 2018 Sci_Dir
Oleuropein, a component of extra virgin olive oil, lowers postprandial glycaemia in healthy subjects British Journal of Clinical Pharmacology 2018 Sci_Dir
Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication Journal of Medicinal Chemistry 2018 Sci_Dir
β-catenin knockdown promotes NHERF1-mediated survival of colorectal cancer cells: implications for a double-targeted therapy Oncogene 2018 Sci_Dir
Anno: 2017
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
3-Aroyl-1;4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin ACS Medicinal Chemistry Letters 2017 Sci_Dir
Annurca apple (M. pumila Miller cv Annurca) extracts act against stress and ageing in S. cerevisiae yeast cells BMC Complementary and Alternative Medicine 2017 Sci_Dir
Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents Journal of Medicinal Chemistry 2017 Sci_Dir
Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity Journal of Medicinal Chemistry 2017 Sci_Dir
Exploring the first Rimonabant analog-opioid peptide hybrid compound; as bivalent ligand for CB1 and opioid receptors Journal of Enzyme Inhibition and Medicinal Chemistry 2017 Sci_Dir
Heterocyclic pharmacochemistry of new rhinovirus antiviral agents: A combined computational and experimental study European Journal of Medicinal Chemistry 2017 Sci_Dir
Inhibition of dengue virus replication by novel inhibitors of RNA-dependent RNA polymerase and protease activities Journal of Enzyme Inhibition and Medicinal Chemistry 2017 Sci_Dir
Mitotic cell death induction by targeting the mitotic spindle with tubulin-inhibitory indole derivative molecules Oncotarget 2017 Sci_Dir
N-pyrrylarylsulfones with high therapeutic potential Molecules 2017 Sci_Dir
p38 MAPK differentially controls NK activating ligands at transcriptional and post-transcriptional level on multiple myeloma cells OncoImmunology 2017 Sci_Dir
Selenotriapine - An isostere of the most studied thiosemicarbazone with pronounced pro-apoptotic activity; low toxicity and ability to challenge phenotype reprogramming of 3-D mammary adenocarcinoma tumors Arabian Journal of Chemistry 2017 Sci_Dir
Anno: 2016
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Bicyclic γ-amino acids as inhibitors of γ-aminobutyrate aminotransferase Journal of Enzyme Inhibition and Medicinal Chemistry 2016 Sci_Dir
Focus on chirality of HIV-1 non-nucleoside reverse transcriptase inhibitors Molecules 2016 Sci_Dir
New Inhibitors of Indoleamine 2;3-Dioxygenase 1: Molecular Modeling Studies; Synthesis; and Biological Evaluation Journal of Medicinal Chemistry 2016 Sci_Dir
Pro-apoptotic and pro-differentiation induction by 8-quinolinecarboxaldehyde selenosemicarbazone and its Co(III) complex in human cancer cell lines MedChemComm 2016 Sci_Dir
Structure-based virtual screening to get new scaffold inhibitors of the Ser/Thr protein kinase PknB from mycobacterium tuberculosis Letters in Drug Design and Discovery 2016 Sci_Dir
Violacein; an indole-derived purple-colored natural pigment produced by Janthinobacterium lividum; inhibits the growth of head and neck carcinoma cell lines both in vitro and in vivo Tumor Biology 2016 Sci_Dir
VP1 crystal structure-guided exploration and optimization of 4;5-dimethoxybenzene-based inhibitors of rhinovirus 14 infection European Journal of Medicinal Chemistry 2016 Sci_Dir
Anno: 2015
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Antiproliferative and proapoptotic effects of a pyrrole containing arylthioindole in human Jurkat leukemia cell line and multidrug-resistant Jurkat/A4 cells Cancer Biology and Therapy 2015 Sci_Dir
Discovery of 1;1′-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors Journal of Medicinal Chemistry 2015 Sci_Dir
Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors Journal of Medicinal Chemistry 2015 Sci_Dir
Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB<inf>1</inf> among different membrane microenvironments Scientific Reports 2015 Sci_Dir
In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses Virology Journal 2015 Sci_Dir
Kinetic characterization of 4;4′-biphenylsulfonamides as selective non-zinc binding MMP inhibitors Journal of Enzyme Inhibition and Medicinal Chemistry 2015 Sci_Dir
New 1-phenyl-5-(1 H -pyrrol-1-yl)-1 H -pyrazole-3-carboxamides inhibit hepatitis C virus replication via suppression of cyclooxygenase-2 European Journal of Medicinal Chemistry 2015 Sci_Dir
New Frontiers in Selective Human MAO-B Inhibitors Journal of Medicinal Chemistry 2015 Sci_Dir
New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression; Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity; and Repression of Hedgehog-Dependent Cancer Journal of Medicinal Chemistry 2015 Sci_Dir
Pharmacological folding chaperones act as allosteric ligands of Frizzled4 Nature Chemical Biology 2015 Sci_Dir
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents Journal of Medicinal Chemistry 2015 Sci_Dir
Synthesis and pharmacological screening of a large library of 1;3;4-thiadiazolines as innovative therapeutic tools for the treatment of prostate cancer and melanoma European Journal of Medicinal Chemistry 2015 Sci_Dir
Anno: 2014
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
A new; simple; and high-yielding synthesis of 2;9-Dihydro-1 H- pyrido[3;4- b ]indol-1-ones Synthesis (Germany) 2014 Sci_Dir
An high-throughput in vivo screening system to select H3K4-specific histone demethylase inhibitors PLoS ONE 2014 Sci_Dir
