Sulfur(vi) fluoride exchange as a key reaction for synthesizing biaryl sulfate core derivatives as potent hepatitis C virus NS5A inhibitors and their structure–activity relationship studies

Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity

(2018) Baomin Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Highlights of the Structure–Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530)

(2018) Rolf Wagner et al.   JOURNAL OF MEDICINAL CHEMISTRY

New potent biaryl sulfate-based hepatitis C virus inhibitors

(2017) Youngsu You et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Nucleophilic Deoxyfluorination of Phenols via Aryl Fluorosulfonate Intermediates

(2017) Sydonie D. Schimler et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Bifluoride-catalysed sulfur(VI) fluoride exchange reaction for the synthesis of polysulfates and polysulfonates

(2017) Bing Gao et al.   Nature Chemistry

SuFEx: a metal-free click ligation for multivalent biomolecules

(2017) Alessandro Dondoni et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

SuFEx Click: New Materials from SO x F and Silyl Ethers

(2016) Jeremy Yatvin et al.   CHEMISTRY-A EUROPEAN JOURNAL

A Click Ligation Based on SuFEx for the Metal-Free Synthesis of Sugar and Iminosugar Clusters

(2016) Renaud Zelli et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Effectiveness of Ledipasvir-Sofosbuvir Combination in Patients With Hepatitis C Virus Infection and Factors Associated With Sustained Virologic Response

(2016) Norah A. Terrault et al.   GASTROENTEROLOGY

Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms

(2016) Ling Tong et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Potent, Selective, and Orally Bioavailable HCV NS5A Inhibitor for Treatment of Hepatitis C Virus: (S)-1-((R)-2-(Cyclopropanecarboxamido)-2-phenylacetyl)-N-(4-phenylthiazol-2-yl)pyrrolidine-2-carboxamide

(2016) Iou-Jiun Kang et al.   JOURNAL OF MEDICINAL CHEMISTRY

2015 Philip S. Portoghese Medicinal Chemistry Lectureship. Curing Hepatitis C Virus Infection with Direct-Acting Antiviral Agents: The Arc of a Medicinal Chemistry Triumph

(2016) Nicholas A. Meanwell   JOURNAL OF MEDICINAL CHEMISTRY

Recent Advances in Antiviral Therapy for Chronic Hepatitis C

(2016) Akihiro Tamori et al.   MEDIATORS OF INFLAMMATION

An atom-efficient and convergent approach to the preparation of NS5A inhibitors by C–H activation

(2016) Thomas O. Moore et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Direct introduction of R-SO2F moieties into proteins and protein-polymer conjugation using SuFEx chemistry

(2016) Shaohua Li et al.   POLYMER

New direct-acting antivirals in hepatitis C therapy: a review of sofosbuvir, ledipasvir, daclatasvir, simeprevir, paritaprevir, ombitasvir and dasabuvir

(2016) Sean M. McConachie et al.   Expert Review of Clinical Pharmacology

SuFEx on the Surface: A Flexible Platform for Postpolymerization Modification of Polymer Brushes

(2015) Jeremy Yatvin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-Symmetric inhibitors with diyne and biphenyl linkers

(2015) Simon Giroux et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: Non-symmetric inhibitors with potent activity against genotype 1a and 1b

(2015) Simon Giroux et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and evaluation of NS5A inhibitors containing diverse heteroaromatic cores

(2015) James A. Henderson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Daclatasvir: A Review of Its Use in Adult Patients with Chronic Hepatitis C Virus Infection

(2015) Paul L. McCormack   DRUGS

Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors

(2015) Il Hak Bae et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Applications of Fluorine in Medicinal Chemistry

(2015) Eric P. Gillis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Resensitizing daclatasvir-resistant hepatitis C variants by allosteric modulation of NS5A

(2015) Jin-Hua Sun et al.   NATURE

Combination of AGET ATRP and SuFEx for post-polymerization chain-end modifications

