Arun K Ghosh

Arun K Ghosh

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Arun K Ghosh

Publications by authors named "Arun K Ghosh"

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Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.

J Med Chem 2019 Dec 2. Epub 2019 Dec 2.

Department of Chemistry and Department of Medicinal Chemistry , Purdue University , West Lafayette , Indiana 47907 , United States.

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http://dx.doi.org/10.1021/acs.jmedchem.9b01541DOI Listing
December 2019

Potent antiviral HIV-1 protease inhibitor combats highly drug resistant mutant PR20.

Biochem Biophys Res Commun 2019 Oct 29;519(1):61-66. Epub 2019 Aug 29.

Department of Biology, Georgia State University, Atlanta, GA, 30303, USA; Department of Chemistry, Georgia State University, Atlanta, GA, 30303, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bbrc.2019.08.126DOI Listing
October 2019

Potent HIV-1 protease inhibitors incorporating squaramide-derived P2 ligands: Design, synthesis, and biological evaluation.

Bioorg Med Chem Lett 2019 Sep 5;29(18):2565-2570. Epub 2019 Aug 5.

Department of Refractory Viral Infections, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch National Cancer Institute, Bethesda, MD 20892, USA; Division of Clinical Sciences, Kumamoto University Hospital, Kumamoto 860-8556, Japan.

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http://dx.doi.org/10.1016/j.bmcl.2019.08.006DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6711809PMC
September 2019

A Photochemical Route to Optically Active Hexahydro-4-furopyranol, a High-Affinity P2 Ligand for HIV-1 Protease Inhibitors.

J Org Chem 2019 Aug 16;84(15):9801-9805. Epub 2019 Jul 16.

Department of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.

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http://dx.doi.org/10.1021/acs.joc.9b01361DOI Listing
August 2019

Structural studies of antiviral inhibitor with HIV-1 protease bearing drug resistant substitutions of V32I, I47V and V82I.

Biochem Biophys Res Commun 2019 Jun 12;514(3):974-978. Epub 2019 May 12.

Department of Biology, Georgia State University, Atlanta, GA, 30303, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bbrc.2019.05.064DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6601333PMC
June 2019

Enantioselective Total Syntheses of (+)-Fendleridine and (+)-Acetylaspidoalbidine.

J Org Chem 2019 May 2;84(9):5167-5175. Epub 2019 Apr 2.

Department of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.

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http://dx.doi.org/10.1021/acs.joc.9b00145DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6594018PMC
May 2019

Enantioselective Total Synthesis of (+)-Monocerin, a Dihydroisocoumarin Derivative with Potent Antimalarial Properties.

J Org Chem 2019 May 29;84(10):6191-6198. Epub 2019 Apr 29.

Department of Chemistry and Department of Medicinal Chemistry , Purdue University , 560 Oval Drive , West Lafayette , Indiana 47907 , United States.

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http://dx.doi.org/10.1021/acs.joc.9b00414DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6637414PMC
May 2019

Activity and structural analysis of GRL-117C: a novel small molecule CCR5 inhibitor active against R5-tropic HIV-1s.

Sci Rep 2019 Mar 18;9(1):4828. Epub 2019 Mar 18.

Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, 20892-1868, USA.

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http://www.nature.com/articles/s41598-019-41080-w
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http://dx.doi.org/10.1038/s41598-019-41080-wDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6423129PMC
March 2019

Design, synthesis, and X-ray studies of potent HIV-1 protease inhibitors incorporating aminothiochromane and aminotetrahydronaphthalene carboxamide derivatives as the P2 ligands.

Eur J Med Chem 2018 Dec 18;160:171-182. Epub 2018 Sep 18.

Department of Refractory Viral Infections, National Center for Global Health & Medicine Research Institute, Tokyo, 162-8655, Japan; Departments of Hematology and Infectious Diseases, Kumamoto University Graduate School of Medical and Pharmaceutical Sciences, Kumamoto, 860-8556, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD, 20892, United States.

