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Discovery and Development of Simeprevir (TMC435), a HCV NS3/4A Protease Inhibitor

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.1673-1693

2014

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Synthesis, X-ray Analysis, and Biological Evaluation of a New Class of Stereopure Lactam-Based HIV-1 Protease Inhibitors

Journal of medicinal chemistry, 2012-03, Vol.55 (6), p.2724-2736

2012

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In Vitro Activity and Preclinical Profile of TMC435350, a Potent Hepatitis C Virus Protease Inhibitor

Antimicrobial Agents and Chemotherapy, 2009-04, Vol.53 (4), p.1377-1385

2009

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Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts

Bone (New York, N.Y.), 2008-01, Vol.42 (1), p.200-211

2008

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Induced-Fit Binding of the Macrocyclic Noncovalent Inhibitor TMC435 to its HCV NS3/NS4A Protease Target

Angewandte Chemie (International ed.), 2010-02, Vol.49 (9), p.1652-1655

2010

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Structure–activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350

Bioorganic & medicinal chemistry, 2008-09, Vol.18 (17), p.4853-4858

2008

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Design and Synthesis of P1–P3 Macrocyclic Tertiary-Alcohol-Comprising HIV‑1 Protease Inhibitors

Journal of medicinal chemistry, 2013-11, Vol.56 (22), p.8999-9007

2013

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Relationships between Structure and Interaction Kinetics for HIV-1 Protease Inhibitors

Journal of medicinal chemistry, 2002-12, Vol.45 (25), p.5430-5439

2002

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Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-Length NS3 (Protease-Helicase/NTPase): A comparative study of different C-terminals

Bioorganic & medicinal chemistry, 2003-06, Vol.11 (12), p.2551-2568

2003

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Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application

Bioorganic & medicinal chemistry letters, 2013-01, Vol.23 (1), p.310-317

2013

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Microwave-Accelerated Synthesis of P1‘-Extended HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol in the Transition-State Mimicking Scaffold

Journal of medicinal chemistry, 2006-03, Vol.49 (5), p.1828-1832

2006

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Plasmepsins as potential targets for new antimalarial therapy

Medicinal research reviews, 2006-09, Vol.26 (5), p.626-666

2006

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Antiviral Activity and Mode of Action of TMC647078, a Novel Nucleoside Inhibitor of the Hepatitis C Virus NS5B Polymerase

Antimicrobial Agents and Chemotherapy, 2011-08, Vol.55 (8), p.3812-3820

2011

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Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II

Bioorganic & medicinal chemistry, 2005-09, Vol.13 (18), p.5371-5390

2005

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Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: Exploration of P2 quinazoline substituents

Bioorganic & medicinal chemistry letters, 2010-07, Vol.20 (14), p.4004-4011

2010

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Synthesis of Novel Thrombin Inhibitors. Use of Ring-Closing Metathesis Reactions for Synthesis of P2 Cyclopentene- and Cyclohexenedicarboxylic Acid Derivatives

Journal of medicinal chemistry, 2003-03, Vol.46 (7), p.1165-1179

2003

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Variations of the P2 group in HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold

Organic & biomolecular chemistry, 2006-01, Vol.4 (16), p.3040-3043

2006

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Erratum to ‘Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts’

Bone (New York, N.Y.), 2021-04, Vol.145, p.115354-115354, Article 115354

2021

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A novel assay for analysis of the regulation of the function of human osteoclasts

Journal of translational medicine, 2006-11, Vol.4 (1), p.45-45, Article 45

2006

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Nucleotide Prodrugs of 2′-Deoxy-2′-spirooxetane Ribonucleosides as Novel Inhibitors of the HCV NS5B Polymerase

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.1836-1844

2014

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Synthesis of Novel, Potent, Diol-Based HIV-1 Protease Inhibitors via Intermolecular Pinacol Homocoupling of (2S)-2-Benzyloxymethyl-4-phenylbutanal

Journal of medicinal chemistry, 2001-10, Vol.44 (21), p.3407-3416

2001

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Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes

Bioorganic & medicinal chemistry, 2012-07, Vol.20 (14), p.4377-4389

2012

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Impact of the Central Hydroxyl Groups on the Activity of Symmetrical HIV-1 Protease Inhibitors Derived From l-Mannaric Acid

Tetrahedron, 2000-05, Vol.56 (20), p.3219-3225

2000

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A One-Pot, Solid-Phase Synthesis of Secondary Amines from Reactive Alkyl Halides and an Alkyl Azide

Synlett, 2008-01, Vol.2008 (1), p.97-99

2008

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Design and Synthesis of Potent and Selective BACE-1 Inhibitors

Journal of medicinal chemistry, 2010-02, Vol.53 (4), p.1458-1464

2010

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Discovery and Development of Simeprevir (TMC435), a HCV NS3/4A Protease Inhibitor

Synthesis, X-ray Analysis, and Biological Evaluation of a New Class of Stereopure Lactam-Based HIV-1 Protease Inhibitors

In Vitro Activity and Preclinical Profile of TMC435350, a Potent Hepatitis C Virus Protease Inhibitor

Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts

Induced-Fit Binding of the Macrocyclic Noncovalent Inhibitor TMC435 to its HCV NS3/NS4A Protease Target

Structure–activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350

Design and Synthesis of P1–P3 Macrocyclic Tertiary-Alcohol-Comprising HIV‑1 Protease Inhibitors

Relationships between Structure and Interaction Kinetics for HIV-1 Protease Inhibitors

Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-Length NS3 (Protease-Helicase/NTPase): A comparative study of different C-terminals

Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application

Microwave-Accelerated Synthesis of P1‘-Extended HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol in the Transition-State Mimicking Scaffold

Plasmepsins as potential targets for new antimalarial therapy

Antiviral Activity and Mode of Action of TMC647078, a Novel Nucleoside Inhibitor of the Hepatitis C Virus NS5B Polymerase

Synthesis, biological evaluation, and modeling studies of inhibitors aimed at the malarial proteases plasmepsins I and II

Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: Exploration of P2 quinazoline substituents

Synthesis of Novel Thrombin Inhibitors. Use of Ring-Closing Metathesis Reactions for Synthesis of P2 Cyclopentene- and Cyclohexenedicarboxylic Acid Derivatives

Variations of the P2 group in HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold

Erratum to ‘Cathepsin K inhibitors prevent matrix-derived growth factor degradation by human osteoclasts’

A novel assay for analysis of the regulation of the function of human osteoclasts

Nucleotide Prodrugs of 2′-Deoxy-2′-spirooxetane Ribonucleosides as Novel Inhibitors of the HCV NS5B Polymerase

Synthesis of Novel, Potent, Diol-Based HIV-1 Protease Inhibitors via Intermolecular Pinacol Homocoupling of (2S)-2-Benzyloxymethyl-4-phenylbutanal

Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes

Impact of the Central Hydroxyl Groups on the Activity of Symmetrical HIV-1 Protease Inhibitors Derived From l-Mannaric Acid

A One-Pot, Solid-Phase Synthesis of Secondary Amines from Reactive Alkyl Halides and an Alkyl Azide

Design and Synthesis of Potent and Selective BACE-1 Inhibitors

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