G. La Regina

发表

Imidazole analogues of fluoxetine, a novel class of anti-Candida agents.

R. Silvestri, M. Artico, G. La Regina, 2004, Journal of medicinal chemistry.

Anticancer Activity of (S)-5-Chloro-3-((3,5-dimethylphenyl)sulfonyl)-N-(1-oxo-1-((pyridin-4-ylmethyl)amino)propan-2-yl)-1H-indole-2-carboxamide (RS4690), a New Dishevelled 1 Inhibitor

A. Coluccia, R. Silvestri, G. La Regina, 2022, Cancers.

New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.

C. Limatola, O. Turriziani, A. Coluccia, 2020, European journal of medicinal chemistry.

Computer-Aided Identification and Lead Optimization of Dual Murine Double Minute 2 and 4 Binders: Structure-Activity Relationship Studies and Pharmacological Activity.

Ettore Novellino, Luciana Marinelli, Sandro Cosconati, 2017, Journal of medicinal chemistry.

Chiral resolution and binding study of 1,3,4,14b-tetrahydro-2,10-dimethyl-2H,10H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine) and 2-methyl-1,3,4,14b-tetrahydro-2H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzothiadiazepine 10,10-dioxide (tiaaptazepine).

R. Silvestri, M. Artico, G. La Regina, 2005, Farmaco.

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

R. Silvestri, G. La Regina, R. Bei, 2016, Tumor Biology.

Inhibition of dengue virus replication by novel inhibitors of RNA-dependent RNA polymerase and protease activities

A. Coluccia, R. Silvestri, G. La Regina, 2017, Journal of enzyme inhibition and medicinal chemistry.

Apple Can Act as Anti-Aging on Yeast Cells

R. Silvestri, G. La Regina, C. Mazzoni, 2012, Oxidative medicine and cellular longevity.

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

R. Silvestri, G. La Regina, V. Jovanović, 2017, Arabian Journal of Chemistry.

New Inhibitors of Indoleamine 2,3-Dioxygenase 1: Molecular Modeling Studies, Synthesis, and Biological Evaluation.

A. Coluccia, R. Silvestri, G. La Regina, 2016, Journal of medicinal chemistry.

New 6- and 7-heterocyclyl-1H-indole derivatives as potent tubulin assembly and cancer cell growth inhibitors.

C. Martini, A. Coluccia, R. Silvestri, 2018, European journal of medicinal chemistry.

Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors.

C. Supuran, A. Coluccia, D. Vullo, 2015, Journal of medicinal chemistry.

Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents

A. Coluccia, R. Silvestri, G. La Regina, 2019, ACS medicinal chemistry letters.

Arylthioindoles: Promising compounds against cancer cell proliferation.

R. Silvestri, G. La Regina, A. Scovassi, 2010, Oncology Letters.

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.

E. Novellino, A. Lavecchia, A. Coluccia, 2009, Journal of medicinal chemistry.

Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.

Y. Ni, E. Novellino, B. Maresca, 2013, Journal of medicinal chemistry.

p38 MAPK differentially controls NK activating ligands at transcriptional and post-transcriptional level on multiple myeloma cells

R. Silvestri, G. La Regina, A. Santoni, 2017, Oncoimmunology.

Enantioselective HPLC combined with spectroscopic methods: a valid strategy to determine the absolute configuration of potential beta-secretase inhibitors.

R. Silvestri, G. La Regina, R. Cirilli, 2010, Talanta.

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.

S. Zanoli, G. Maga, R. Silvestri, 2009, Antiviral research.

1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: an effective scaffold for the design of either CB1 or CB2 receptor ligands.

E. Novellino, R. Silvestri, G. La Regina, 2011, European journal of medicinal chemistry.

RS4651 suppresses lung fibroblast activation via the TGF-β1/SMAD signalling pathway.