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https://linkinghub.elsevier.com/retrieve/pii/S02235234183081
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http://dx.doi.org/10.1016/j.ejmech.2018.09.046DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6237192PMC
December 2018

The Curtius Rearrangement: Applications in Modern Drug Discovery and Medicinal Chemistry.

ChemMedChem 2018 11 11;13(22):2351-2373. Epub 2018 Oct 11.

Department of Chemistry and Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, IN, 47907, USA.

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http://dx.doi.org/10.1002/cmdc.201800518DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6604631PMC
November 2018

Enantioselective Synthesis of a Cyclopropane Derivative of Spliceostatin A and Evaluation of Bioactivity.

Org Lett 2018 11 5;20(22):7293-7297. Epub 2018 Nov 5.

Department of Molecular Cell and Developmental Biology and Center for Molecular Biology of RNA , University of California , Santa Cruz , California 95064 , United States.

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http://pubs.acs.org/doi/10.1021/acs.orglett.8b03228
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http://dx.doi.org/10.1021/acs.orglett.8b03228DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6519444PMC
November 2018

Drug Resistance Mutation L76V Alters Nonpolar Interactions at the Flap-Core Interface of HIV-1 Protease.

ACS Omega 2018 Sep 27;3(9):12132-12140. Epub 2018 Sep 27.

Department of Biology, Molecular Basis of Disease Program, Department of Computer Science, and Department of Chemistry, Georgia State University, Atlanta, Georgia 30303, United States.

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http://dx.doi.org/10.1021/acsomega.8b01683DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6167001PMC
September 2018

Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand.

Bioorg Med Chem Lett 2018 08 26;28(15):2605-2610. Epub 2018 Jun 26.

Department of Chemistry, Purdue University, West Lafayette, IN 47907, United States; Department of Biochemistry, Purdue University, West Lafayette, IN 47907, United States; Department of Biological Sciences, Purdue University, West Lafayette, IN 47907, United States.

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http://dx.doi.org/10.1016/j.bmcl.2018.06.045DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6085084PMC
August 2018

Nature Inspired Molecular Design: Stereoselective Synthesis of Bicyclic and Polycyclic Ethers for Potent HIV-1 Protease Inhibitors.

Asian J Org Chem 2018 Aug 8;7(8):1448-1466. Epub 2018 Jun 8.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907 (USA).

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http://dx.doi.org/10.1002/ajoc.201800255DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6781882PMC
August 2018

Enantioselective total synthesis of decytospolide A and decytospolide B using an Achmatowicz reaction.

Org Biomol Chem 2018 08;16(33):5979-5986

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, USA.

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http://dx.doi.org/10.1039/c8ob01529eDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6128299PMC
August 2018

Determination of absolute configuration and binding efficacy of benzimidazole-based FabI inhibitors through the support of electronic circular dichroism and MM-GBSA techniques.

Bioorg Med Chem Lett 2018 06 22;28(11):2074-2079. Epub 2018 Apr 22.

Center for Biomolecular Sciences, University of Illinois at Chicago, 900 S. Ashland Ave, Chicago, IL 60607, USA; Novalex Therapeutics, Inc., 2242 W Harrison, Chicago, IL 60612, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2018.04.052DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5970947PMC
June 2018

GRL-079, a Novel HIV-1 Protease Inhibitor, Is Extremely Potent against Multidrug-Resistant HIV-1 Variants and Has a High Genetic Barrier against the Emergence of Resistant Variants.

Antimicrob Agents Chemother 2018 05 26;62(5). Epub 2018 Apr 26.

Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA

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http://dx.doi.org/10.1128/AAC.02060-17DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5923169PMC
May 2018

Enantioselective Synthesis of Thailanstatin A Methyl Ester and Evaluation of in Vitro Splicing Inhibition.

J Org Chem 2018 05 26;83(9):5187-5198. Epub 2018 Apr 26.

Department of Molecular, Cell and Developmental Biology and Center for Molecular Biology of RNA , University of California, Santa Cruz , California 95064 , United States.

