List of works - Dante Rotili

"Shock and kill" effects of class I-selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV-1 quiescence

scientific article

2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies

scientific article

5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile

scientific article published on 17 July 2008

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 new water soluble MAPK activator exerts antitumor activity in melanoma cells resistant to the BRAF inhibitor vemurafenib

scientific article

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

scientific article published on 01 September 2005

A photoreactive small-molecule probe for 2-oxoglutarate oxygenases

scientific article

An Analog of BIX-01294 Selectively Inhibits a Family of Histone H3 Lysine 9 Jumonji Demethylases

scientific article

Analytical and semipreparative high performance liquid chromatography separation of stereoisomers of novel 3,4-dihydropyrimidin-4(3H)-one derivatives on the immobilised amylose-based Chiralpak IA chiral stationary phase

scientific article published on 01 July 2006

At Long Last Potent and Selective KDM5 Inhibitors

scholarly article by Dante Rotili published in July 2016

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

scientific article published on 7 September 2012

Biological effects of MC2050, a quinazoline-based PARP-1 inhibitor, in human neuroblastoma and EBV-positive Burkitt's lymphoma cells

scientific article published on 01 March 2011

Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies

scientific article published on November 2012

Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues

scientific article published in February 2010

Chiral HPLC separation and absolute configuration of novel S-DABO derivatives

scientific article

Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides

scientific article published in May 2005

Class II-selective histone deacetylase inhibitors. Part 2: Alignment-independent GRIND 3-D QSAR, homology and docking studies

scientific article published on 27 May 2007

Context-selective death of acute myeloid leukemia cells triggered by the novel hybrid retinoid-HDAC inhibitor MC2392.

scientific article published on 24 February 2014

Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level

scientific article published on 25 March 2011

Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells

scientific article published on 12 December 2012

Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans

scientific article

Emerging Therapeutic Potential of SIRT6 Modulators

scientific article published in 2021

Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer

scientific article published on 12 November 2019

Enzyme kinetics and inhibition of histone acetyltransferase KAT8.

scientific article published on 22 October 2015

Erratum: Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

scholarly article published in Oncogene

Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies.

scientific article

Evaluation of histone deacetylases as drug targets in Huntington's disease models. Study of HDACs in brain tissues from R6/2 and CAG140 knock-in HD mouse models and human patients and in a neuronal HD cell model

scientific article

Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates

scientific article

Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes

scientific article

HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation

scientific article published on 16 July 2010

Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells

scientific article published on 08 February 2016

Histone deacetylase inhibition modulates deoxyribonucleotide pools and enhances the antitumor effects of the ribonucleotide reductase inhibitor 3'-C-methyladenosine in leukaemia cells.

scientific article published on 11 February 2011

Histone deacetylase inhibitors and hemoglobin F induction in beta-thalassemia

scientific article published on 29 May 2008

Histone deacetylase inhibitors and neurodegenerative disorders: holding the promise

scientific article published on January 2009

Histone deacetylase inhibitors may reduce pathogenicity and virulence in Candida albicans

scientific article

Histone deacetylation in epigenetics: an attractive target for anticancer therapy

scientific article

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

scientific article published on 30 December 2008

Identification of Inhibitors to Trypanosoma cruzi Sirtuins Based on Compounds Developed to Human Enzymes ⬇️

scientific article published on 22 May 2020

Identification of Two New Synthetic Histone Deacetylase Inhibitors That Modulate Globin Gene Expression in Erythroid Cells from Healthy Donors and Patients with Thalassemia

article

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

scientific article published on 11 April 2008

Identification of tri- and tetracyclic pyrimidinediones as sirtuin inhibitors

scientific article published on May 2010

Inhibition of Histone Demethylases LSD1 and UTX Regulates ERα Signaling in Breast Cancer

scientific article published on 16 December 2019

Inhibition of class I histone deacetylases unveils a mitochondrial signature and enhances oxidative metabolism in skeletal muscle and adipose tissue

scientific article published on 15 October 2012

IκB kinase ε targets interferon regulatory factor 1 in activated T lymphocytes.

