M. Varasi

发表

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding.

Anna Vulpetti, Antonella Isacchi, Enrico Pesenti, 2004, Journal of medicinal chemistry.

Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.

A. Mai, S. Minucci, C. Mercurio, 2010, Journal of medicinal chemistry.

Synthesis and biological characterization of spiro[2H-(1,3)-benzoxazine-2,4'-piperidine] based histone deacetylase inhibitors.

S. Minucci, C. Mercurio, M. Varasi, 2013, European journal of medicinal chemistry.

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 2: Structure-Based Drug Design and Structure-Activity Relationship.

S. Minucci, C. Mercurio, L. Moretti, 2017, 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.

A new glycociamidine ring precursor: syntheses of (Z)-hymenialdisine, (Z)-2-debromohymenialdisine, and (+/-)-endo-2-debromohymenialdisine.

D. Borghi, M. Varasi, G. Papeo, 2005, Organic letters.

Chiral Resolution and Pharmacological Characterization of the Enantiomers of the Hsp90 Inhibitor 2‐Amino‐7‐[4‐fluoro‐2‐(3‐pyridyl)phenyl]‐4‐methyl‐7,8‐dihydro‐6H‐quinazolin‐5‐one Oxime

S. Minucci, C. Mercurio, R. Amici, 2014, ChemMedChem.

High-throughput screening identifies histone deacetylase inhibitors that modulate GTF2I expression in 7q11.23 microduplication autism spectrum disorder patient-derived cortical neurons

C. Mercurio, M. Varasi, M. Gabriele, 2020, Molecular Autism.

PHA-680632, a Novel Aurora Kinase Inhibitor with Potent Antitumoral Activity

D. Ballinari, V. Croci, P. Cappella, 2006, Clinical Cancer Research.

(E) and (Z)-3-Styrylpiperidines as sigma ligands

C. Caccia, M. Varasi, S. Mantegani, 1997 .

Synthesis and in vitro and in vivo evaluation of dopaminergic ergoline derivatives.

C. Caccia, G. Traquandi, M. Varasi, 1998, Farmaco.

Derivatives of kynurenine as inhibitors of rat brain kynurenine aminotransferase

R. Schwarcz, P. Pevarello, M. Varasi, 1996 .

28833, A Selective Kynurenine 3-Hydroxylase Inhibitor

R. Schwarcz, M. Varasi, C. Speciale, 1996 .

Kynurenic acid-enhancing and anti-ischemic effects of the potent kynurenine 3-hydroxylase inhibitor FCE 28833 in rodents.

R. Schwarcz, M. Varasi, C. Speciale, 1996, Advances in experimental medicine and biology.

New targets to modulate the DNA damage response.

C. Mercurio, M. Varasi, 2018, Future medicinal chemistry.

Kynurenergic manipulations influence excitatory synaptic function and excitotoxic vulnerability in the rat hippocampus in vivo

H. Scharfman, R. Schwarcz, M. Varasi, 2000, Neuroscience.

(R,S)-3,4-dichlorobenzoylalanine (FCE 28833A) causes a large and persistent increase in brain kynurenic acid levels in rats.

R. Schwarcz, M. Varasi, H. Wu, 1996, European journal of pharmacology.

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.

5(10→9)Abeo-ergoline derivatives: Synthesis, 5-HT1A-receptor affinity and selectivity

C. Caccia, M. Varasi, S. Mantegani, 1998 .

Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

S. Minucci, C. Mercurio, L. Moretti, 2016, European journal of medicinal chemistry.

Synthesis and Biological Characterization of Amidopropenyl Hydroxamates as HDAC Inhibitors

A. Mai, S. Minucci, C. Mercurio, 2010, ChemMedChem.

Inhibitors of Aβ Peptide Aggregation as Potential anti-Alzheimer Agents

T. Bandiera, M. Varasi, C. Post, 1997 .

Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin αVβ3

T. Bandiera, D. Volpi, A. Galvani, 2004 .

PNU-151774E protects against kainate-induced status epilepticus and hippocampal lesions in the rat.