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http://dx.doi.org/10.1021/acs.joc.8b00593DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5972027PMC
May 2018

The Curtius rearrangement: mechanistic insight and recent applications in natural product syntheses.

Org Biomol Chem 2018 03 26;16(12):2006-2027. Epub 2018 Feb 26.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.

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http://xlink.rsc.org/?DOI=C8OB00138C
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http://dx.doi.org/10.1039/c8ob00138cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5864567PMC
March 2018

Mechanism of Darunavir (DRV)'s High Genetic Barrier to HIV-1 Resistance: A Key V32I Substitution in Protease Rarely Occurs, but Once It Occurs, It Predisposes HIV-1 To Develop DRV Resistance.

mBio 2018 03 6;9(2). Epub 2018 Mar 6.

Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA

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http://dx.doi.org/10.1128/mBio.02425-17DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5844992PMC
March 2018

Enantioselective Synthesis of Spliceostatin G and Evaluation of Bioactivity of Spliceostatin G and Its Methyl Ester.

Org Lett 2018 01 8;20(1):96-99. Epub 2017 Dec 8.

Department of Molecular Cell and Developmental Biology and Center for Molecular Biology of RNA, University of California , Santa Cruz, California 95064, United States.

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http://dx.doi.org/10.1021/acs.orglett.7b03456DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5972028PMC
January 2018

Design, Synthesis, Biological Evaluation, and X-ray Studies of HIV-1 Protease Inhibitors with Modified P2' Ligands of Darunavir.

ChemMedChem 2017 12 24;12(23):1942-1952. Epub 2017 Nov 24.

Departments of Hematology and Infectious Diseases, Kumamoto University School of Medicine, Kumamoto, 860-8556, Japan.

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http://dx.doi.org/10.1002/cmdc.201700614DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5896574PMC
December 2017

Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.

Bioorg Med Chem Lett 2017 11 6;27(21):4925-4931. Epub 2017 Sep 6.

Departments of Hematology and Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch National Cancer Institute, Bethesda, MD 20892, USA; Center for Clinical Sciences, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan.

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http://dx.doi.org/10.1016/j.bmcl.2017.09.003DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5647257PMC
November 2017

Design of novel HIV-1 protease inhibitors incorporating isophthalamide-derived P2-P3 ligands: Synthesis, biological evaluation and X-ray structural studies of inhibitor-HIV-1 protease complex.

Bioorg Med Chem 2017 10 9;25(19):5114-5127. Epub 2017 Apr 9.

Department of Hematology, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Department of Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch National Cancer Institute, Bethesda, MD 20892, USA; Department of Refractory Viral Infection, National Center for Global Health and Medicine Research Institute, Shinjuku, Tokyo 162-8655, Japan.

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https://linkinghub.elsevier.com/retrieve/pii/S09680896173073
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http://dx.doi.org/10.1016/j.bmc.2017.04.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5617771PMC
October 2017

Highly Stereoselective Asymmetric Aldol Routes to -Butyl-2-(3,5-difluorophenyl)-1-oxiran-2-yl)ethyl)carbamates: Building Blocks for Novel Protease Inhibitors.

Tetrahedron Lett 2017 10 14;58(43):4062-4065. Epub 2017 Sep 14.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1016/j.tetlet.2017.09.025DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5765997PMC
October 2017

Lewis Acid Mediated Cyclizations: Diastereoselective Synthesis of Six- to Eight-Membered Substituted Cyclic Ethers.

Synthesis (Stuttg) 2017 Sep 25;49(18):4229-4246. Epub 2017 Jul 25.

Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN, 47907, USA.

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http://dx.doi.org/10.1055/s-0036-1589054DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6034514PMC
September 2017

An enantioselective enzymatic desymmetrization route to hexahydro-4-furopyranol, a high-affinity ligand for HIV-1 protease inhibitors.

Tetrahedron Lett 2017 08 3;58(33):3230-3233. Epub 2017 Jul 3.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 479 07, United States.

