List of works - Gianluca Sbardella

3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A.

scientific article published in March 2002

3-(1H-pyrrol-2-yl)-2-oxazolidinones as novel monoamine oxidase type A inhibitors

scientific article published in March 2005

3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors

scientific article published in June 2001

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives

scientific article

5-Alkyl-2-alkylamino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family.

scientific article published on March 2005

6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase

scientific article published on November 2005

6-alkylthio-4-[1-(2,6-difluorophenyl)alkyl]-1H-[1,3,5]triazin-2-ones (ADATs): novel regulators of cell differentiation and proliferation

scientific article published on October 2006

A TR‐FRET‐Based Functional Assay for Screening Activators of CARM1 ⬇️

scientific article published on April 12, 2013

A novel Gcn5p inhibitor represses cell growth, gene transcription and histone acetylation in budding yeast

scientific article published on 01 September 2005

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

scientific article

A practical, green, and selective approach toward the synthesis of pharmacologically important quinone-containing heterocyclic systems using alumina-catalyzed Michael addition reaction

article

A regioselective approach toward the synthesis of pharmacologically important quinone-containing heterocyclic systems

scholarly article by Sabrina Castellano et al published December 2009 in Tetrahedron Letters

A transcriptional coregulator, SPIN·DOC, attenuates the coactivator activity of Spindlin1.

scientific article published on 23 October 2017

Antifungal activity of azole compounds CPA18 and CPA109 against azole-susceptible and -resistant strains of Candida albicans

scientific article published on 04 January 2013

Arginine Demethylation of G3BP1 Promotes Stress Granule Assembly

scientific article published on 6 September 2016

Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation

scientific article published in April 2002

CARM1 modulators affect epigenome of stem cells and change morphology of nucleoli.

scientific article published on 5 June 2015

CYP19 (aromatase): Exploring the scaffold flexibility for novel selective inhibitors

scientific article published in September 2008

Chemical biology of histone acetyltransferase natural compounds modulators

scientific article published on January 2011

Combined HAT/EZH2 modulation leads to cancer-selective cell death.

scientific article published on 22 May 2018

Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C

scientific article published on February 2004

Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.

scientific article

Design, synthesis and biological evaluation of carboxy analogues of arginine methyltransferase inhibitor 1 (AMI-1).

scientific article published in March 2010

Developing Spindlin1 small-molecule inhibitors by using protein microarrays

scientific article

Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells

scientific article published on 28 November 2018

Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series

scientific article published on May 1997

Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure

scientific article published on 26 February 2019

Dynamical aspects of TEM-1 beta-lactamase probed by molecular dynamics

scientific article published in May 2005

Ellagic Acid-Changed Epigenome of Ribosomal Genes and Condensed RPA194-Positive Regions of Nucleoli in Tumour Cells

scientific article published in January 2015

Enhancement of lysine acetylation accelerates wound repair

scientific article published on 02 July 2013

Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO).

scientific article

GE-05STUDY OF EPIGENETIC DEREGULATION OF A NOVEL DEUBIQUITYLASE IN MEDULLOBLASTOMA.

scientific article published on 21 April 2015

Highly efficient synthesis and chemical separation of 5-amino- and 7-amino-4-hydroxy-2-naphthoic acids

Histone deacetylase inhibitor activity in royal jelly might facilitate caste switching in bees.

scientific article

Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases

scientific article published on 30 December 2008

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

scientific article

Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.

scientific article published on 11 April 2008

Identification of small-molecule enhancers of arginine methylation catalyzed by coactivator-associated arginine methyltransferase 1.

scientific article

Identification of structural features of 2-alkylidene-1,3-dicarbonyl derivatives that induce inhibition and/or activation of histone acetyltransferases KAT3B/p300 and KAT2B/PCAF.

scientific article

Inhibition of Wnt/β-Catenin pathway and Histone acetyltransferase activity by Rimonabant: a therapeutic target for colon cancer.

scientific article published on 15 September 2017

Look for methods, not conclusions

scientific article published on 05 December 2019

Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors

scientific article published on 22 July 2011

Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).

scientific article published on 14 January 2011

N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480.

scientific article published on June 1998

New 6-nitroquinolones: synthesis and antimicrobial activities

scientific article published on June 2004

Nitroquinolones with broad-spectrum antimycobacterial activity in vitro

scientific article

Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity

scientific article published on 13 June 2011

Nε-lysine acetylation determines dissociation from GAP junctions and lateralization of connexin 43 in normal and dystrophic heart

scientific article

P300/CBP associated factor regulates nitroglycerin-dependent arterial relaxation by N(ε)-lysine acetylation of contractile proteins

scientific journal article

Progress in the Development of Lysine Methyltransferase SETD8 Inhibitors.

