Jan Balzarini

Jan Balzarini

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Jan Balzarini

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Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents.

Bioorg Chem 2020 Jun 2;101:103960. Epub 2020 Jun 2.

Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, via L. Borsari 46, 44121 Ferrara, Italy.

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http://dx.doi.org/10.1016/j.bioorg.2020.103960DOI Listing
June 2020

Prodrugs of γ-Alkyl-modified Nucleoside Triphosphates - improved Inhibition of HIV Reverse Transcriptase.

Angew Chem Int Ed Engl 2020 May 7. Epub 2020 May 7.

Katholieke Universiteit Leuven Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, BELGIUM.

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http://dx.doi.org/10.1002/anie.202003073DOI Listing
May 2020

Novel Conjugated Unsaturated Ketones with Submicromolar Potencies Towards some Leukemic and Colon Cancer Cells.

Med Chem 2019 ;15(4):430-438

Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, 104 Clinic Place, Saskatoon, Saskatchewan S7N 2Z5, Canada.

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http://www.eurekaselect.com/166245/article
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http://dx.doi.org/10.2174/1573406414666181015142633DOI Listing
June 2019

Alpha-carboxynucleoside phosphonates: direct-acting inhibitors of viral DNA polymerases.

Future Med Chem 2019 01 16;11(2):137-154. Epub 2019 Jan 16.

Department of Chemistry, Analytical & Biological Chemistry Research Facility, Synthesis & Solid State Pharmaceutical Centre, University College, Cork, Ireland.

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https://www.future-science.com/doi/10.4155/fmc-2018-0324
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http://dx.doi.org/10.4155/fmc-2018-0324DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6362432PMC
January 2019

Engineering Lactobacillus rhamnosus GG and GR-1 to express HIV-inhibiting griffithsin.

Int J Antimicrob Agents 2018 Nov 21;52(5):599-607. Epub 2018 Jul 21.

KU Leuven, Centre of Microbial and Plant Genetics, Kasteelpark Arenberg 20, B-3001 Leuven, Belgium; University of Antwerp, Department of Bioscience Engineering, Groenenborgerlaan 171, B-2020 Antwerp, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.ijantimicag.2018.07.013DOI Listing
November 2018

Synthesis and Antiviral Activity of Water-Soluble Polycarboxylic Derivatives of [60]Fullerene Loaded with 3,4-Dichlorophenyl Units.

Chem Biodivers 2018 Nov 29;15(11):e1800293. Epub 2018 Oct 29.

Institute for Problems of Chemical Physics of RAS, Semenov Prospect 1, Chernogolovka, 142432, Russia.

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http://dx.doi.org/10.1002/cbdv.201800293DOI Listing
November 2018

Symmetrical Diamidates as a Class of Phosphate Prodrugs to Deliver the 5'-Monophosphate Forms of Anticancer Nucleoside Analogues.

ChemMedChem 2018 11;13(21):2305-2316

School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff, CF10 3NB, UK.

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http://dx.doi.org/10.1002/cmdc.201800504DOI Listing
November 2018

Synthesis of Guanine α-Carboxy Nucleoside Phosphonate (G-α-CNP), a Direct Inhibitor of Multiple Viral DNA Polymerases.

J Org Chem 2018 09 22;83(17):10510-10517. Epub 2018 Aug 22.

School of Chemistry and School of Pharmacy, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre , University College Cork , Cork , Ireland.

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http://dx.doi.org/10.1021/acs.joc.8b01124DOI Listing
September 2018

The ProTide Prodrug Technology: From the Concept to the Clinic.

J Med Chem 2018 03 24;61(6):2211-2226. Epub 2017 Aug 24.

Laboratory of Virology and Chemotherapy , Rega Institute for Medical Research , Herestraat 49 , 3000 Leuven , Belgium.

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http://dx.doi.org/10.1021/acs.jmedchem.7b00734DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7075648PMC
March 2018

Surface Glycans: A Therapeutic Opportunity for Kinetoplastid Diseases.

Trends Parasitol 2017 10 28;33(10):775-787. Epub 2017 Jul 28.

Instituto de Parasitología y Biomedicina 'López-Neyra', Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Avenida del Conocimiento, s/n 18016-Armilla (Granada), Spain. Electronic address:

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http://dx.doi.org/10.1016/j.pt.2017.06.009DOI Listing
October 2017

New prodrugs of two pyrimidine acyclic nucleoside phosphonates: Synthesis and antiviral activity.

Bioorg Med Chem 2017 09 6;25(17):4637-4648. Epub 2017 Jul 6.