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https://linkinghub.elsevier.com/retrieve/pii/S00404039173084
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http://dx.doi.org/10.1016/j.tetlet.2017.07.010DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5708567PMC
August 2017

Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.

Bioorg Med Chem Lett 2017 06 8;27(11):2432-2438. Epub 2017 Apr 8.

Department of Chemistry, Purdue University, West Lafayette, IN 47907, United States; Department of Biological Sciences, Purdue University, West Lafayette, IN 47907, United States; Department of Biochemistry, Purdue University, West Lafayette, IN 47907, United States.

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http://dx.doi.org/10.1016/j.bmcl.2017.04.011DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5479133PMC
June 2017

HIV-Associated Neurocognitive Disorder (HAND) and the Prospect of Brain-Penetrating Protease Inhibitors for Antiretroviral Treatment.

Med Res Arch 2017 Apr 15;5(4). Epub 2017 Apr 15.

Departments of Infectious Diseases and Hematology, Kumamoto University Graduate School of Biomedical Sciences, Kumamoto 860-8556, Japan.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6034681PMC
April 2017

Total syntheses of both enantiomers of amphirionin 4: A chemoenzymatic based strategy for functionalized tetrahydrofurans.

Tetrahedron 2017 Apr 17;73(14):1820-1830. Epub 2017 Feb 17.

Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1016/j.tet.2017.02.031DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5621746PMC
April 2017

Benzimidazole-Based FabI Inhibitors: A Promising Novel Scaffold for Anti-staphylococcal Drug Development.

ACS Infect Dis 2017 01 27;3(1):54-61. Epub 2016 Oct 27.

Novalex Therapeutics , 2242 W. Harrison, Chicago, Illinois 60612, United States.

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http://dx.doi.org/10.1021/acsinfecdis.6b00123DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5659837PMC
January 2017

A fission yeast cell-based system for multidrug resistant HIV-1 proteases.

Cell Biosci 2017 11;7. Epub 2017 Jan 11.

Department of Pathology, University of Maryland School of Medicine, Baltimore, MD 21201 USA ; Department of Microbiology-Immunology, University of Maryland School of Medicine, Baltimore, MD 21201 USA ; Institute of Human Virology, University of Maryland School of Medicine, Baltimore, MD 21201 USA ; Children's Memorial Institute for Education and Research, Northwestern University Feinberg School of Medicine, Chicago, IL 10164 USA.

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http://cellandbioscience.biomedcentral.com/articles/10.1186/
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http://dx.doi.org/10.1186/s13578-016-0131-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5225522PMC
January 2017

Enantioselective total synthesis and structural assignment of callyspongiolide.

Org Biomol Chem 2016 Dec;14(48):11357-11370

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, USA.

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http://xlink.rsc.org/?DOI=C6OB02051H
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http://dx.doi.org/10.1039/c6ob02051hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5143229PMC
December 2016

Enantioselective Syntheses of (-)-Alloyohimbane and (-)-Yohimbane by an Efficient Enzymatic Desymmetrization Process.

European J Org Chem 2016 Dec 28;2016(36):6001-6009. Epub 2016 Nov 28.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana, 47906 (USA).

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http://dx.doi.org/10.1002/ejoc.201601171DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5526648PMC
December 2016

Achmatowicz Reaction and its Application in the Syntheses of Bioactive Molecules.

RSC Adv 2016 24;6(112):111564-111598. Epub 2016 Nov 24.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.

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http://dx.doi.org/10.1039/C6RA22611FDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5603243PMC
November 2016

Enantioselective Synthesis of Both Epimers at C-21 in the Proposed Structure of Cytotoxic Macrolide Callyspongiolide.

Org Lett 2016 07 22;18(13):3274-7. Epub 2016 Jun 22.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://pubs.acs.org/doi/10.1021/acs.orglett.6b01523
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http://dx.doi.org/10.1021/acs.orglett.6b01523DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6037179PMC
July 2016

Correction to Enantioselective Total Synthesis of (+)-Amphirionin-4.