(2015) Shaohua Li et al.   POLYMER

Sulfonyl fluorides as privileged warheads in chemical biology

(2015) Arjun Narayanan et al.   Chemical Science

Sulfur(VI) Fluoride Exchange (SuFEx): Another Good Reaction for Click Chemistry

(2014) Jiajia Dong et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

SuFEx-Based Synthesis of Polysulfates

(2014) Jiajia Dong et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Comparison of Daclatasvir Resistance Barriers on NS5A from Hepatitis C Virus Genotypes 1 to 6: Implications for Cross-Genotype Activity

(2014) Chunfu Wang et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Update on hepatitis C virus resistance to direct-acting antiviral agents

(2014) Eva Poveda et al.   ANTIVIRAL RESEARCH

Current race in the development of DAAs (direct-acting antivirals) against HCV

(2014) Erik De Clercq   BIOCHEMICAL PHARMACOLOGY

Discovery of functionalized bisimidazoles bearing cyclic aliphatic-phenyl motifs as HCV NS5A inhibitors

(2014) Min Zhong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent bisimidazole-based HCV NS5A inhibitors bearing annulated tricyclic motifs

(2014) Min Zhong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hepatitis C virus NS5A: enigmatic but still promiscuous 10 years on!

(2014) D. Ross-Thriepland et al.   JOURNAL OF GENERAL VIROLOGY

Novel Spiroketal Pyrrolidine GSK2336805 Potently Inhibits Key Hepatitis C Virus Genotype 1b Mutants: From Lead to Clinical Compound

(2014) Wieslaw M. Kazmierski et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hepatitis C Virus NS5A Replication Complex Inhibitors. Part 6: Discovery of a Novel and Highly Potent Biarylimidazole Chemotype with Inhibitory Activity Toward Genotypes 1a and 1b Replicons

(2014) Makonen Belema et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery and Development of Hepatitis C Virus NS5A Replication Complex Inhibitors

(2014) Makonen Belema et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Highly Potent Hepatitis C Virus NS5A Inhibitor (AV4025)

(2014) Alexandre V. Ivachtchenko et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Daclatasvir, a Pan-Genotypic Hepatitis C Virus NS5A Replication Complex Inhibitor with Potent Clinical Effect

(2014) Makonen Belema et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of ABT-267, a Pan-Genotypic Inhibitor of HCV NS5A

(2014) David A. DeGoey et al.   JOURNAL OF MEDICINAL CHEMISTRY

Asymmetric Binding to NS5A by Daclatasvir (BMS-790052) and Analogs Suggests Two Novel Modes of HCV Inhibition

(2014) James H. Nettles et al.   JOURNAL OF MEDICINAL CHEMISTRY

Treatment of hepatitis C: Perspectives

(2014) S. Pol et al.   MEDECINE ET MALADIES INFECTIEUSES

Daclatasvir plus Sofosbuvir for Previously Treated or Untreated Chronic HCV Infection

(2014) Mark S. Sulkowski et al.   NEW ENGLAND JOURNAL OF MEDICINE

Resistance Patterns Associated with HCV NS5A Inhibitors Provide Limited Insight into Drug Binding

(2014) Moheshwarnath Issur et al.   Viruses-Basel

Potent hepatitis C inhibitors bind directly to NS5A and reduce its affinity for RNA

(2014) David B. Ascher et al.   Scientific Reports

Antiviral treatment of hepatitis C

(2014) E. R. Feeney et al.   BMJ-British Medical Journal

Synthesis and evaluation of non-dimeric HCV NS5A inhibitors

(2013) Franck Amblard et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

HCV NS5A replication complex inhibitors. Part 5: Discovery of potent and pan-genotypic glycinamide cap derivatives

(2013) Makonen Belema et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of MK-8742: An HCV NS5A Inhibitor with Broad Genotype Activity

(2013) Craig A. Coburn et al.   ChemMedChem

New horizons in hepatitis C antiviral therapy with direct-acting antivirals

(2013) Alessio Aghemo et al.   HEPATOLOGY

HCV NS5A Replication Complex Inhibitors. Part 4.1 Optimization for Genotype 1a Replicon Inhibitory Activity