Rega Institute for Medical Research, KU Leuven, Herestraat 49, Box 1043, B-3000 Leuven, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2017.06.046DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126465PMC
September 2017

Guanine α-carboxy nucleoside phosphonate (G-α-CNP) shows a different inhibitory kinetic profile against the DNA polymerases of human immunodeficiency virus (HIV) and herpes viruses.

Biochem Pharmacol 2017 07 6;136:51-61. Epub 2017 Apr 6.

Department of Chemistry, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre, University College Cork, Ireland; School of Pharmacy, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre, University College Cork, Ireland.

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http://dx.doi.org/10.1016/j.bcp.2017.04.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5557014PMC
July 2017

Pronounced anti-proliferative activity and tumor cell selectivity of 5-alkyl-2-amino-3-methylcarboxylate thiophenes.

Eur J Med Chem 2017 May 23;132:219-235. Epub 2017 Mar 23.

KU Leuven, Rega Institute for Medical Research, Herestraat 49, Postbus 1043, B-3000 Leuven, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2017.03.044DOI Listing
May 2017

A Multitarget Approach toward the Development of 8-Substituted Purines for Photoprotection and Prevention of UV-Related Damage.

ChemMedChem 2017 05 3;12(10):760-769. Epub 2017 May 3.

Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, via L. Borsari 46, 44121, Ferrara, Italy.

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http://dx.doi.org/10.1002/cmdc.201700137DOI Listing
May 2017

A new four-component reaction involving the Michael addition and the Gewald reaction, leading to diverse biologically active 2-aminothiophenes.

Org Biomol Chem 2017 May;15(18):3892-3900

Molecular Design and Synthesis, Department of Chemistry, KU Leuven, Celestijnenlaan 200F, 3001 Leuven, Belgium.

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http://dx.doi.org/10.1039/c7ob00707hDOI Listing
May 2017

6-Benzylidene-2-[4-(pyridin-3-ylcarboxy)benzylidene]cyclohexanones: A novel cluster of tumour-selective cytotoxins.

Bioorg Med Chem Lett 2017 04 10;27(7):1611-1615. Epub 2017 Feb 10.

Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan S7N 5E5, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2017.02.016DOI Listing
April 2017

Facile functionalization at the C4 position of pyrimidine nucleosides via amide group activation with (benzotriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (BOP) and biological evaluations of the products.

Org Biomol Chem 2017 Feb;15(5):1130-1139

Department of Chemistry and Biochemistry, The City College of New York, 160 Convent Avenue, New York, New York 10031, USA. and The Ph.D. Program in Chemistry, The Graduate Center of the City University of New York, New York, New York 10016, USA.

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http://xlink.rsc.org/?DOI=C6OB02334G
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http://dx.doi.org/10.1039/c6ob02334gDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5367150PMC
February 2017

Correction: Facile functionalization at the C4 position of pyrimidine nucleosides via amide group activation with (benzotriazol-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (BOP) and biological evaluations of the products.

Org Biomol Chem 2017 02;15(5):1268

Department of Chemistry and Biochemistry, The City College of New York, 160 Convent Avenue, New York, New York 10031, USA. and The Ph.D. Program in Chemistry, The Graduate Center of the City University of New York, New York, New York 10016, USA.

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http://dx.doi.org/10.1039/c7ob90013aDOI Listing
February 2017

Niacin esters of chalcones with tumor-selective properties.

J Enzyme Inhib Med Chem 2016 Dec 2;31(6):1451-6. Epub 2016 Jun 2.

a Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan , Saskatoon , Canada .

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http://dx.doi.org/10.3109/14756366.2016.1144595DOI Listing
December 2016

ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites.

Bioorg Med Chem Lett 2016 12 27;26(23):5618-5623. Epub 2016 Oct 27.

School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.

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http://dx.doi.org/10.1016/j.bmcl.2016.10.077DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5131913PMC
December 2016

Novel isoxazolidine analogues of homonucleosides and homonucleotides.

Tetrahedron 2016 Dec 2;72(50):8294-8308. Epub 2016 Nov 2.

Bioorganic Chemistry Laboratory, Faculty of Pharmacy, Medical University of Łódź, 90-151, Łódź, Muszyńskiego 1, Poland.

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http://dx.doi.org/10.1016/j.tet.2016.10.073DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7111885PMC
December 2016

The role of cellular oxidoreductases in viral entry and virus infection-associated oxidative stress: potential therapeutic applications.

Expert Opin Ther Targets 2016 15;20(1):123-43. Epub 2015 Jul 15.

b 2 Rega Institute for Medical Research, KU Leuven , Minderbroedersstraat 10 blok x - bus 1030, Leuven, Belgium +32 16 3 37352 ; +32 16 3 37340 ;

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http://dx.doi.org/10.1517/14728222.2015.1068760DOI Listing
September 2016

Carbohydrate-Binding Non-Peptidic Pradimicins for the Treatment of Acute Sleeping Sickness in Murine Models.