Org Lett 2016 07 22;18(14):3509. Epub 2016 Jun 22.

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http://dx.doi.org/10.1021/acs.orglett.6b01620DOI Listing
July 2016

Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS.

J Med Chem 2016 06 22;59(11):5172-208. Epub 2016 Jan 22.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , West Lafayette, Indiana 47907, United States.

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http://pubs.acs.org/doi/10.1021/acs.jmedchem.5b01697
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http://dx.doi.org/10.1021/acs.jmedchem.5b01697DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5598487PMC
June 2016

Design, synthesis and in vitro splicing inhibition of desmethyl and carba-derivatives of herboxidiene.

Org Biomol Chem 2016 Jun 18;14(23):5263-71. Epub 2016 May 18.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.

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http://dx.doi.org/10.1039/c6ob00725bDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5333946PMC
June 2016

Anharmonic modeling of the conformation-specific IR spectra of ethyl, n-propyl, and n-butylbenzene.

J Chem Phys 2016 Jun;144(22):224310

Department of Chemistry and Theoretical Chemistry Institute, University of Wisconsin-Madison, Madison, Wisconsin 53706, USA.

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http://dx.doi.org/10.1063/1.4953181DOI Listing
June 2016

An enantioselective synthesis of the C3-C21 segment of the macrolide immunosuppressive agent FR252921.

Tetrahedron Lett 2016 Jun 18;57(26):2884-2887. Epub 2016 May 18.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1016/j.tetlet.2016.05.067DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5094281PMC
June 2016

Defining Viral Defective Ribosomal Products: Standard and Alternative Translation Initiation Events Generate a Common Peptide from Influenza A Virus M2 and M1 mRNAs.

J Immunol 2016 05 25;196(9):3608-17. Epub 2016 Mar 25.

Laboratory of Viral Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD 20892; and

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http://dx.doi.org/10.4049/jimmunol.1502303DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4868770PMC
May 2016

Enantioselective Total Synthesis of (+)-Amphirionin-4.

Org Lett 2016 05 26;18(9):2296-9. Epub 2016 Apr 26.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1021/acs.orglett.6b00942DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5328589PMC
May 2016

Design of Potent and Highly Selective Inhibitors for Human β-Secretase 2 (Memapsin 1), a Target for Type 2 Diabetes.

Chem Sci 2016 May 4;7:3117-3122. Epub 2016 Feb 4.

Department of Biological Sciences, Purdue University, West Lafayette, IN 47907 (USA); Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907 (USA); Department of Biochemistry, Purdue University, West Lafayette, IN 47907 (USA).

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http://dx.doi.org/10.1039/C5SC03718BDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4916918PMC
May 2016

Interchangeable SF3B1 inhibitors interfere with pre-mRNA splicing at multiple stages.

RNA 2016 Mar 7;22(3):350-9. Epub 2016 Jan 7.

Department of Molecular Cell and Developmental Biology, University of California, Santa Cruz, California 95064, USA Center for Molecular Biology of RNA, University of California, Santa Cruz, California 95064, USA.

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http://rnajournal.cshlp.org/lookup/doi/10.1261/rna.053108.11
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http://dx.doi.org/10.1261/rna.053108.115DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4748813PMC
March 2016

Stereoselective Synthesis of Substituted Oxocene Cores by Lewis Acid Promoted Cyclization.

Org Lett 2016 Feb 27;18(3):396-9. Epub 2016 Jan 27.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://pubs.acs.org/doi/10.1021/acs.orglett.5b03411
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http://dx.doi.org/10.1021/acs.orglett.5b03411DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5317094PMC
February 2016

Structure-based design, synthesis, X-ray studies, and biological evaluation of novel HIV-1 protease inhibitors containing isophthalamide-derived P2-ligands.

Bioorg Med Chem Lett 2015 Nov 30;25(21):4903-4909. Epub 2015 May 30.