R. Silvestri, G. La Regina, Haoyan Wang, 2021, European journal of pharmacology.

Discovery of novel human lactate dehydrogenase inhibitors: Structure-based virtual screening studies and biological assessment.

A. Coluccia, R. Silvestri, G. La Regina, 2022, European journal of medicinal chemistry.

Towards modern anticancer agents that interact with tubulin

A. Coluccia, R. Silvestri, G. La Regina, 2019, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Radiosynthesis and in vivo evaluation of [11C]-labelled pyrrole-2-carboxamide derivates as novel radioligands for PET imaging of monoamine oxidase A.

R. Silvestri, G. La Regina, S. Staelens, 2010, Nuclear medicine and biology.

Induction of Ferroptosis in Glioblastoma and Ovarian Cancers by a New Pyrrole Tubulin Assembly Inhibitor

A. Coluccia, A. Ciogli, R. Silvestri, 2022, Journal of medicinal chemistry.

Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.

A. Coluccia, R. Silvestri, M. Artico, 2005, Journal of medicinal chemistry.

An Innovation 10 Years in the Making: The Stories in the Pages of ACS Medicinal Chemistry Letters.

G. La Regina, W. Pomerantz, Zhengqiu Li, 2022, ACS medicinal chemistry letters.

Switching on the activity of 1,5-diaryl-pyrrole derivatives against drug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies.

Mohammad K. Islam, A. Coluccia, R. Silvestri, 2019, European journal of medicinal chemistry.

Arylsulfone-based HIV-1 non-nucleoside reverse transcriptase inhibitors.

A. Coluccia, A. Brancale, R. Silvestri, 2013, Future medicinal chemistry.

New arylthioindoles: potent inhibitors of tubulin polymerization. 2. Structure-activity relationships and molecular modeling studies.

Andrea Brancale, Gabriela Chiosis, Ernest Hamel, 2006, Journal of medicinal chemistry.

Arylthioindoles, potent inhibitors of tubulin polymerization.

Andrea Brancale, Ernest Hamel, Antonio Coluccia, 2004, Journal of medicinal chemistry.

New pyrrole inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A and MAO-B selectivity.

E. Novellino, A. Lavecchia, R. Silvestri, 2007, Journal of medicinal chemistry.

Synthesis, structure-activity relationships and molecular modeling studies of new indole inhibitors of monoamine oxidases A and B.

E. Novellino, A. Lavecchia, R. Silvestri, 2008, Bioorganic & medicinal chemistry.

New arylthioindoles and related bioisosteres at the sulfur bridging group. 4. Synthesis, tubulin polymerization, cell growth inhibition, and molecular modeling studies.

E. Novellino, B. Maresca, A. Coluccia, 2009, Journal of medicinal chemistry.

Indolyl Aryl Sulphones as HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: Synthesis, Biological Evaluation and Binding Mode Studies of New Derivatives at Indole-2-carboxamide

A. Bergamini, C. Ciaprini, A. Coluccia, 2006, Antiviral chemistry & chemotherapy.

Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.

E. Novellino, C. Pannecouque, A. Coluccia, 2011, Journal of medicinal chemistry.

Arylthioindole inhibitors of tubulin polymerization. 3. Biological evaluation, structure-activity relationships and molecular modeling studies.

Anna Ivana Scovassi, Ettore Novellino, Andrea Brancale, 2007, Journal of medicinal chemistry.

Anti-HIV-1 activity of pyrryl aryl sulfone (PAS) derivatives: synthesis and SAR studies of novel esters and amides at the position 2 of the pyrrole nucleus.

R. Silvestri, M. Artico, G. La Regina, 2004, Farmaco.

Venting-while-heating microwave-assisted synthesis of 3-arylthioindoles.

R. Silvestri, G. La Regina, F. Piscitelli, 2012, ACS combinatorial science.

Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.

A. Bergamini, C. Ciaprini, E. Novellino, 2006, Journal of medicinal chemistry.

Open vessel and cooling while heating microwave-assisted synthesis of pyridinyl N-aryl hydrazones.

