Search filters

List of works by Antonio Lavecchia

2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching

scientific article published in December 2005

3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.

scientific article published on February 2001

5'-C-Ethyl-tetrazolyl-N(6)-substituted adenosine and 2-chloro-adenosine derivatives as highly potent dual acting A1 adenosine receptor agonists and A3 adenosine receptor antagonists

scientific article published on 27 February 2015

A compound-based proteomic approach discloses 15-ketoatractyligenin methyl ester as a new PPARγ partial agonist with anti-proliferative ability

scientific article (publication date: 24 January 2017)

A1 adenosine receptor antagonists, 3-aryl[1,2,4]triazino[4,3-a]benzimidazol-4-(10H)-ones (ATBIs) andN-alkyl andN-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs): Different recognition of bovine and human binding sites

APP Maturation and Intracellular Localization Are Controlled by a Specific Inhibitor of 37/67 kDa Laminin-1 Receptor in Neuronal Cells

scientific article published on 04 March 2020

Adenosine signalling mediates the anti-inflammatory effects of the COX-2 inhibitor nimesulide

scientific article published on 14 May 2016

Amorfrutins are efficient modulators of peroxisome proliferator-activated receptor gamma (PPARγ) with potent antidiabetic and anticancer properties: a patent evaluation of WO2014177593 A1.

scientific article published in January 2015

Antitumor agents 4. Characterization of free radicals produced during reduction of the antitumor drug 5H-pyridophenoxazin-5-one: an EPR study

scientific article published in October 2003

Antitumor agents 6. Synthesis, structure-activity relationships, and biological evaluation of spiro[imidazolidine-4,3'-thieno[2,3-g]quinoline]-tetraones and spiro[thieno[2,3-g]quinoline-3,5'-[1,2,4]triazinane]-tetraones with potent antiproliferative

scientific article

Antitumor agents 7. Synthesis, antiproliferative activity and molecular modeling of new l-lysine-conjugated pyridophenoxazinones as potent DNA-binding ligands and topoisomerase IIα inhibitors

scientific article published on 14 December 2019

Antitumor agents. 1. Synthesis, biological evaluation, and molecular modeling of 5H-pyrido[3,2-a]phenoxazin-5-one, a compound with potent antiproliferative activity

scientific article published in November 2002

Antitumor agents. 2. Synthesis, structure-activity relationships, and biological evaluation of substituted 5H-pyridophenoxazin-5-ones with potent antiproliferative activity

scientific article published in November 2002

Antitumor agents. 3. Design, synthesis, and biological evaluation of new pyridoisoquinolindione and dihydrothienoquinolindione derivatives with potent cytotoxic activity

scientific article published on February 2004

Antitumor agents. 5. synthesis, structure-activity relationships, and biological evaluation of dimethyl-5H-pyridophenoxazin-5-ones, tetrahydro-5h-benzopyridophenoxazin-5-ones, and 5h-benzopyridophenoxazin-5-ones with potent antiproliferative activit

scientific article published on August 2006

Architecture of the Human Urotensin II Receptor: Comparison of the Binding Domains of Peptide and Non-Peptide Urotensin II Agonists

scientific article published on 01 April 2005

Architecture of the Human Urotensin II Receptor: Comparison of the Binding Domains of Peptide and Non-Peptide Urotensin II Agonists

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

scientific article published on 12 May 2007

Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 1).

scientific article published on December 2006

Arylthiopyrrole (AThP) derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors: synthesis, structure-activity relationships, and docking studies (part 2).

scientific article published on December 2006

Benzothiopyranoindole-Based Antiproliferative Agents: Synthesis, Cytotoxicity, Nucleic Acids Interaction, and Topoisomerases Inhibition Properties

scientific article published on 01 September 2009

CDC25 Inhibition in Acute Myeloid Leukemia-A Study of Patient Heterogeneity and the Effects of Different Inhibitors

scientific article

CDC25 phosphatase inhibitors: an update

scientific article published on January 2012

CDC25A and B dual-specificity phosphatase inhibitors: potential agents for cancer therapy.