Departments of Hematology and Infectious Diseases, Kumamoto University of Medicine, Kumamoto 860-8556, Japan; Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, Bethesda, MD 20892, USA; Center for Clinical Sciences, National Center for Global Health and Medicine, Shinjuku, Tokyo 162-8655, Japan.

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http://dx.doi.org/10.1016/j.bmcl.2015.05.052DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4607586PMC
November 2015

C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including Darunavir.

J Virol 2015 Nov 18;90(5):2180-94. Epub 2015 Nov 18.

Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA Departments of Infectious Diseases and Hematology, Kumamoto University Graduate School of Medical Sciences, Kumamoto, Japan Research Institute and Center for Clinical Sciences, National Center for Global Health and Medicine, Tokyo, Japan

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http://dx.doi.org/10.1128/JVI.01829-15DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4810716PMC
November 2015

X-ray structure and inhibition of the feline infectious peritonitis virus 3C-like protease: Structural implications for drug design.

Bioorg Med Chem Lett 2015 Nov 13;25(22):5072-7. Epub 2015 Oct 13.

Departments of Biochemistry and Biological Sciences, Purdue University, West Lafayette, IN, USA; Centers for Cancer Research & Drug Discovery, Purdue University, West Lafayette, IN, USA; Department of Chemistry, Purdue University, West Lafayette, IN, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2015.10.023DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5896745PMC
November 2015

Prospects of β-Secretase Inhibitors for the Treatment of Alzheimer's Disease.

ChemMedChem 2015 Sep 3;10(9):1463-6. Epub 2015 Jul 3.

Protein Studies Program, Oklahoma Medical Research Foundation, Oklahoma City, OK 73104 (USA).

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http://dx.doi.org/10.1002/cmdc.201500216DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6029879PMC
September 2015

Structure-based design of potent HIV-1 protease inhibitors with modified P1-biphenyl ligands: synthesis, biological evaluation, and enzyme-inhibitor X-ray structural studies.

J Med Chem 2015 Jul 24;58(13):5334-43. Epub 2015 Jun 24.

§Departments of Hematology and Infectious Diseases, Kumamoto University Graduate School of Medical and Pharmaceutical Sciences, Kumamoto 860-8556, Japan.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00676DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4765733PMC
July 2015

Inhibitor recognition specificity of MERS-CoV papain-like protease may differ from that of SARS-CoV.

ACS Chem Biol 2015 Jun 16;10(6):1456-65. Epub 2015 Mar 16.

†Center for Pharmaceutical Biotechnology and Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 900 S. Ashland, Chicago, Illinois 60607, United States.

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http://dx.doi.org/10.1021/cb500917mDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4845099PMC
June 2015

Substituted Bis-THF Protease Inhibitors with Improved Potency against Highly Resistant Mature HIV-1 Protease PR20.

J Med Chem 2015 Jun 4;58(12):5088-95. Epub 2015 Jun 4.

†Department of Biology, Molecular Basis of Disease Program, Georgia State University, Atlanta, Georgia 30303, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00474DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4522690PMC
June 2015

Activation of RAF1 (c-RAF) by the Marine Alkaloid Lasonolide A Induces Rapid Premature Chromosome Condensation.

Mar Drugs 2015 Jun 5;13(6):3625-39. Epub 2015 Jun 5.

Developmental Therapeutics Branch and Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute (CCR-NCI), NIH, Bethesda, MD 20892-9760, USA.

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http://dx.doi.org/10.3390/md13063625DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4483648PMC
June 2015

Enantioselective Synthesis of Dioxatriquinane Structural Motifs for HIV-1 Protease Inhibitors Using a Cascade Radical Cyclization.

Tetrahedron Lett 2015 Jun;56(23):3314-3317

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1016/j.tetlet.2015.01.019DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4500529PMC
June 2015

A novel tricyclic ligand-containing nonpeptidic HIV-1 protease inhibitor, GRL-0739, effectively inhibits the replication of multidrug-resistant HIV-1 variants and has a desirable central nervous system penetration property in vitro.

Antimicrob Agents Chemother 2015 May 17;59(5):2625-35. Epub 2015 Feb 17.