R. Silvestri, G. La Regina, F. Piscitelli, 2011, ACS combinatorial science.

Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.

M. Conconi, A. Coluccia, P. Brun, 2014, Journal of medicinal chemistry.

Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors.

E. Novellino, A. Coluccia, A. Brancale, 2013, Journal of medicinal chemistry.

Design and synthesis of 2-heterocyclyl-3-arylthio-1H-indoles as potent tubulin polymerization and cell growth inhibitors with improved metabolic stability.

Ettore Novellino, Andrea Brancale, Ilaria Granata, 2011, Journal of medicinal chemistry.

Simple, potent, and selective pyrrole inhibitors of monoamine oxidase types A and B.

Enzo Agostinelli, Romano Silvestri, R. Silvestri, 2003, Journal of medicinal chemistry.

Synthesis, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.

E. Novellino, A. Lavecchia, M. Botta, 2008, Journal of medicinal chemistry.

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.

E. Novellino, L. Di Marcotullio, C. Martini, 2015, Journal of medicinal chemistry.

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.

Ettore Novellino, Andrea Brancale, Ruoli Bai, 2014, Journal of medicinal chemistry.

Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.

E. Novellino, A. Lavecchia, R. Silvestri, 2010, European journal of medicinal chemistry.

Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.

A. Bergamini, C. Ciaprini, E. Crespan, 2005, Journal of medicinal chemistry.

Comparative study between the polysaccharide-based chiralcel OJ and chiralcel OD CSPSs in chromatographic enantioseparation of imidazole analogues of fluoxetine and miconazole.

R. Silvestri, G. La Regina, R. Cirilli, 2005, Journal of separation science.

Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.

R. Silvestri, M. Artico, G. La Regina, 2004, Journal of medicinal chemistry.

Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.

Silvio Massa, Romano Silvestri, R. Silvestri, 2003, Journal of medicinal chemistry.

Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.

E. Novellino, A. Coluccia, A. Brancale, 2014, Journal of Medicinal Chemistry.

New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.

E. Novellino, B. Clotet, A. Coluccia, 2014, European journal of medicinal chemistry.

Single‐run chemo‐ and enantio‐selective high‐performance liquid chromatography separation of tramadol and its principal metabolite, O‐desmethyltramadol, using a chlorinated immobilized amylose‐based chiral stationary phase under multimodal elution conditions

R. Silvestri, G. La Regina, Chiara Cantatore, 2022, SEPARATION SCIENCE PLUS.

Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A new class of agents with high apoptotic activity in chronic myelogenous leukemia K562 cells and in cells from patients at onset and who were imatinib-resistant.

E. Novellino, M. Russo, A. Lavecchia, 2006, Journal of medicinal chemistry.

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 profile.

E. Novellino, A. Lavecchia, R. Silvestri, 2009, Bioorganic & medicinal chemistry.

PYRROLO[1,2-b][1,2,5]BENZOTHIADIAZEPINES (PBTDs) induce apoptosis in K562 cells

M. Russo, R. Silvestri, G. La Regina, 2007, BMC Cancer.

High Potency of Indolyl Aryl Sulfone Nonnucleoside Inhibitors towards Drug-Resistant Human Immunodeficiency Virus Type 1 Reverse Transcriptase Mutants Is Due to Selective Targeting of Different Mechanistic Forms of the Enzyme

E. Crespan, S. Zanoli, G. Maga, 2005, Antimicrobial Agents and Chemotherapy.

CXCR4 antagonism sensitizes cancer cells to novel indole-based MDM2/4 inhibitors in glioblastoma multiforme.

E. Novellino, S. Taliani, C. Martini, 2021, European journal of pharmacology.

Bax Activation Blocks Self-Renewal and Induces Apoptosis of Human Glioblastoma Stem Cells.