PLoS Pathog 2016 Sep 23;12(9):e1005851. Epub 2016 Sep 23.

Instituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Armilla (Granada), Spain.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5035034PMC
http://dx.doi.org/10.1371/journal.ppat.1005851DOI Listing
September 2016

Conformational States of HIV-1 Reverse Transcriptase for Nucleotide Incorporation vs Pyrophosphorolysis-Binding of Foscarnet.

ACS Chem Biol 2016 08 6;11(8):2158-64. Epub 2016 Jun 6.

Center for Advanced Biotechnology and Medicine (CABM), Department of Chemistry and Chemical Biology, Rutgers University , Piscataway, New Jersey, United States.

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http://pubs.acs.org/doi/10.1021/acschembio.6b00187
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http://dx.doi.org/10.1021/acschembio.6b00187DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4992415PMC
August 2016

N-substituted pyrrole-based scaffolds as potential anticancer and antiviral lead structures.

Med Chem 2015 ;11(6):602-8

Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece..

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https://lirias.kuleuven.be/bitstream/123456789/503991/1/Pegk
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http://dx.doi.org/10.2174/1573406411666150313161225DOI Listing
May 2016

Tumour-specific cytotoxicity and structure-activity relationships of novel 1-[3-(2-methoxyethylthio)propionyl]-3,5-bis(benzylidene)-4-piperidones.

Bioorg Med Chem 2016 05 30;24(10):2206-14. Epub 2016 Mar 30.

Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan S7N 5C9, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2016.03.056DOI Listing
May 2016

Exploring the purine core of 3'-C-ethynyladenosine (EAdo) in search of novel nucleoside therapeutics.

Bioorg Med Chem Lett 2016 Apr 3;26(8):1970-2. Epub 2016 Mar 3.

Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.03.005DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7126545PMC
April 2016

Membrane-permeable Triphosphate Prodrugs of Nucleoside Analogues.

Angew Chem Int Ed Engl 2016 Apr 23;55(17):5255-8. Epub 2016 Mar 23.

Organic Chemistry, Department of Chemistry, Faculty of Sciences, University of Hamburg, Martin-Luther-King-Platz 6, 20146, Hamburg, Germany.

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http://dx.doi.org/10.1002/anie.201511808DOI Listing
April 2016

Design, Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones.

Molecules 2016 Apr 30;21(5). Epub 2016 Apr 30.

KU Leuven-University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven B-3000, Belgium.

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http://dx.doi.org/10.3390/molecules21050579DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273944PMC
April 2016

NICTABA and UDA, two GlcNAc-binding lectins with unique antiviral activity profiles.

J Antimicrob Chemother 2015 19;70(6):1674-85. Epub 2015 Feb 19.

Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, 3000 Leuven, Belgium

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http://dx.doi.org/10.1093/jac/dkv034DOI Listing
February 2016

Photochemical studies and nanomolar photodynamic activities of phthalocyanines functionalized with 1,4,7-trioxanonyl moieties at their non-peripheral positions.

J Inorg Biochem 2016 Feb 14;155:76-81. Epub 2015 Nov 14.

Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.jinorgbio.2015.11.006DOI Listing
February 2016

Exploring the role of the α-carboxyphosphonate moiety in the HIV-RT activity of α-carboxy nucleoside phosphonates.

Org Biomol Chem 2016 Feb;14(8):2454-65

Department of Chemistry, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre, University College, Cork, Ireland. and School of Pharmacy, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre, University College, Cork, Ireland.

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http://dx.doi.org/10.1039/c5ob02507aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4755898PMC
February 2016

3,5-Bis(3-alkylaminomethyl-4-hydroxybenzylidene)-4-piperidones: A Novel Class of Potent Tumor-Selective Cytotoxins.

J Med Chem 2016 Jan 7;59(2):763-9. Epub 2016 Jan 7.

Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan , Saskatoon, Saskatchewan S7H 5C9, Canada.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01706DOI Listing
January 2016

Dipeptidyl-peptidase IV (DPP IV/CD26)-activated prodrugs: a successful strategy for improving water solubility and oral bioavailability.

Curr Med Chem 2015 ;22(8):1041-54

Institute of Medicinal Chemistry (IQM-CSIC), Juan de la Cierva 3, E-28006 Madrid, Spain.

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http://dx.doi.org/10.2174/0929867322666150114163449DOI Listing
November 2015

Conservation of antiviral activity and improved selectivity in PMEO-DAPym upon pyrimidine to triazine scaffold hopping.