scientific article published on January 2009

Characterizing the 1,4-dihydropyridines binding interactions in the L-type Ca2+ channel: model construction and docking calculations

scientific article published on 3 March 2007

Chiral phenoxyacetic acid analogues inhibit colon cancer cell proliferation acting as PPARγ partial agonists

scientific article published on 01 April 2019

Computer-assisted design, synthesis and biological evaluation of novel pyrrolyl heteroaryl sulfones targeted at HIV-1 reverse transcriptase as non-nucleoside inhibitors.

scientific article

Conformational analysis of furanoid epsilon-sugar amino acid containing cyclic peptides by NMR spectroscopy, molecular dynamics simulation, and X-ray crystallography: evidence for a novel turn structure

scientific article published in September 2003

Conformational switch of a flexible loop in human laminin receptor determines laminin-1 interaction ⬇️

scientific article published on 01 March 2012

Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design

scientific article

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

scientific article published on 21 November 2011

Design, Molecular Modeling, Synthesis, and Anti-HIV-1 Activity of New Indolyl Aryl Sulfones. Novel Derivatives of the Indole-2-carboxamide

article

Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175.

scientific article

Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists

scientific article published in November 2002

Design, synthesis, biological evaluation, and molecular modeling studies of TIBO-like cyclic sulfones as non-nucleoside HIV-1 reverse transcriptase inhibitors

scientific article published on January 2006

Development of Novel Amides as Noncovalent Inhibitors of Immunoproteasomes

scientific article published on 26 March 2019

Development of novel selective peptidomimetics containing a boronic acid moiety, targeting the 20S proteasome as anticancer agents

scientific article

Development of peptidomimetic boronates as proteasome inhibitors

article

Diarylheterocycle Core Ring Features Effect in Selective COX-1 Inhibition

scientific article published on 25 January 2012

Discovery of New Inhibitors of Cdc25B Dual Specificity Phosphatases by Structure-Based Virtual Screening

scientific article published on 01 May 2012

Discovery of New Small Molecules Targeting the Vitronectin-Binding Site of the Urokinase Receptor That Block Cancer Cell Invasion ⬇️

scientific article published on May 22, 2013

Discovery of Novel Naphthylphenylketone and Naphthylphenylamine Derivatives as Cell Division Cycle 25B (CDC25B) Phosphatase Inhibitors: Design, Synthesis, Inhibition Mechanism, and in Vitro Efficacy against Melanoma Cell Lines

scientific article published on 24 July 2019

Discovery of a novel small molecule inhibitor targeting the frataxin/ubiquitin interaction via structure-based virtual screening and bioassays

scientific article

Discovery of new small molecules inhibiting 67 kDa laminin receptor interaction with laminin and cancer cell invasion

scientific article

Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design

scientific article published in October 2003

Elucidation of the enantioselective recognition mechanism of a penicillin G acylase-based chiral stationary phase towards a series of 2-aryloxy-2-arylacetic acids

scientific article published on 01 August 2006

Emerging role of the β-catenin-PPARγ axis in the pathogenesis of colorectal cancer

scientific article

Enantiomeric separation of 2-aryloxyalkyl- and 2-arylalkyl-2-aryloxyacetic acids on a Penicillin G Acylase-based chiral stationary phase: influence of the chemical structure on retention and enantioselectivity.

scientific article published on 12 June 2007

Enantioselective hydrolysis of some 2-aryloxyalkanoic acid methyl esters and isosteric analogues using a penicillin G acylase-based HPLC monolithic silica column

scientific article published in February 2003

Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors

scientific article published in March 2009

Exploring Structural Relationships between Bioactive and Commercial Chemical Space and Developing Target Hypotheses for Compound Acquisition