Departments of Infectious Diseases and Hematology, Kumamoto University School of Medicine, Kumamoto, Japan Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA Center for Clinical Sciences, National Center for Global Health and Medicine, Tokyo, Japan

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http://dx.doi.org/10.1128/AAC.04757-14DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4394833PMC
May 2015

Organic carbamates in drug design and medicinal chemistry.

J Med Chem 2015 Apr 7;58(7):2895-940. Epub 2015 Jan 7.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1021/jm501371sDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4393377PMC
April 2015

Insights into the mechanism of inhibition of CXCR4: identification of Piperidinylethanamine analogs as anti-HIV-1 inhibitors.

Antimicrob Agents Chemother 2015 Apr 12;59(4):1895-904. Epub 2015 Jan 12.

Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA Departments of Hematology and Infectious Diseases, Kumamoto University Graduate School of Medical and Pharmaceutical Sciences, Kumamoto, Japan.

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http://dx.doi.org/10.1128/AAC.04654-14DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4356787PMC
April 2015

Structural and biological evaluation of a novel series of benzimidazole inhibitors of Francisella tularensis enoyl-ACP reductase (FabI).

Bioorg Med Chem Lett 2015 Mar 29;25(6):1292-6. Epub 2015 Jan 29.

Center for Pharmaceutical Biotechnology, University of Illinois at Chicago, Chicago, IL 60607, United States; Novalex Therapeutics, 2242 W. Harrison, Chicago, IL 60612, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2015.01.048DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4348352PMC
March 2015

Structure-based design, synthesis and biological evaluation of novel β-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.

Bioorg Med Chem Lett 2015 Feb 6;25(3):668-72. Epub 2014 Dec 6.

Department of Chemistry, Purdue University, West Lafayette, IN 47907, United States; Protein Studies Program, Oklahoma Medical Research Foundation, United States; Department of Biochemistry and Molecular Biology, University of Oklahoma Health Science Center, Oklahoma City, OK 73104, United States.

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http://dx.doi.org/10.1016/j.bmcl.2014.11.087DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4297543PMC
February 2015

Characterization of a Drosophila ortholog of the Cdc7 kinase: a role for Cdc7 in endoreplication independent of Chiffon.

J Biol Chem 2015 Jan 1;290(3):1332-47. Epub 2014 Dec 1.

From the Departments of Biochemistry and Purdue University Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907

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http://dx.doi.org/10.1074/jbc.M114.597948DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4340381PMC
January 2015

Enantioselective synthesis of spliceostatin E and evaluation of biological activity.

Org Lett 2014 Dec 25;16(23):6200-3. Epub 2014 Nov 25.

‡Department of Molecular Cell and Developmental Biology and Center for Molecular Biology of RNA, University of California, Santa Cruz, California 95064, United States.

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http://pubs.acs.org/doi/10.1021/ol503127r
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4260646PMC
December 2014

BACE1 (β-secretase) inhibitors for the treatment of Alzheimer's disease.

Chem Soc Rev 2014 Oct;43(19):6765-813

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.

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http://dx.doi.org/10.1039/c3cs60460hDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4159447PMC
October 2014

A convergent synthesis of carbocyclic sinefungin and its C5 epimer.

Authors:
Arun K Ghosh Kai Lv

European J Org Chem 2014 Oct;2014(30):6761-6768

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, Indiana, 47906 (USA).

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http://dx.doi.org/10.1002/ejoc.201402812DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4267295PMC
October 2014

Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1-P2 ligands.

Org Biomol Chem 2014 Sep;12(35):6842-54

Departments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.

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http://dx.doi.org/10.1039/c4ob00738gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4133278PMC
September 2014

An Enantioselective Synthesis of a MEM-Protected Aetheramide A Derivative.

Tetrahedron Lett 2014 Sep;55(37):5191-5194

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1016/j.tetlet.2014.07.077DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4153992PMC
September 2014

Dimerization of HIV-1 protease occurs through two steps relating to the mechanism of protease dimerization inhibition by darunavir.