R. Maj, P. Pevarello, M. Varasi, 1998, European journal of pharmacology.

Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors.

A. Mai, S. Minucci, C. Mercurio, 2011, Journal of medicinal chemistry.

GTF2I dosage regulates neuronal differentiation and social behavior in 7q11.23 neurodevelopmental disorders

T. Bonaldi, C. Mercurio, M. Varasi, 2022, bioRxiv.

Anticonvulsant Activity of PNU‐151774E 1 in the Amygdala Kindled Model of Complex Partial Seizures

R. Maj, P. Pevarello, M. Varasi, 1999, Epilepsia.

Laboratory Research Anticonvulsant Activity of PNU-15 1774E' in the Amygdala Kindled Model of Complex Partial Seizures

R. Maj, M. Varasi, R. Fariello, 1999 .

Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.

A. Mai, S. Minucci, C. Mercurio, 2015, ACS medicinal chemistry letters.

Biochemical and electrophysiological studies on the mechanism of action of PNU-151774E, a novel antiepileptic compound.

R. Maj, C. Caccia, P. Pevarello, 1999, Journal of Pharmacology and Experimental Therapeutics.

4-Phenyl-4-oxo-butanoic acid derivatives inhibitors of kynurenine 3-hydroxylase.

P. Pevarello, M. Varasi, C. Speciale, 1998, Bioorganic & medicinal chemistry letters.

Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models.

S. Minucci, C. Mercurio, C. So, 2020, ACS medicinal chemistry letters.

Tranylcypromine‐Based LSD1 Inhibitors: Structure‐Activity Relationships, Antiproliferative Effects in Leukemia, and Gene Target Modulation

A. Mai, S. Minucci, C. Mercurio, 2020, ChemMedChem.

Synthesis of new fenmetazole analogues with potential mixed α2-adrenergic antagonistic activity and noradrenaline-uptake inhibiting properties

P. Pevarello, M. Varasi, P. Dostert, 1991 .

Spiro[chromane‐2,4′‐piperidine]‐Based Histone Deacetylase Inhibitors with Improved in vivo Activity

S. Minucci, C. Mercurio, M. Varasi, 2012, ChemMedChem.

Research of potential antidepressant drugs with α2-adrenoreceptor antagonist and NA-uptake inhibiting properties: synthesis of 2-(1-hydroxy-2-phenoxy-2-phenyl)ethyl-4,5-dihydro-1H-imidazole derivatives

M. Varasi, P. Dostert, L. Merlini, 1990 .

A revised mechanism for the Mitsunobu reaction

M. Varasi, M. L. Maddox, K. A. Walker, 1987 .

Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships.

R. Bosotti, A. Isacchi, A. Montagnoli, 2008, Journal of medicinal chemistry.

3-Amino-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: a new class of CDK2 inhibitors.

J. Bischoff, C. Mercurio, A. Vulpetti, 2006, Bioorganic & medicinal chemistry letters.

First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.

A. Isacchi, A. Montagnoli, J. Berthelsen, 2009, Journal of medicinal chemistry.

Cdc7 kinase inhibitors: 5-heteroaryl-3-carboxamido-2-aryl pyrroles as potential antitumor agents. 1. Lead finding.

A. Isacchi, A. Montagnoli, R. D'Alessio, 2010, Journal of medicinal chemistry.

1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.

Paola Storici, Maurizio Rocchetti, Enrico Pesenti, 2006, Journal of medicinal chemistry.

Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.

A. Vulpetti, F. Roletto, P. Cappella, 2005, Journal of medicinal chemistry.

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

V. Croci, D. Volpi, F. Roletto, 2010, Bioorganic & 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.

3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 2. Lead optimization.

Anna Vulpetti, Enrico Pesenti, Ciro Mercurio, 2005, Journal of medicinal chemistry.

Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.

C. Caccia, M. Varasi, R. Mcarthur, 1997, Journal of medicinal chemistry.

Total synthesis of (±)-cyclooroidin

D. Borghi, M. Varasi, G. Papeo, 2005 .

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.

Nitrile oxide cycloaddition of non-activated alkynes: a novel approach to the synthesis of neuroactive isoxazoles

P. Pevarello, R. Amici, M. Varasi, 1993 .

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.

A. Mai, S. Minucci, M. Tortorici, 2014, European journal of medicinal chemistry.

PP2A Controls Genome Integrity by Integrating Nutrient-Sensing and Metabolic Pathways with the DNA Damage Response

S. Minucci, M. Varasi, M. Elgendy, 2017, Molecular cell.

D1 Agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: a structure–activity study

T. Bandiera, C. Caccia, G. Traquandi, 1999 .

Serotoninergic 5-HT3 and 5-HT4 receptor activities of dihydrobenzofuran carboxylic acid derivatives

C. Caccia, M. Varasi, R. Mcarthur, 1996 .

Ergoline derivatives: receptor affinity and selectivity.

M. Varasi, S. Mantegani, E. Brambilla, 1999, Farmaco.

Serotonergic ergoline derivatives.

C. Caccia, M. Varasi, S. Mantegani, 1998, Bioorganic & medicinal chemistry letters.

Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.

P. Pevarello, M. Varasi, P. Dostert, 1998, Journal of medicinal chemistry.

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration.

S. Minucci, C. Mercurio, L. Moretti, 2017, Journal of medicinal chemistry.

Preclinical evaluation of PNU-151774E as a novel anticonvulsant.

R. Maj, P. Pevarello, M. Varasi, 1998, The Journal of pharmacology and experimental therapeutics.

Nicotinoyl azide (NCA)-mediated Mitsunobu reaction: An expedient one-pot transformation of alcohols into azides

M. Varasi, P. Vianello, G. Papeo, 2004 .

Novel potent inhibitors of the histone demethylase KDM1A (LSD1), orally active in a murine promyelocitic leukemia model.

S. Minucci, C. Mercurio, M. Villa, 2017, Future medicinal chemistry.

Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.

A. Mai, S. Minucci, C. Mercurio, 2016, Journal of medicinal chemistry.

Cinnamic anilides as new mitochondrial permeability transition pore inhibitors endowed with ischemia-reperfusion injury protective effect in vivo.

S. Minucci, P. Pelicci, R. Amici, 2014, Journal of Medicinal Chemistry.

Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.

A. Isacchi, E. Casale, J. Bischoff, 2010, Bioorganic & medicinal chemistry.

Pure enantiomers of benzoylamino-tranylcypromine: LSD1 inhibition, gene modulation in human leukemia cells and effects on clonogenic potential of murine promyelocytic blasts.

A. Mai, S. Minucci, C. Mercurio, 2015, European journal of medicinal chemistry.

6‐Substituted Pyrrolo[3,4‐c]pyrazoles: An Improved Class of CDK2 Inhibitors

C. Mercurio, A. Vulpetti, D. Ballinari, 2007, ChemMedChem.

Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid–induced differentiation

G. Pavesi, R. Ravasio, A. Mai, 2020, Science Advances.

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

A. Mai, S. Minucci, C. Mercurio, 2015 .

Synthesis of dihydrolysergol analogues

G. Traquandi, M. Varasi, S. Mantegani, 2001 .

Discovery and Development of Safinamide, a New Drug for the Treatment of Parkinson's Disease

P. Pevarello, M. Varasi, 2018 .

Novel Pyridine‐Based Hydroxamates and 2′‐Aminoanilides as Histone Deacetylase Inhibitors: Biochemical Profile and Anticancer Activity

L. Altucci, A. Mai, A. Nebbioso, 2020, ChemMedChem.

LSD1-directed therapy affects glioblastoma tumorigenicity by deregulating the protective ATF4-dependent integrated stress response

S. Minucci, B. Costanza, B. Pollo, 2021, Science Translational Medicine.

Fragment‐based Identification of Hsp90 Inhibitors

Mark Whittaker, Thomas Hesterkamp, Dirk Winkler, 2009, ChemMedChem.

