V. Summa

发表

HCV NS5b RNA-Dependent RNA Polymerase Inhibitors: From α,γ-Diketoacids to 4,5-Dihydroxypyrimidine- or 3-Methyl-5- hydroxypyrimidinonecarboxylic Acids. Design and Synthesis

R. Francesco, S. Altamura, V. Summa, 2004 .

Discovery of α,γ-Diketo Acids as Potent Selective and Reversible Inhibitors of Hepatitis C Virus NS5b RNA-Dependent RNA Polymerase

Uwe Koch, Victor Giulio Matassa, U. Koch, 2004 .

4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.

M. Rowley, V. Summa, A. Petrocchi, 2006, Journal of medicinal chemistry.

Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.

D. Hazuda, S. Harper, M. Rowley, 2007, Journal of medicinal chemistry.

Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.

D. Hazuda, M. Rowley, V. Summa, 2008, Journal of medicinal chemistry.

Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.

Michael Rowley, Michael D. Miller, M. Rowley, 2006, Bioorganic & medicinal chemistry letters.

Application of an in Vitro Blood-Brain Barrier Model in the Selection of Experimental Drug Candidates for the Treatment of Huntington's Disease.

C. Dominguez, Laura Orsatti, V. Summa, 2019, Molecular pharmaceutics.

MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants

Adam T. Gates, D. Hazuda, M. Rudd, 2012, Antimicrobial Agents and Chemotherapy.

Quantitative Prediction of Human Clearance Guiding the Development of Raltegravir (MK-0518, Isentress) and Related HIV Integrase Inhibitors

M. Rowley, V. Summa, R. Laufer, 2009, Drug Metabolism and Disposition.

Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: structure-based design and synthesis of new templates.

U. Koch, M. Rowley, V. Summa, 2010, Bioorganic & medicinal chemistry.

The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase.

R. De Francesco, S. Altamura, V. Summa, 2004, Bioorganic & medicinal chemistry letters.

VX-950 (Vertex/Mitsubishi).

V. Summa, 2005, Current opinion in investigational drugs.

Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology

M. Brindisi, V. Summa, A. Alfano, 2022, Journal of medicinal chemistry.

Structure-Based Identification of HIV-1 Nucleocapsid Protein Inhibitors Active against Wild-Type and Drug-Resistant HIV-1 Strains.

F. Lori, E. Réal, S. Harper, 2017, ACS chemical biology.

Natural Compounds Inhibit SARS-CoV-2 nsp13 Unwinding and ATPase Enzyme Activities

Daniela Iaconis, V. Summa, M. Nowotny, 2022, ACS pharmacology & translational science.

Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy.

U. Koch, V. Summa, P. Pace, 2010, Bioorganic & medicinal chemistry letters.

The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease

X. Chu, R. Evers, S. Harper, 2010, Xenobiotica; the fate of foreign compounds in biological systems.

Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.

M. Rudd, P. Coleman, S. Harper, 2012, ACS medicinal chemistry letters.

5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.

E. Réal, S. Harper, M. Botta, 2020, ACS medicinal chemistry letters.

Identification of inhibitors of SARS-CoV-2 3CL-Pro enzymatic activity using a small molecule in-vitro repurposing screen

F. Musiani, Daniela Iaconis, V. Summa, 2020, bioRxiv.

Visible-Light Photocatalytic Functionalization of Isocyanides for the Synthesis of Secondary Amides and Ketene Aminals

E. Novellino, V. Summa, Jussara Amato, 2020, The Journal of organic chemistry.

Synthesis and Biological Evaluation of RGD–Cryptophycin Conjugates for Targeted Drug Delivery

V. Summa, Giulio Auciello, P. Gallinari, 2019, Pharmaceutics.

Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.

P. Mäser, V. Summa, R. Di Santo, 2019, Journal of medicinal chemistry.

Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.

S. Harper, S. Altamura, N. Gennari, 2016, ACS medicinal chemistry letters.

Identification and in vitro Characterization of a New Series of Potent and Highly Selective G9a Inhibitors as Novel Anti-Fibroadipogenic Agents.