Exploring the Role of N6-Substituents in Potent Dual Acting 5'-C-Ethyltetrazolyladenosine Derivatives: Synthesis, Binding, Functional Assays, and Antinociceptive Effects in Mice ∇.

scientific article published on 27 April 2017

Exploring the molecular basis of the enantioselective binding of penicillin G acylase towards a series of 2-aryloxyalkanoic acids: a docking and molecular dynamics study

scientific article published on 8 August 2006

Frontal affinity chromatography with MS detection of the ligand binding domain of PPARγ receptor: Ligand affinity screening and stereoselective ligand–macromolecule interaction ⬇️

scientific article published on October 19, 2011

Identification of a new series of amides as non-covalent proteasome inhibitors.

scientific article published on 25 January 2014

Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual screening.

scientific article

Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation

scientific article published on 18 September 2018

In silico methods to address polypharmacology: current status, applications and future perspectives

scientific article

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

scientific article published on April 2009

Inhibition of 37/67kDa Laminin-1 Receptor Restores APP Maturation and Reduces Amyloid-β in Human Skin Fibroblasts from Familial Alzheimer's Disease

scientific article published on 16 November 2020

Inhibitors of Cdc25 phosphatases as anticancer agents: a patent review

scientific article published on March 2010

Insights into the mechanism of partial agonism: crystal structures of the peroxisome proliferator-activated receptor gamma ligand-binding domain in the complex with two enantiomeric ligands

scientific article

Investigational drugs targeting cyclin-dependent kinases for the treatment of cancer: an update on recent findings (2013-2016).

scientific article published on 8 September 2016

Isoxazole-Based-Scaffold Inhibitors Targeting Cyclooxygenases (COXs)

scientific article published on 02 May 2016

LT175 is a novel PPARα/γ ligand with potent insulin-sensitizing effects and reduced adipogenic properties.

scientific article published on 22 January 2014

Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists

scientific article published in June 2005

Ligand-based chemoinformatic discovery of a novel small molecule inhibitor targeting CDC25 dual specificity phosphatases and displaying in vitro efficacy against melanoma cells

scientific article published on 13 October 2015

Machine-learning approaches in drug discovery: methods and applications

scientific article

Modeling of Cdc25B Dual Specifity Protein Phosphatase Inhibitors: Docking of Ligands and Enzymatic Inhibition Mechanism

article

Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists.

scientific article published on 24 February 2013

N-Formyl Peptide Receptors Induce Radical Oxygen Production in Fibroblasts Derived From Systemic Sclerosis by Interacting With a Cleaved Form of Urokinase Receptor

scientific article published on 4 April 2018

N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice

scientific article

N6-Cycloalkyl- andN6-Bicycloalkyl-C5′(C2′)-modified Adenosine Derivatives as High-Affinity and Selective Agonists at the Human A1Adenosine Receptor with Antinociceptive Effects in Mice

Naphtho[1,2-d]isothiazole acetic acid derivatives as a novel class of selective aldose reductase inhibitors.

scientific article

New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression

scientific article

New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function

scientific article

New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.

scientific article published on 24 December 2016

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

scientific article

Novel Benzylidene Thiazolidinedione Derivatives as Partial PPARγ Agonists and their Antidiabetic Effects on Type 2 Diabetes

scientific article

Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.

scientific article

Novel bifunctional quinolonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, biological activities, and mechanism of action

scientific article published on March 2006

Novel inhibitors of signal transducer and activator of transcription 3 signaling pathway: an update on the recent patent literature.

scientific article published on 16 January 2014

Novel non-peptide small molecules preventing IKKβ/NEMO association inhibit NF-κB activation in LPS-stimulated J774 macrophages.

scientific article published on 14 January 2016

Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities

scientific article published on 23 July 2008

Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.