High-throughput NMR-based screening with competition binding experiments.

Stefan Knapp, Marina Veronesi, Claudio Dalvit, 2002, Journal of the American Chemical Society.

REDUCTIVE ALKYLATION OF a-AMINOAMIDES

P. Pevarello, R. Amici, M. Varasi, 1996 .

Quantitative Chemical Proteomics Identifies Novel Targets of the Anti-cancer Multi-kinase Inhibitor E-3810*

Tiziana Bonaldi, S. Minucci, T. Bonaldi, 2014, Molecular & Cellular Proteomics.

Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells.

L. Altucci, A. Mai, A. Nebbioso, 2022, European journal of medicinal chemistry.

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.

Anthracyclines and Amyloidosis

F. Tagliavini, T. Bandiera, M. Varasi, 1998 .

Effects of mlacemide on glutamate decarboxylase activity in rat striatum syraaptosomal fractions

R. Roncucci, M. Varasi, P. Dostert, 1990 .

alpha-substituted quisqualic acid analogs: new metabotropic glutamate receptor group II selective antagonists.

J. Wroblewski, M. Varasi, A. Kozikowski, 1998, Bioorganic & medicinal chemistry letters.

Further insights into the SAR of α-substituted cyclopropylamine derivatives as inhibitors of histone demethylase KDM1A.

C. Mercurio, M. Villa, M. Varasi, 2015, European journal of medicinal chemistry.

Benzoylalanine analogues as inhibitors of rat brain kynureninase and kynurenine 3-hydroxylase.

R. Schwarcz, M. Varasi, P. Guidetti, 1996, Advances in experimental medicine and biology.

Pyrrolo[3,2-c]quinoline derivatives: a new class of kynurenine-3-hydroxylase inhibitors.

P. Pevarello, M. Varasi, A. della Torre, 1999, Farmaco.

Effectiveness of anthracycline against experimental prion disease in Syrian hamsters.

G. Forloni, F. Tagliavini, T. Bandiera, 1997, Science.

Tuning mTORC1 activity dictates the response of acute myeloid leukemia to LSD1 inhibition

S. Minucci, M. Varasi, G. Meroni, 2019, Haematologica.

Discovery of a Novel Hsp90 Inhibitor by Fragment Linking

Mark Whittaker, Thomas Hesterkamp, Oliver Barker, 2010, ChemMedChem.

Sodium channel activity and sigma binding of 2-aminopropanamide anticonvulsants.

C. Caccia, P. Pevarello, R. Amici, 1999, Bioorganic & medicinal chemistry letters.

Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety.

R. Maj, C. Caccia, G. Traquandi, 1999, Bioorganic & medicinal chemistry letters.

Anticonvulsant activity of FCE 26743 in the kindling model of epilepsy

R. Maj, M. Varasi, R. Mcarthur, 1995 .

Synthesis and in vitro structure-activity relationship of 13-tert-butyl-ergoline derivatives as 5-HT1A receptor ligands

C. Caccia, M. Varasi, S. Mantegani, 1997 .

Modulation of the kynurine pathway of tryptophan metabolism in search for neuroprotective agents. Focus on kynurenine-3-hydroxylase.

P. Pevarello, M. Varasi, C. Speciale, 2003, Advances in experimental medicine and biology.

STRUCTURE OF CDK2-CYCLIN A WITH PHA-630529

J. Bischoff, C. Mercurio, A. Vulpetti, 2005 .

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.

Caloric restriction leads to druggable LSD1-dependent cancer stem cells expansion

S. Minucci, M. Varasi, M. Elgendy, 2024, Nature communications.