E. Novellino, F. Da Settimo, S. Taliani, 2017, ACS chemical neuroscience.

Targeting PDZ domains as potential treatment for viral infections, neurodegeneration and cancer

A. Coluccia, R. Silvestri, G. La Regina, 2021, Biology direct.

Emerging Therapeutic Agents for Colorectal Cancer

R. Silvestri, G. La Regina, S. Gianni, 2021, Molecules.

Sulfonamide Inhibitors of β‐Catenin Signaling as Anticancer Agents with Different Output on c‐MYC

A. Coluccia, A. Ciogli, R. Silvestri, 2020 .

Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.

C. Limatola, E. Novellino, A. Coluccia, 2017, Journal of medicinal chemistry.

Kinetic characterization of 4,4′-biphenylsulfonamides as selective non-zinc binding MMP inhibitors

C. Supuran, R. Silvestri, G. La Regina, 2015, Journal of enzyme inhibition and medicinal chemistry.

An High-Throughput In Vivo Screening System to Select H3K4-Specific Histone Demethylase Inhibitors

E. Cundari, A. Coluccia, R. Silvestri, 2014, PloS one.

Rimonabant-Based Compounds Bearing Hydrophobic Amino Acid Derivatives as Cannabinoid Receptor Subtype 1 Ligands

A. Mollica, R. Silvestri, G. La Regina, 2023, ACS medicinal chemistry letters.

Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.

E. Novellino, S. Taliani, C. Martini, 2015, Journal of medicinal chemistry.

Small Molecule Inhibitors of KDM5 Histone Demethylases Increase the Radiosensitivity of Breast Cancer Cells Overexpressing JARID1B

A. Mollica, E. Cundari, A. Coluccia, 2018, Molecules.

Pharmacological folding chaperones act as allosteric ligands of Frizzled4.

E. Novellino, R. Silvestri, G. La Regina, 2015, Nature chemical biology.

3-Aroyl-1,4-diarylpyrroles Inhibit Chronic Myeloid Leukemia Cell Growth through an Interaction with Tubulin.

A. Coluccia, A. Brancale, R. Silvestri, 2017, ACS medicinal chemistry letters.

Discovery of a Novel Class of Norovirus Inhibitors with High Barrier of Resistance

J. Matthijnssens, R. Silvestri, G. La Regina, 2021, Pharmaceuticals.

'Normolipidemic' tendinous and tuberous xanthomatosis.

G. La Regina, P. Preda, A. Gaddi, 1996, Dermatology.

Indole-2-carboxamides as allosteric modulators of the cannabinoid CB₁ receptor.

E. Novellino, A. Coluccia, R. Silvestri, 2012, Journal of medicinal chemistry.

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.

C. Martini, A. Coluccia, R. Silvestri, 2019, European journal of medicinal chemistry.

Indolyl aryl sulphones as HIV-1 reverse transcriptase inhibitors: docking and 3D QSAR studies

R. Silvestri, G. La Regina, R. Ragno, 2007, Expert opinion on drug discovery.

Emerging Direct Targeting β-Catenin Agents

R. Silvestri, G. La Regina, A. Urbani, 2022, Molecules.

A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist.

Ettore Novellino, Antonella Accardo, Romano Silvestri, 2018, Biochemistry.

Structure-Based Drug Design of Potent Pyrazole Derivatives against Rhinovirus Replication.

A. Coluccia, R. Silvestri, G. La Regina, 2018, Journal of medicinal chemistry.

New 1-phenyl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides inhibit hepatitis C virus replication via suppression of cyclooxygenase-2.

A. Coluccia, C. Zamperini, M. Botta, 2015, European journal of medicinal chemistry.

Study of the effects of a new pyrazolecarboxamide: changes in mitochondria and induction of apoptosis.

R. Silvestri, G. La Regina, A. Scovassi, 2009, The international journal of biochemistry & cell biology.

1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studies.