V. Summa, G. Peruzzi, E. Monteagudo, 2022, Bioorganic & medicinal chemistry letters.

Largazole Analogues as Histone Deacetylase Inhibitors and Anticancer Agents: An Overview of Structure–Activity Relationships

M. Botta, V. Summa, R. Di Fabio, 2017, ChemMedChem.

Discovery of 4-((1-(1H-imidazol-2-yl)alkoxy)methyl)pyridines as a new class of Trypanosoma cruzi growth inhibitors.

S. Harper, V. Summa, P. Pace, 2020, Bioorganic & medicinal chemistry letters.

Discovery and Development of HIV Integrase Inhibitor Raltegravir

V. Summa, P. Pace, 2011 .

Easy access to α-ketoamides as SARS-CoV-2 and MERS Mpro inhibitors via the PADAM oxidation route

M. Brindisi, V. Summa, P. Storici, 2022, European Journal of Medicinal Chemistry.

Cytopathic SARS-CoV-2 screening on VERO-E6 cells in a large-scale repurposing effort

C. Collard, Daniela Iaconis, V. Summa, 2022, Scientific data.

Synthesis and antiviral properties of novel 7-heterocyclic substituted 7-deaza-adenine nucleoside inhibitors of Hepatitis C NS5B polymerase.

M. Rowley, V. Summa, S. Avolio, 2012, Bioorganic & medicinal chemistry.

Discovery and Antiviral Profile of New Sulfamoylbenzamide Derivatives as HBV Capsid Assembly Modulators.

A. Prandi, R. De Francesco, V. Summa, 2022, Bioorganic & Medicinal Chemistry Letters.

Synthesis and Antiviral Properties of Novel Tetracyclic Nucleoside Inhibitors of Hepatitis C NS5B Polymerase

U. Koch, M. Rowley, V. Summa, 2012, Nucleosides, nucleotides & nucleic acids.

Discovery of alpha,gamma-diketo acids as potent selective and reversible inhibitors of hepatitis C virus NS5b RNA-dependent RNA polymerase.

U. Koch, R. De Francesco, L. Tomei, 2004, Journal of medicinal chemistry.

HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.

R. De Francesco, S. Altamura, V. Summa, 2004, Journal of medicinal chemistry.

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.

Mark Embrey, Samson M Jolly, Wei Xu, 2004, Proceedings of the National Academy of Sciences of the United States of America.

Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease.

Qian Huang, Adam T. Gates, M. Rudd, 2012, Bioorganic & medicinal chemistry letters.

P2‐Quinazolinones and Bis‐Macrocycles as New Templates for Next‐Generation Hepatitis C Virus NS3/4a Protease Inhibitors: Discovery of MK‐2748 and MK‐6325

Qian Huang, Adam T. Gates, M. Rudd, 2015, ChemMedChem.

A Focus on Severe Acute Respiratory Syndrome ( SARS ) Coronavirus ( SARS‐CoVs ) 1 and 2

V. Summa, E. Tramontano, R. Cannalire, 2021, New Drug Development for Known and Emerging Viruses.

Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities

V. Summa, F. S. Di Leva, A. Beccari, 2020, Journal of medicinal chemistry.

A Useful Methodology for the Regioselective Deprotection of 1,3-Dibenzyluracils

M. Botta, R. Saladino, V. Summa, 1991 .

4-Hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors.

V. Summa, P. Pace, S. Spieser, 2008, Bioorganic & medicinal chemistry letters.

Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.

M. Rowley, V. Summa, R. Laufer, 2006, Bioorganic & medicinal chemistry letters.

Synthesis of aryl 2-benzofuranyl and aryl 2-indolyl carbinols of high enantiomeric purity via palladium-catalyzed heteroannulation of chiral arylpropargylic alcohols

M. Botta, V. Summa, F. Corelli, 1996 .

Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement.

U. Koch, M. Rowley, V. Summa, 2009, Journal of medicinal chemistry.

3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors.

V. Summa, M. Donghi, O. Kinzel, 2009, Bioorganic & medicinal chemistry letters.

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.