scientific article published on 06 January 2014

Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly disruption of protein-protein interactions

scholarly article

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

scientific article published on 22 July 2011

Nitric oxide determines mesodermic differentiation of mouse embryonic stem cells by activating class IIa histone deacetylases: potential therapeutic implications in a mouse model of hindlimb ischemia

scientific article

Nitric oxide modulates chromatin folding in human endothelial cells via protein phosphatase 2A activation and class II histone deacetylases nuclear shuttling

scientific article published on 01 November 2007

Non-cancer uses of histone deacetylase inhibitors: effects on infectious diseases and beta-hemoglobinopathies

scientific article published on January 2009

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

scientific article published on 30 April 2015

Novel pyrrole-containing histone deacetylase inhibitors endowed with cytodifferentiation activity

scientific article published on 4 April 2007

Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities

scientific article published on 22 March 2008

PARP-1 modulates amyloid beta peptide-induced neuronal damage

scientific article

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

scientific article

Photoactivable peptides for identifying enzyme–substrate and protein–protein interactions

scientific article published on 13 December 2010

Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity

scientific article

Proteomic profile of differentially expressed plasma proteins from dystrophic mice and following suberoylanilide hydroxamic acid treatment.

scientific article published on 11 November 2009

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

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

scientific article published on 06 February 2014

SIRT5 regulation of ammonia-induced autophagy and mitophagy

scientific article published in January 2015

Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect.

scientific article

Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes ⬇️

scientific article

Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile

scientific article published on 19 January 2011

Sirtuin functions and modulation: from chemistry to the clinic

scientific article

Sirtuin modulators control reactive gliosis in an in vitro model of Alzheimer's disease

scientific article published on 13 May 2014

Sirtuin modulators: where are we now? A review of patents from 2015 to 2019

scientific article published on 13 April 2020

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 acetyltransferase activity: identification and biological properties

scientific article published on November 2006

Substrate-induced stable enzyme-inhibitor complex formation allows tight binding of novel 2-aminopyrimidin-4(3H)-ones to drug-resistant HIV-1 reverse transcriptase mutants

scientific article published in September 2008

Synthesis and Biological Properties of Novel, Uracil-Containing Histone Deacetylase Inhibitors

scientific article published on 01 October 2006

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

scientific article

Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis

scientific article published on 01 December 2019

Synthesis and structure--activity relationship of new cytotoxic agents targeting human glutathione-S-transferases

scientific article

Targeting Histone Demethylases: A New Avenue for the Fight against Cancer ⬇️

scientific article published on June 1, 2011

Targeting Lysine Deacetylases (KDACs) in Parasites

scientific article

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.

scientific article

The histone deacetylase inhibitor suberoylanilide hydroxamic acid reduces cardiac arrhythmias in dystrophic mice

scientific article published on 17 February 2010

c-Jun N-terminal kinase activation by nitrobenzoxadiazoles leads to late-stage autophagy inhibition

scientific article published on 4 February 2016

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

scientific article

List of works by Dante Rotili

"Shock and kill" effects of class I-selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV-1 quiescence

2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies

5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile

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 new water soluble MAPK activator exerts antitumor activity in melanoma cells resistant to the BRAF inhibitor vemurafenib

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

A photoreactive small-molecule probe for 2-oxoglutarate oxygenases

An Analog of BIX-01294 Selectively Inhibits a Family of Histone H3 Lysine 9 Jumonji Demethylases

Analytical and semipreparative high performance liquid chromatography separation of stereoisomers of novel 3,4-dihydropyrimidin-4(3H)-one derivatives on the immobilised amylose-based Chiralpak IA chiral stationary phase

At Long Last Potent and Selective KDM5 Inhibitors

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

Biological effects of MC2050, a quinazoline-based PARP-1 inhibitor, in human neuroblastoma and EBV-positive Burkitt's lymphoma cells

Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies

Characterization of sirtuin inhibitors in nematodes expressing a muscular dystrophy protein reveals muscle cell and behavioral protection by specific sirtinol analogues

Chiral HPLC separation and absolute configuration of novel S-DABO derivatives

Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides

Class II-selective histone deacetylase inhibitors. Part 2: Alignment-independent GRIND 3-D QSAR, homology and docking studies

Context-selective death of acute myeloid leukemia cells triggered by the novel hybrid retinoid-HDAC inhibitor MC2392.

Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level

Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells

Discovery of uracil-based histone deacetylase inhibitors able to reduce acquired antifungal resistance and trailing growth in Candida albicans

Emerging Therapeutic Potential of SIRT6 Modulators

Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer

Enzyme kinetics and inhibition of histone acetyltransferase KAT8.

Erratum: Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies.

Evaluation of histone deacetylases as drug targets in Huntington's disease models. Study of HDACs in brain tissues from R6/2 and CAG140 knock-in HD mouse models and human patients and in a neuronal HD cell model

Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates

Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes

HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation

Histone acetyltransferase inhibitor CPTH6 preferentially targets lung cancer stem-like cells

Histone deacetylase inhibition modulates deoxyribonucleotide pools and enhances the antitumor effects of the ribonucleotide reductase inhibitor 3'-C-methyladenosine in leukaemia cells.

Histone deacetylase inhibitors and hemoglobin F induction in beta-thalassemia

Histone deacetylase inhibitors and neurodegenerative disorders: holding the promise

Histone deacetylase inhibitors may reduce pathogenicity and virulence in Candida albicans

Histone deacetylation in epigenetics: an attractive target for anticancer therapy

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

Identification of Inhibitors to Trypanosoma cruzi Sirtuins Based on Compounds Developed to Human Enzymes ⬇️

Identification of Two New Synthetic Histone Deacetylase Inhibitors That Modulate Globin Gene Expression in Erythroid Cells from Healthy Donors and Patients with Thalassemia

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

Identification of tri- and tetracyclic pyrimidinediones as sirtuin inhibitors

Inhibition of Histone Demethylases LSD1 and UTX Regulates ERα Signaling in Breast Cancer

Inhibition of class I histone deacetylases unveils a mitochondrial signature and enhances oxidative metabolism in skeletal muscle and adipose tissue

IκB kinase ε targets interferon regulatory factor 1 in activated T lymphocytes.

Mass spectrometry enables the discovery of inhibitors of an LPS transport assembly disruption of protein-protein interactions

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

Nitric oxide determines mesodermic differentiation of mouse embryonic stem cells by activating class IIa histone deacetylases: potential therapeutic implications in a mouse model of hindlimb ischemia

Nitric oxide modulates chromatin folding in human endothelial cells via protein phosphatase 2A activation and class II histone deacetylases nuclear shuttling

Non-cancer uses of histone deacetylase inhibitors: effects on infectious diseases and beta-hemoglobinopathies

Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells

Novel pyrrole-containing histone deacetylase inhibitors endowed with cytodifferentiation activity

Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities

PARP-1 modulates amyloid beta peptide-induced neuronal damage

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Photoactivable peptides for identifying enzyme–substrate and protein–protein interactions

Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity

Proteomic profile of differentially expressed plasma proteins from dystrophic mice and following suberoylanilide hydroxamic acid treatment.

Pyrrole- and indole-containing tranylcypromine derivatives as novel lysine-specific demethylase 1 inhibitors active on cancer cells

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

SIRT5 regulation of ammonia-induced autophagy and mitophagy

Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect.

Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes ⬇️

Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile

Sirtuin functions and modulation: from chemistry to the clinic

Sirtuin modulators control reactive gliosis in an in vitro model of Alzheimer's disease

Sirtuin modulators: where are we now? A review of patents from 2015 to 2019

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

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

Substrate-induced stable enzyme-inhibitor complex formation allows tight binding of novel 2-aminopyrimidin-4(3H)-ones to drug-resistant HIV-1 reverse transcriptase mutants

Synthesis and Biological Properties of Novel, Uracil-Containing Histone Deacetylase Inhibitors

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

Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis

Synthesis and structure--activity relationship of new cytotoxic agents targeting human glutathione-S-transferases

Targeting Histone Demethylases: A New Avenue for the Fight against Cancer ⬇️

Targeting Lysine Deacetylases (KDACs) in Parasites

The histone acetyltransferase p300 inhibitor C646 reduces pro-inflammatory gene expression and inhibits histone deacetylases.

The histone deacetylase inhibitor suberoylanilide hydroxamic acid reduces cardiac arrhythmias in dystrophic mice

c-Jun N-terminal kinase activation by nitrobenzoxadiazoles leads to late-stage autophagy inhibition