scientific article

Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells

scientific article published on 06 February 2014

Regulation of USP37 Expression by REST-Associated G9a-Dependent Histone Methylation.

scientific article published on 8 May 2017

Slow-, tight-binding HIV-1 reverse transcriptase non-nucleoside inhibitors highly active against drug-resistant mutants

scientific article published on 01 April 2007

Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations

scientific article published on 27 February 2007

Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties

scientific article published on November 2006

Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors

scientific article published on 17 March 2014

Structure-activity relationship studies on new DABOS: effect of substitutions at pyrimidine C-5 and C-6 positions on anti-HIV-1 activity

scientific article

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

Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.

scientific article published on August 1995

Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors

scientific article published on 7 October 2011

Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS.

scientific article published on February 2005

Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein

scientific article

Synthesis and biological evaluation of enantiomerically pure pyrrolyl-oxazolidinones as a new class of potent and selective monoamine oxidase type A inhibitors

scientific article

Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains

scientific article

Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors

scientific article published on July 2007

Synthesis and evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single nucleotide polymorphism rs6971.

scientific article

Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.

scientific article published on March 2004

Synthesis of 3-aryl/benzyl-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole derivatives: a comparison between conventional, microwave-assisted and flow-based methodologies

scientific article published on November 2010

The 23(rd) National Meeting of the Medicinal Chemistry Division of the Italian Chemical Society (DCF-SCI) in Salerno (NMMC 2015).

scientific article

The European Federation for Medicinal Chemistry (EFMC) Best Practice Initiative: Validating Chemical Probes

scientific article published on 03 September 2020

The Histone Acetylase Activator Pentadecylidenemalonate 1b Rescues Proliferation and Differentiation in the Human Cardiac Mesenchymal Cells of Type 2 Diabetic Patients

scientific article published on 23 January 2014

The emerging role of lysine methyltransferase SETD8 in human diseases ⬇️

scientific article

The identification of a novel natural activator of p300 histone acetyltranferase provides new insights into the modulation mechanism of this enzyme.

scientific article published on April 2010

Transition state mimics are valuable mechanistic probes for structural studies with the arginine methyltransferase CARM1.

scientific article published on 22 March 2017

Two novel SIRT1 activators, SCIC2 and SCIC2.1, enhance SIRT1-mediated effects in stress response and senescence

scientific article published on 16 January 2020

epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors.

scientific article

p300/CBP-associated factor selectively regulates the extinction of conditioned fear

scientific article

List of works by Gianluca Sbardella

3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A.

3-(1H-pyrrol-2-yl)-2-oxazolidinones as novel monoamine oxidase type A inhibitors

3-(4-aroyl-1H-pyrrol-2-yl)-N-hydroxy-2-propenamides, a new class of synthetic histone deacetylase inhibitors

5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives

5-Alkyl-2-alkylamino-6-(2,6-difluorophenylalkyl)-3,4-dihydropyrimidin-4(3H)-ones, a new series of potent, broad-spectrum non-nucleoside reverse transcriptase inhibitors belonging to the DABO family.

6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase

6-alkylthio-4-[1-(2,6-difluorophenyl)alkyl]-1H-[1,3,5]triazin-2-ones (ADATs): novel regulators of cell differentiation and proliferation

A TR‐FRET‐Based Functional Assay for Screening Activators of CARM1 ⬇️

A novel Gcn5p inhibitor represses cell growth, gene transcription and histone acetylation in budding yeast

A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach.

A practical, green, and selective approach toward the synthesis of pharmacologically important quinone-containing heterocyclic systems using alumina-catalyzed Michael addition reaction

A regioselective approach toward the synthesis of pharmacologically important quinone-containing heterocyclic systems

A transcriptional coregulator, SPIN·DOC, attenuates the coactivator activity of Spindlin1.

Antifungal activity of azole compounds CPA18 and CPA109 against azole-susceptible and -resistant strains of Candida albicans

Arginine Demethylation of G3BP1 Promotes Stress Granule Assembly

Binding mode analysis of 3-(4-benzoyl-1-methyl-1H-2-pyrrolyl)-N-hydroxy-2-propenamide: a new synthetic histone deacetylase inhibitor inducing histone hyperacetylation, growth inhibition, and terminal cell differentiation

CARM1 modulators affect epigenome of stem cells and change morphology of nucleoli.

