Kevin X. Chen

发表

The Journey to the Discovery of Boceprevir: an NS3-NS4 HCV protease inhibitor for the treatment of chronic hepatitis C.

F. G. Njoroge, Kevin X. Chen, 2010, Progress in medicinal chemistry.

I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.

B. Feld, R. Palermo, J. Duca, 2011, Bioorganic & medicinal chemistry letters.

Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.

B. Feld, J. Duca, F. G. Njoroge, 2012, Journal of medicinal chemistry.

A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors.

B. Feld, J. Duca, F. G. Njoroge, 2012, Journal of medicinal chemistry.

P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile.

X. Tong, A. Prongay, V. Girijavallabhan, 2010, Bioorganic & medicinal chemistry letters.

Design and synthesis of novel fluoro amino acids: synthons for potent macrocyclic HCV NS3 protease inhibitors

F. G. Njoroge, Weing Yang, N. Shih, 2010 .

Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings.

X. Tong, F. G. Njoroge, K. Cheng, 2009, Bioorganic & medicinal chemistry letters.

Potent and selective small molecule NS3 serine protease inhibitors of Hepatitis C virus with dichlorocyclopropylproline as P2 residue.

F. G. Njoroge, K. Cheng, J. Pichardo, 2008, Bioorganic & medicinal chemistry.

The role of P-glycoprotein in the pharmacokinetics and tissue distribution of a hepatitis C virus protease inhibitor.

F. G. Njoroge, Tongtong Liu, A. Uss, 2009, Drug metabolism letters.

Proline-based macrocyclic inhibitors of the hepatitis C virus: stereoselective synthesis and biological activity.

V. Madison, F. G. Njoroge, A. Prongay, 2005, Angewandte Chemie.

Discovery of SCH 900188: A Potent Hepatitis C Virus NS5B Polymerase Inhibitor Prodrug As a Development Candidate.

F. G. Njoroge, K. Cheng, S. Agrawal, 2014, ACS medicinal chemistry letters.

Optimization of potency and pharmacokinetics of tricyclic indole derived inhibitors of HCV NS5B polymerase. Identification of ester prodrugs with improved oral pharmacokinetics.

J. Duca, F. G. Njoroge, S. Agrawal, 2014, Bioorganic & medicinal chemistry.

P2-P4 macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease.

V. Madison, A. Arasappan, F. G. Njoroge, 2006, Bioorganic & medicinal chemistry letters.

Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease.

V. Madison, F. G. Njoroge, A. Prongay, 2005, Bioorganic & medicinal chemistry letters.

Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection.

F. G. Njoroge, N. Shih, J. Piwinski, 2008, Accounts of chemical research.

Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease.

N. Yao, V. Madison, F. G. Njoroge, 2006, Journal of medicinal chemistry.

Stereoselective Synthesis of β-Substituted β-Amino Sulfones and Sulfonamides via Addition of Sulfonyl Anions to Chiral N-Sulfinyl Imines

A. McPhail, A. Arasappan, T. Chan, 2006 .

Discovery of an irreversible HCV NS5B polymerase inhibitor.

J. Gesell, J. Duca, F. G. Njoroge, 2013, Bioorganic & medicinal chemistry letters.

The introduction of P4 substituted 1-methylcyclohexyl groups into Boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor.

Zhuyan Guo, Frank Bennett, X. Tong, 2010, Bioorganic & medicinal chemistry letters.

Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor:

Weiying Yang, Zhuyan Guo, Andrea Hart, 2006, Journal of medicinal chemistry.

A review of HCV protease inhibitors.

F. G. Njoroge, Kevin X. Chen, 2009, Current opinion in investigational drugs.

Discovery of Boceprevir and Narlaprevir: The First and Second Generation of HCV NS3 Protease Inhibitors

F. G. Njoroge, Kevin X. Chen, F. Njoroge, 2012 .

Discovery of novel P3 sulfonamide-capped inhibitors of HCV NS3 protease. Inhibitors with improved cellular potencies.

X. Tong, A. Arasappan, K. Cheng, 2009, Bioorganic & medicinal chemistry.

Discovery of the HCV NS3/4A protease inhibitor (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3- [2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (Sch 503034) II. Key steps in structure-based optimization.

Zhuyan Guo, Frank Bennett, Rong-Sheng Yang, 2007, Journal of medicinal chemistry.

Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor.

Weiying Yang, Frank Bennett, Jesse Wong, 2010, ACS medicinal chemistry letters.

Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication.

S. Tamura, S. Kemp, M. Lim-Wilby, 2006, Journal of medicinal chemistry.

Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.

James I. Fells, E. Asante-Appiah, C. Coburn, 2016, Bioorganic & medicinal chemistry letters.

Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease.

N. Yao, V. Madison, F. G. Njoroge, 2005, Journal of medicinal chemistry.

Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease.

Weiying Yang, Frank Bennett, X. Tong, 2009, Journal of medicinal chemistry.

Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase.

J. Duca, F. G. Njoroge, S. Agrawal, 2013, Bioorganic & medicinal chemistry.

2′-Modified Guanosine Analogs for the Treatment of HCV

Q. Dang, A. Stamford, Vishal A. Verma, 2016, Nucleosides, Nucleotides & Nucleic Acids.

Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles.

Zhuyan Guo, Frank Bennett, Sumei Ruan, 2009, Journal of medicinal chemistry.

Toward second generation hepatitis C virus NS3 serine protease inhibitors: discovery of novel P4 modified analogues with improved potency and pharmacokinetic profile.

Frank Bennett, X. Tong, A. Arasappan, 2009, Journal of medicinal chemistry.

Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease.

Andrea Hart, Robert Chase, Sony Agrawal, 2009, Journal of medicinal chemistry.

Design, synthesis, and evaluation of oxygen-containing macrocyclic peptidomimetics as inhibitors of HCV NS3 protease.

X. Tong, Melissa L. Blackman, J. Pichardo, 2009, Journal of medicinal chemistry.

Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection.

N. Shih, J. Piwinski, Kevin X. Chen, 2008, Accounts of chemical research.

Stereoselective Synthesis of β‐Substituted β‐Amino Sulfones and Sulfonamides via Addition of Sulfonyl Anions to Chiral N‐Sulfinyl Imines.

A. McPhail, A. Arasappan, T. Chan, 2006 .

Stereoselective synthesis of beta-substituted beta-amino sulfones and sulfonamides via addition of sulfonyl anions to chiral N-sulfinyl imines.

A. McPhail, A. Arasappan, T. Chan, 2006, Organic letters.