Michael Rowley, Cristina Gardelli, Marco Ferrara, 2007, Journal of medicinal chemistry.

Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.

E. H. Rydberg, U. Koch, R. De Francesco, 2009, Journal of medicinal chemistry.

Inhibitors of hepatitis C virus NS3/4A: alpha-ketoamide based macrocyclic inhibitors.

J. I. Hernando, V. Summa, S. Avolio, 2009, Bioorganic & medicinal chemistry letters.

Synthesis of amides: An efficient and chemoselective method for the preparation of β-lactam derivatives related to HLE inhibitors

V. Summa, R. Fabio, T. Rossi, 1993 .

A Useful Methodology for the Regioselective Deprotection of 1,3- Dibenzyluracils.

M. Botta, R. Saladino, V. Summa, 1992 .

Approaching a new era for hepatitis C virus therapy: inhibitors of the NS3-4A serine protease and the NS5B RNA-dependent RNA polymerase.

Giovanni Migliaccio, R. De Francesco, L. Tomei, 2003, Antiviral research.

Routes to HIV-integrase inhibitors: efficient synthesis of bicyclic pyrimidones by ring expansion or amination at a benzylic position

V. Summa, P. Pace, G. Cecere, 2009 .

A novel method using nuclear magnetic resonance for plasma protein binding assessment in drug discovery programs

V. Summa, M. Orsale, E. Monteagudo, 2019, Journal of pharmaceutical and biomedical analysis.

Aryl propargylic alcohols of high enantiomeric purity via lipase catalyzed resolutions

M. Botta, V. Summa, M. Schneider, 1996 .

Researches on antiviral agents. 4. Studies on the chemistry of 6-methyl-2-methoxy-4-O-acyloxy and 6-methyl-2,4-di-O-acyloxypyrimidine derivatives as new acylation reagents and inhibitors of uracil DNA glycosylases.

M. Botta, R. Saladino, V. Summa, 1994 .

Stereospecific synthesis of 1-alkylimidazole derivatives via mitsunobu reactions

M. Botta, V. Summa, F. Corelli, 1994 .

Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein.

M. Botta, M. Zazzi, Y. Mély, 2018, ACS medicinal chemistry letters.

Researches on Antiviral Agents. Part 4. Studies on the Chemistry of 6‐ Methyl‐2‐methoxy‐4‐O‐acyloxy and 6‐Methyl‐2,4‐di‐O‐acyloxypyrimidine Derivatives as New Acylation Reagents and Inhibitors of Uracil DNA Glycosylases.

M. Botta, R. Saladino, V. Summa, 1994 .

Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.

S. Harper, V. Summa, P. Pace, 2018, ACS medicinal chemistry letters.

Evaluation of HIV-1 integrase inhibitors on human primary macrophages using a luciferase-based single-cycle phenotypic assay.

Y. Pommier, V. Summa, R. Di Santo, 2010, Journal of Virological Methods.

Phosphorous acid analogs of novel P2-P4 macrocycles as inhibitors of HCV-NS3 protease.

N. Liverton, U. Koch, V. Summa, 2009, Bioorganic & medicinal chemistry letters.

SARS-CoV-2 Entry Inhibitors: Small Molecules and Peptides Targeting Virus or Host Cells

V. Summa, A. Beccari, Sveva Pelliccia, 2020, International journal of molecular sciences.

Structural characterization of the Hepatitis C Virus NS3 protease from genotype 3a: the basis of the genotype 1b vs. 3a inhibitor potency shift.

R. Bazzo, U. Koch, M. Bottomley, 2010, Virology.

Binding of a noncovalent inhibitor exploiting the S' region stabilizes the hepatitis C virus NS3 protease conformation in the absence of cofactor.

R. Bazzo, U. Koch, M. Bottomley, 2009, Journal of molecular biology.

Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.