S. Kelly, D. Lamb, M. Botta, 2008, Journal of medicinal chemistry.

β-catenin knockdown promotes NHERF1-mediated survival of colorectal cancer cells: implications for a double-targeted therapy

I. Fournier, A. Coluccia, R. Silvestri, 2018, Oncogene.

A Novel Validated UHPLC Method for the Estimation of Rosuvastatin and Its Complete Impurity Profile in Tablet Formulations

R. Silvestri, G. La Regina, Michela Puxeddu, 2023, Molecules.

RS6077 induces mitotic arrest and selectively activates cell death in human cancer cell lines and in a lymphoma tumor in vivo.

D. Trisciuoglio, R. Silvestri, G. La Regina, 2022, European journal of medicinal chemistry.

Novel N-(Heterocyclylphenyl)benzensulfonamide Sharing an Unreported Binding Site with T-Cell Factor 4 at the β-Catenin Armadillo Repeats Domain as an Anticancer Agent.

A. Coluccia, R. Silvestri, G. La Regina, 2023, ACS pharmacology & translational science.

Sulfonamide Inhibitors of ß-Catenin Signaling with Different Output on c-MYC as Anticancer Agents.

A. Coluccia, A. Ciogli, R. Silvestri, 2020, ChemMedChem.

Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.

C. Martini, A. Coluccia, R. Silvestri, 2021, European journal of medicinal chemistry.

Targeting the Grb2 cSH3 domain: Design, synthesis and biological evaluation of the first series of modulators.

A. Coluccia, R. Silvestri, G. La Regina, 2023, Bioorganic chemistry (Print).

New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.

E. Novellino, B. Clotet, A. Coluccia, 2012, Journal of medicinal chemistry.

Discovery of Zika Virus NS2B/NS3 Inhibitors That Prevent Mice from Life-Threatening Infection and Brain Damage.

A. Coluccia, R. Silvestri, G. La Regina, 2020, ACS medicinal chemistry letters.

Modulating undruggable targets to overcome cancer therapy resistance.

R. Silvestri, G. La Regina, A. Vessières, 2021, Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy.

Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.

C. Limatola, E. Novellino, A. Coluccia, 2017, Journal of medicinal chemistry.

Recent Advances in Drug Discovery for Triple-Negative Breast Cancer Treatment

R. Silvestri, G. La Regina, C. Naro, 2023, Molecules.

New pyrrole derivatives with potent tubulin polymerization inhibiting activity as anticancer agents including hedgehog-dependent cancer.

E. Novellino, L. Di Marcotullio, A. Brancale, 2014, Journal of medicinal chemistry.

Toward highly potent cancer agents by modulating the C-2 group of the arylthioindole class of tubulin polymerization inhibitors.

Y. Ni, E. Novellino, B. Maresca, 2013, Journal of medicinal chemistry.

RS6077 induces mitotic arrest and selectively activates cell death in human cancer cell lines and in a lymphoma tumor in vivo.

D. Trisciuoglio, R. Silvestri, G. La Regina, 2022, European journal of medicinal chemistry.

Open vessel and cooling while heating microwave-assisted synthesis of pyridinyl N-aryl hydrazones.

R. Silvestri, G. La Regina, F. Piscitelli, 2011, ACS combinatorial science.

Metabolic Rewiring in Cancer: Small Molecule Inhibitors in Colorectal Cancer Therapy

R. Silvestri, G. La Regina, Michela Puxeddu, 2024, Molecules.

4-(3-Phenyl-4-(3,4,5-trimethoxybenzoyl)-1H-pyrrol-1-yl)benzenesulfonamide, a Novel Carbonic Anhydrase and Wnt/β-Catenin Signaling Pathway Dual-Targeting Inhibitor with Potent Activity against Multidrug Resistant Cancer Cells

C. Supuran, R. Silvestri, G. La Regina, 2023, Journal of medicinal chemistry.