(2013) Denis R. St. Laurent et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Ledipasvir (GS-5885): A Potent, Once-Daily Oral NS5A Inhibitor for the Treatment of Hepatitis C Virus Infection

(2013) John O. Link et al.   JOURNAL OF MEDICINAL CHEMISTRY

Future therapies for chronic hepatitis C

(2013) Noura M. Dabbouseh et al.   Nature Reviews Gastroenterology & Hepatology

Characterizations of HCV NS5A replication complex inhibitors

(2013) Donald R. O'Boyle II et al.   VIROLOGY

Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors

(2013) Simon Giroux et al.   ACS Medicinal Chemistry Letters

Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core

(2013) Il Hak Bae et al.   ACS Medicinal Chemistry Letters

Direct-Acting Antiviral Agents for Hepatitis C Virus Infection

(2012) Jennifer J. Kiser et al.   Annual Review of Pharmacology and Toxicology

Hepatitis C Virus RNA Elimination and Development of Resistance in Replicon Cells Treated with BMS-790052

(2012) Chunfu Wang et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis and biological evaluation of new potent and selective HCV NS5A inhibitors

(2012) Junxing Shi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

HCV NS5A replication complex inhibitors. Part 3: discovery of potent analogs with distinct core topologies

(2012) Omar D. Lopez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Interferon-Free Hepatitis C Therapy

(2012) Paul J. Pockros   DRUGS

Correlation between NS5A Dimerization and Hepatitis C Virus Replication

(2012) Precious J. Lim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Drugs in development for chronic hepatitis C: a promising future

(2011) Paul J Pockros   EXPERT OPINION ON BIOLOGICAL THERAPY

Multiple ascending dose study of BMS-790052, a nonstructural protein 5A replication complex inhibitor, in patients infected with hepatitis C virus genotype 1

(2011) Richard E. Nettles et al.   HEPATOLOGY

Genotypic and phenotypic analysis of variants resistant to hepatitis C virus nonstructural protein 5A replication complex inhibitor BMS-790052 in Humans: In Vitro and In Vivo Correlations

(2011) Robert A. Fridell et al.   HEPATOLOGY

Small Molecules Targeting Hepatitis C Virus-Encoded NS5A Cause Subcellular Redistribution of Their Target: Insights into Compound Modes of Action

(2011) P. Targett-Adams et al.   JOURNAL OF VIROLOGY

Therapeutics: New drugs hit the target

(2011) Jana Schlütter   NATURE

New Merck and Vertex drugs raise standard of care in hepatitis C

(2011) Cormac Sheridan   NATURE BIOTECHNOLOGY

Hepatitis C: move over interferon

(2011) Ken Garber   NATURE BIOTECHNOLOGY

Generation of a Cell Culture-Adapted Hepatitis C Virus with Longer Half Life at Physiological Temperature

(2011) Chon Saeng Kim et al.   PLoS One

Inhibitors of HCV NS5A: From Iminothiazolidinones to Symmetrical Stilbenes

(2011) Jeffrey L. Romine et al.   ACS Medicinal Chemistry Letters

Receptor activity and conformational analysis of 5′-halogenated resiniferatoxin analogs as TRPV1 ligands

(2010) Kwang Su Lim et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Drugs for Hepatitis C: Unlocking a New Mechanism of Action

(2010) Thomas W. Bell   ChemMedChem

The C-Terminal  -Helix Domain of Apolipoprotein E Is Required for Interaction with Nonstructural Protein 5A and Assembly of Hepatitis C Virus

(2010) W. Cun et al.   JOURNAL OF VIROLOGY

Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect

(2010) Min Gao et al.   NATURE

Assembly of infectious hepatitis C virus particles

(2010) Ralf Bartenschlager et al.   TRENDS IN MICROBIOLOGY

Crystal Structure of a Novel Dimeric Form of NS5A Domain I Protein from Hepatitis C Virus

(2009) R. A. Love et al.   JOURNAL OF VIROLOGY

The global burden of hepatitis C

(2009) Daniel Lavanchy   LIVER INTERNATIONAL