CYP19 (aromatase): Exploring the scaffold flexibility for novel selective inhibitors

Chemical biology of histone acetyltransferase natural compounds modulators

Combined HAT/EZH2 modulation leads to cancer-selective cell death.

Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C

Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.

Design, synthesis and biological evaluation of carboxy analogues of arginine methyltransferase inhibitor 1 (AMI-1).

Developing Spindlin1 small-molecule inhibitors by using protein microarrays

Development of alkyl glycerone phosphate synthase inhibitors: Structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells

Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series

Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure

Dynamical aspects of TEM-1 beta-lactamase probed by molecular dynamics

Ellagic Acid-Changed Epigenome of Ribosomal Genes and Condensed RPA194-Positive Regions of Nucleoli in Tumour Cells

Enhancement of lysine acetylation accelerates wound repair

Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO).

GE-05STUDY OF EPIGENETIC DEREGULATION OF A NOVEL DEUBIQUITYLASE IN MEDULLOBLASTOMA.

Highly efficient synthesis and chemical separation of 5-amino- and 7-amino-4-hydroxy-2-naphthoic acids

Histone deacetylase inhibitor activity in royal jelly might facilitate caste switching in bees.

Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases

Identification of PR-SET7 and EZH2 selective inhibitors inducing cell death in human leukemia U937 cells

Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases.

Identification of small-molecule enhancers of arginine methylation catalyzed by coactivator-associated arginine methyltransferase 1.

Identification of structural features of 2-alkylidene-1,3-dicarbonyl derivatives that induce inhibition and/or activation of histone acetyltransferases KAT3B/p300 and KAT2B/PCAF.

Inhibition of Wnt/β-Catenin pathway and Histone acetyltransferase activity by Rimonabant: a therapeutic target for colon cancer.

Look for methods, not conclusions

Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors

Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).

N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480.

New 6-nitroquinolones: synthesis and antimicrobial activities

Nitroquinolones with broad-spectrum antimycobacterial activity in vitro

Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity

Nε-lysine acetylation determines dissociation from GAP junctions and lateralization of connexin 43 in normal and dystrophic heart

P300/CBP associated factor regulates nitroglycerin-dependent arterial relaxation by N(ε)-lysine acetylation of contractile proteins

Progress in the Development of Lysine Methyltransferase SETD8 Inhibitors.

Quinoline-Based p300 Histone Acetyltransferase Inhibitors with Pro-apoptotic Activity in Human Leukemia U937 Cells

Regulation of USP37 Expression by REST-Associated G9a-Dependent Histone Methylation.

Slow-, tight-binding HIV-1 reverse transcriptase non-nucleoside inhibitors highly active against drug-resistant mutants

Small molecule inhibitors of histone arginine methyltransferases: homology modeling, molecular docking, binding mode analysis, and biological evaluations

Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties

Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors

Structure-activity relationship studies on new DABOS: effect of substitutions at pyrimidine C-5 and C-6 positions on anti-HIV-1 activity

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

Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.

Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors

Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS.

Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein

Synthesis and biological evaluation of enantiomerically pure pyrrolyl-oxazolidinones as a new class of potent and selective monoamine oxidase type A inhibitors

Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains

Synthesis and biological validation of novel synthetic histone/protein methyltransferase inhibitors

Synthesis and evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single nucleotide polymorphism rs6971.

Synthesis and in vitro antimycobacterial activity of novel 3-(1H-pyrrol-1-yl)-2-oxazolidinone analogues of PNU-100480.

Synthesis of 3-aryl/benzyl-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole derivatives: a comparison between conventional, microwave-assisted and flow-based methodologies

The 23(rd) National Meeting of the Medicinal Chemistry Division of the Italian Chemical Society (DCF-SCI) in Salerno (NMMC 2015).

The European Federation for Medicinal Chemistry (EFMC) Best Practice Initiative: Validating Chemical Probes

The Histone Acetylase Activator Pentadecylidenemalonate 1b Rescues Proliferation and Differentiation in the Human Cardiac Mesenchymal Cells of Type 2 Diabetic Patients

The emerging role of lysine methyltransferase SETD8 in human diseases ⬇️

The identification of a novel natural activator of p300 histone acetyltranferase provides new insights into the modulation mechanism of this enzyme.

Transition state mimics are valuable mechanistic probes for structural studies with the arginine methyltransferase CARM1.

Two novel SIRT1 activators, SCIC2 and SCIC2.1, enhance SIRT1-mediated effects in stress response and senescence

epigenetic multiple ligands: mixed histone/protein methyltransferase, acetyltransferase, and class III deacetylase (sirtuin) inhibitors.

p300/CBP-associated factor selectively regulates the extinction of conditioned fear