Proc Natl Acad Sci U S A 2014 Aug 4;111(33):12234-9. Epub 2014 Aug 4.

Departments of Hematology, Rheumatology, and Infectious Disease, Kumamoto University Graduate School of Medicine, 1-1-1 Honjo, Chuo-ku, Kumamoto 860-8556, Japan;Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892;

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http://dx.doi.org/10.1073/pnas.1400027111DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4142999PMC
August 2014

A conserved hydrogen-bonding network of P2 bis-tetrahydrofuran-containing HIV-1 protease inhibitors (PIs) with a protease active-site amino acid backbone aids in their activity against PI-resistant HIV.

Antimicrob Agents Chemother 2014 Jul 21;58(7):3679-88. Epub 2014 Apr 21.

Experimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA Departments of Hematology and Infectious Diseases, Kumamoto University Graduate School of Biomedical Sciences, Kumamoto, Japan

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http://dx.doi.org/10.1128/AAC.00107-14DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4068604PMC
July 2014

FeCl-Catalyzed Tandem Prins and Friedel-Crafts Cyclization: A Highly Diastereoselective Route to Polycyclic Ring Structures.

Tetrahedron Lett 2014 Jul;55(30):4251-4254

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1016/j.tetlet.2014.05.092DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4120523PMC
July 2014

An intramolecular cascade cyclization of 2-aryl indoles: efficient methods for the construction of 2,3-functionalized indolines and 3-indolinones.

Org Biomol Chem 2014 Jun 1;12(22):3567-71. Epub 2014 May 1.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.

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http://dx.doi.org/10.1039/c4ob00511bDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4088936PMC
June 2014

Total synthesis of GEX1Q1, assignment of C-5 stereoconfiguration and evaluation of spliceosome inhibitory activity.

Org Lett 2014 Jun 28;16(11):3154-7. Epub 2014 May 28.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://pubs.acs.org/doi/10.1021/ol501345d
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http://dx.doi.org/10.1021/ol501345dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4051430PMC
June 2014

Enantioselective total syntheses of FR901464 and spliceostatin A and evaluation of splicing activity of key derivatives.

J Org Chem 2014 Jun 30;79(12):5697-709. Epub 2014 May 30.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , 560 Oval Drive, West Lafayette, Indiana 4790, United States.

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http://dx.doi.org/10.1021/jo500800kDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4066912PMC
June 2014

Metabolism-directed structure optimization of benzimidazole-based Francisella tularensis enoyl-reductase (FabI) inhibitors.

Xenobiotica 2014 May 30;44(5):404-16. Epub 2013 Oct 30.

Department of Pharmacy Practice, Department of Biopharmaceutical Sciences, College of Pharmacy, University of Illinois at Chicago , Chicago, IL , USA .

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http://dx.doi.org/10.3109/00498254.2013.850553DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4355941PMC
May 2014

Enantioselective total synthesis of macrolide (+)-neopeltolide.

Org Biomol Chem 2013 Nov 11;11(44):7768-77. Epub 2013 Oct 11.

Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, Indiana, USA.

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http://dx.doi.org/10.1039/c3ob41541dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6037168PMC
November 2013

Enantioselective syntheses of FR901464 and spliceostatin A: potent inhibitors of spliceosome.

Org Lett 2013 Oct 19;15(19):5088-91. Epub 2013 Sep 19.

Department of Chemistry and Department of Medicinal Chemistry, Purdue University , 560 Oval Drive, West Lafayette, Indiana 47907, United States.

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http://dx.doi.org/10.1021/ol4024634DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3827971PMC
October 2013

Bifunctional cinchona alkaloid-squaramide-catalyzed highly enantioselective aza-Michael addition of indolines to α,β-unsaturated ketones.

Tetrahedron Lett 2013 Jul;54(27):3500-3502

Department of Chemistry and Medicinal Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907, United States.

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http://dx.doi.org/10.1016/j.tetlet.2013.04.080DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3763959PMC
July 2013