S. Harper, N. Liverton, U. Koch, 2009, Journal of medicinal chemistry.

Hepatitis C Virus NS5A Is a Direct Substrate of Casein Kinase I-α, a Cellular Kinase Identified by Inhibitor Affinity Chromatography Using Specific NS5A Hyperphosphorylation Inhibitors*

R. De Francesco, Laura Orsatti, V. Summa, 2007, Journal of Biological Chemistry.

Identification of Inhibitors of SARS-CoV-2 3CL-Pro Enzymatic Activity Using a Small Molecule in Vitro Repurposing Screen

F. Musiani, Daniela Iaconis, V. Summa, 2021, ACS pharmacology & translational science.

6-Bromoindirubin-3′-oxime intercepts GSK3 signaling to promote and enhance skeletal muscle differentiation affecting miR-206 expression in mice

S. Altamura, V. Summa, G. Minchiotti, 2019, Scientific Reports.

HIV Integrase Inhibitors: From Diketo Acids to Heterocyclic Templates: History of HIV Integrase Medicinal Chemistry at Merck West Point and Merck Rome (IRBM) Leading to Discovery of Raltegravir

V. Summa, M. Egbertson, N. Anthony, 2011 .

From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety.

U. Koch, V. Summa, A. Petrocchi, 2007, Bioorganic & medicinal chemistry letters.

Broad-spectrum coronavirus 3C-like protease peptidomimetic inhibitors effectively block SARS-CoV-2 replication in cells: Design, synthesis, biological evaluation, and X-ray structure determination

M. Brindisi, V. Summa, P. Storici, 2023, European Journal of Medicinal Chemistry.

Synthesis of Aryl 2-Benzofuranyl and Aryl 2-Indolyl Carbinols of High Enantiomeric Purity via Palladium-Catalyzed Heteroannulation of Chiral Arylpropargylic Alcohols.

M. Botta, V. Summa, F. Corelli, 1996 .

MK-5172, a Selective Inhibitor of Hepatitis C Virus NS3/4a Protease with Broad Activity across Genotypes and Resistant Variants

Qian Huang, Adam T. Gates, D. Hazuda, 2014, Antimicrobial Agents and Chemotherapy.

Discovery of 2-(1H-imidazo-2-yl)piperazines as a new class of potent and non-cytotoxic inhibitors of Trypanosoma brucei growth in vitro.

S. Harper, N. Gennari, V. Summa, 2018, Bioorganic & medicinal chemistry letters.

Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center.

V. Summa, E. Muraglia, M. Orsale, 2009, Bioorganic & Medicinal Chemistry Letters.

Development of 2-t butyl-N-methyl pyrimidones as potent inhibitors of HIV integrase.

M. Rowley, V. Summa, P. Pace, 2008, Bioorganic & Medicinal Chemistry Letters.

Optimization of 2-(1H-imidazo-2-yl)piperazines series of Trypanosoma brucei growth inhibitors as potential treatment for the second stage of HAT.

S. Harper, N. Gennari, V. Summa, 2020, Bioorganic & medicinal chemistry letters.

Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.

S. Steinbacher, M. Augustin, S. Harper, 2020, ACS medicinal chemistry letters.

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Fabrizio Fiore, Michael Rowley, Cristina Gardelli, 2008, Journal of medicinal chemistry.

Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction.

S. Steinbacher, M. Augustin, C. Dominguez, 2020, Bioorganic & medicinal chemistry.

Advances in the development of macrocyclic inhibitors of hepatitis C virus NS3-4A protease.

V. Summa, Salvatore Avolio, 2010, Current Topics in Medicinal Chemistry.

Synthesis and Antiproliferative Activity of Nitric Oxide-Donor Largazole Prodrugs.

C. Zamperini, M. Botta, V. Summa, 2020, ACS medicinal chemistry letters.

N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.

M. Rowley, V. Summa, A. Petrocchi, 2009, Bioorganic & medicinal chemistry letters.

Rejuvenating the [1, 2, 3]-triazolo [1,5-a]quinoxalin-4(5H)-one scaffold: Synthesis and derivatization in a sustainable guise and preliminary antimicrobial evaluation

M. Brindisi, V. Summa, E. Buommino, 2023, Frontiers in Chemistry.

Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.

S. Harper, S. Altamura, N. Gennari, 2016, ACS medicinal chemistry letters.