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors Journal of Medicinal Chemistry 2014 Sci_Dir
Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors Journal of Medicinal Chemistry 2014 Sci_Dir
New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors European Journal of Medicinal Chemistry 2014 Sci_Dir
New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer Journal of Medicinal Chemistry 2014 Sci_Dir
Anno: 2013
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Arylsulfone-based HIV-1 non-nucleoside reverse transcriptase inhibitors Future Medicinal Chemistry 2013 Sci_Dir
Computer-aided identification; design and synthesis of a novel series of compounds with selective antiviral activity against chikungunya virus Antiviral Research 2013 Sci_Dir
Design; synthesis; and biological evaluation of 1-phenylpyrazolo[3;4- e ]pyrrolo[3;4- G ]indolizine-4;6(1 H;5 h)-diones as new glycogen synthase kinase-3β inhibitors Journal of Medicinal Chemistry 2013 Sci_Dir
Exploring 4-substituted-2-thiazolylhydrazones from 2-; 3-; and 4-acetylpyridine as selective and reversible hMAO-B inhibitors European Journal of Medicinal Chemistry 2013 Sci_Dir
New prospects for vinblastine analogues as anticancer agents Journal of Medicinal Chemistry 2013 Sci_Dir
Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors Journal of Medicinal Chemistry 2013 Sci_Dir
Anno: 2012
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Apple can act as anti-aging on yeast cells Oxidative Medicine and Cellular Longevity 2012 Sci_Dir
De novo computer-aided design of novel antiviral agents Drug Discovery Today: Technologies 2012 Sci_Dir
Histone deacetylase inhibitors: Structure-based modeling and isoform-selectivity prediction Journal of Chemical Information and Modeling 2012 Sci_Dir
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB 1 receptor Journal of Medicinal Chemistry 2012 Sci_Dir
Mechanism of interaction of novel indolylarylsulfone derivatives with K103N and Y181I mutant HIV-1 reverse transcriptase in complex with its substrates Antiviral Chemistry and Chemotherapy 2012 Sci_Dir
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors Journal of Medicinal Chemistry 2012 Sci_Dir
The tubulin colchicine domain: A molecular modeling perspective ChemMedChem 2012 Sci_Dir
Venting-while-heating microwave-assisted synthesis of 3-arylthioindoles ACS Combinatorial Science 2012 Sci_Dir
Anno: 2011
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: An effective scaffold for the design of either CB 1 or CB 2 receptor ligands European Journal of Medicinal Chemistry 2011 Sci_Dir
Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability Journal of Medicinal Chemistry 2011 Sci_Dir
Drug-induced inhibition of tubulin polymerization induces mitochondrion-mediated apoptosis in yeast Cell Cycle 2011 Sci_Dir
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: New cyclic substituents at indole-2-carboxamide Journal of Medicinal Chemistry 2011 Sci_Dir
Open vessel and cooling while heating microwave-assisted synthesis of pyridinyl N-Aryl hydrazones ACS Combinatorial Science 2011 Sci_Dir
Anno: 2010
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds PLoS ONE 2010 Sci_Dir
Arylthioindoles: Promising compounds against cancer cell proliferation Oncology Letters 2010
Enantioselective HPLC combined with spectroscopic methods: A valid strategy to determine the absolute configuration of potential β-secretase inhibitors Talanta 2010 Sci_Dir
Looking for an active conformation of the future HIV type-1 non-nucleoside reverse transcriptase inhibitors Antiviral Chemistry and Chemotherapy 2010 Sci_Dir
Pyrrolo[1;2-b][1;2;5]benzothiadiazepines (PBTDs) exert their anti-proliferative activity by interfering with Akt-mTOR signaling and bax:bcl-2 ratio modulation in cells from chronic myeloid leukemic patients Cancer Science 2010 Sci_Dir
Radiosynthesis and in vivo evaluation of [11C]-labelled pyrrole-2-carboxamide derivates as novel radioligands for PET imaging of monoamine oxidase A Nuclear Medicine and Biology 2010 Sci_Dir
Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1- yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands European Journal of Medicinal Chemistry 2010 Sci_Dir
Anno: 2009
Titolo pubblicazione Rivista Anno link Scopus link Sci_Dir
Boom in the development of non-peptidic β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease Medicinal Research Reviews 2009 Sci_Dir
Indolylarylsulfones bearing natural and unnatural amino acids. discovery of potent inhibitors of hiv-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie b4 virus Journal of Medicinal Chemistry 2009 Sci_Dir
New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis; tubulin polymerization; cell growth inhibition; and molecular modeling studies Journal of Medicinal Chemistry 2009 Sci_Dir
Non-nucleoside HIV-1 reverse transcriptase inhibitors di-halo-indolyl aryl sulfones achieve tight binding to drug-resistant mutants by targeting the enzyme-substrate complex Antiviral Research 2009 Sci_Dir
Study of the effects of a new pyrazolecarboxamide: Changes in mitochondria and induction of apoptosis International Journal of Biochemistry and Cell Biology 2009 Sci_Dir
Synthesis; cannabinoid receptor affinity; molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivity Bioorganic and Medicinal Chemistry 2009 Sci_Dir
Synthetic strategies of nonpeptidic β-secretase (BACE1) inhibitors Journal of Heterocyclic Chemistry 2009 Sci_Dir

© Università degli Studi di Roma "La Sapienza" - Piazzale Aldo Moro 5, 00185 Roma