scientific article published in August 2005

Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives

scientific article

On the metabolically active form of metaglidasen: improved synthesis and investigation of its peculiar activity on peroxisome proliferator-activated receptors and skeletal muscles

scientific article

Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors

scientific article

Pyrido[1,2-a]pyrimidin-4-one Derivatives as a Novel Class of Selective Aldose Reductase Inhibitors Exhibiting Antioxidant Activity

scientific article published on 11 September 2007

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

article

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

Reaction between quinone and thiazolidine. A study on the formation mechanism of new antiproliferative quinolindiones

Ribose-modified purine nucleosides as ribonucleotide reductase inhibitors. Synthesis, antitumor activity, and molecular modeling of N6-substituted 3'-C-methyladenosine derivatives.

scientific article

STAT-3 inhibitors: state of the art and new horizons for cancer treatment.

scientific article published on January 2011

Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles.

scientific article published on 2 January 2014

Selective PPARγ modulators for Type 2 diabetes treatment: how far have we come and what does the future hold?

scientific article published on 19 April 2018

Small Molecule Drugs And Targeted Therapy For Melanoma: Current Strategies And Future Directions.

scientific article published on 14 April 2017

Spirohydantoin derivatives of thiopyrano[2,3-b]pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors.

scientific article published in January 2005

Structural basis for PPAR partial or full activation revealed by a novel ligand binding mode

scientific article published on 6 October 2016

Structural development studies of PPARs ligands based on tyrosine scaffold

scientific article published on 31 October 2014

Structural insight into peroxisome proliferator-activated receptor gamma binding of two ureidofibrate-like enantiomers by molecular dynamics, cofactor interaction analysis, and site-directed mutagenesis

scientific article published on June 2010

Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A1 Adenosine Receptor Agonists.

scientific article published on 19 December 2017

Structure-activity studies of the melanocortin peptides: discovery of potent and selective affinity antagonists for the hMC3 and hMC4 receptors

scientific article published in November 2002

Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase

scientific article

Syntheses, biological evaluation, and molecular modeling of 18F-labeled 4-anilidopiperidines as mu-opioid receptor imaging agents

scientific article published in December 2005

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

scientific article published on October 2010

Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors α/γ dual agonists

scientific article

Synthesis, biological evaluation, and molecular modeling investigation of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives with PPARalpha and PPARgamma agonist activity.

scientific article published on 19 September 2008

Synthesis, biological evaluation, and molecular modeling investigation of chiral phenoxyacetic acid analogues with PPARalpha and PPARgamma agonist activity.

scientific article published on May 2007

Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity

scientific article published on August 2005

Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists

scientific article published in March 2005

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

scientific article

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 selec

scientific article published on 21 June 2009

Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity

scientific article

Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors

scientific article published on 16 May 2013

Synthesis, pharmacological evaluation, and molecular modeling studies of novel peptidic CAAX analogues as farnesyl-protein-transferase inhibitors

scientific article published on March 2006

The 37/67 kDa laminin receptor (LR) inhibitor, NSC47924, affects 37/67 kDa LR cell surface localization and interaction with the cellular prion protein.

scientific article published on 13 April 2016

The antiproliferative and proapoptotic effects of cladosporols A and B are related to their different binding mode as PPARγ ligands

scientific article published on 16 March 2016

Therapeutic targeting the cell division cycle 25 (CDC25) phosphatases in human acute myeloid leukemia--the possibility to target several kinases through inhibition of the various CDC25 isoforms.

scientific article

Thiazolidin-4-one formation. Mechanistic and synthetic aspects of the reaction of imines and mercaptoacetic acid under microwave and conventional heating

scientific article published on 3 September 2004

Urokinase-type plasminogen activator receptor (uPAR) expression enhances invasion and metastasis in RAS mutated tumors.

scientific article published on 24 August 2017

Virtual screening strategies in drug discovery: a critical review.

scientific article published on January 2013

[1,2,4]Triazino[4,3-a]benzimidazole acetic acid derivatives: a new class of selective aldose reductase inhibitors.

scientific article published in December 2001

Paulina is supported by:

About Paulina

Help