Antiviral Res 2015 Oct 11;122:64-8. Epub 2015 Aug 11.

Instituto de Química Médica (IQM-CSIC), Juan de la Cierva 3, E-28006 Madrid, Spain. Electronic address:

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http://dx.doi.org/10.1016/j.antiviral.2015.08.006DOI Listing
October 2015

Synthesis of Novel Nucleoside Analogues Built on a Bicyclo[4.1.0]heptane Scaffold.

J Org Chem 2015 Oct;80(19):9495-505

Departament de Quı́mica, Universitat Autònoma de Barcelona , 08193 Bellaterra, Spain.

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http://dx.doi.org/10.1021/acs.joc.5b01413DOI Listing
October 2015

A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.

Bioorg Med Chem 2015 Oct 11;23(20):6587-93. Epub 2015 Sep 11.

KU Leuven, Department of Microbiology and Immunology, Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, B-3000 Leuven, Belgium.

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http://dx.doi.org/10.1016/j.bmc.2015.09.020DOI Listing
October 2015

Pronounced Inhibition Shift from HIV Reverse Transcriptase to Herpetic DNA Polymerases by Increasing the Flexibility of α-Carboxy Nucleoside Phosphonates.

J Med Chem 2015 Oct 9;58(20):8110-27. Epub 2015 Oct 9.

Department of Medical Microbiology and Immunology, University of Alberta , 6-020 Katz Group Centre, Edmonton, Alberta T6G 2E1, Canada.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01180DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4893804PMC
October 2015

Lipophilic prodrugs of nucleoside triphosphates as biochemical probes and potential antivirals.

Nat Commun 2015 Oct 27;6:8716. Epub 2015 Oct 27.

Institute of Organic Chemistry, Department of Chemistry, Faculty of Sciences, University of Hamburg, Martin-Luther-King-Platz 6, D-20146 Hamburg, Germany.

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http://dx.doi.org/10.1038/ncomms9716DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4640093PMC
October 2015

Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids.

Eur J Med Chem 2015 Aug 12;101:52-62. Epub 2015 Jun 12.

Department of Chemistry, UGC-Centre of Advance Study-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.06.024DOI Listing
August 2015

Antiproliferative activities of halogenated pyrrolo[3,2-d]pyrimidines.

Bioorg Med Chem 2015 Aug 16;23(15):4354-63. Epub 2015 Jun 16.

Department of Chemistry and Biochemistry, University of Maryland Baltimore County, 1000 Hilltop Circle, Baltimore, MD 21250, USA. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.06.025DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5661880PMC
August 2015

Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides.

J Med Chem 2015 Aug 22;58(15):6114-30. Epub 2015 Jul 22.

†Organic Chemistry, Department of Chemistry, Faculty of Sciences, University of Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg, Germany.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00737DOI Listing
August 2015

Design, synthesis and antiproliferative activity of novel heterobivalent hybrids based on imidazo[2,1-b][1,3,4]thiadiazole and imidazo[2,1-b][1,3]thiazole scaffolds.

Eur J Med Chem 2015 Aug 25;101:205-17. Epub 2015 Jun 25.

Department of Biochemistry, University of Las Palmas de Gran Canaria, Plaza Dr. Pasteur s/n, 35016 Las Palmas de Gran Canaria, Spain.

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http://dx.doi.org/10.1016/j.ejmech.2015.06.042DOI Listing
August 2015

Mycoplasma hyorhinis-encoded cytidine deaminase efficiently inactivates cytosine-based anticancer drugs.

FEBS Open Bio 2015 3;5:634-9. Epub 2015 Aug 3.

Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, blok x - bus 1030, B-3000 Leuven, Belgium.

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http://dx.doi.org/10.1016/j.fob.2015.07.007DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4541722PMC
August 2015

Photosensitizers mediated photodynamic inactivation against virus particles.

Mini Rev Med Chem 2015 ;15(6):503-21

Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium.

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http://dx.doi.org/10.2174/1389557515666150415151505DOI Listing
July 2015

Antiviral Activity of Synthetic Aminopyrrolic Carbohydrate Binding Agents: Targeting the Glycans of Viral gp120 to Inhibit HIV Entry.

Chemistry 2015 Jul 1;21(28):10089-93. Epub 2015 Jun 1.

Istituto di Metodologie Chimiche (IMC), Consiglio Nazionale delle Ricerche (CNR), Dipartimento di Chimica, Polo Scientifico e Tecnologico, 50019 Sesto Fiorentino, Firenze (Italy).

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http://dx.doi.org/10.1002/chem.201501030DOI Listing
July 2015

Bis(benzoyloxybenzyl)-DiPPro nucleoside diphosphates of anti-HIV active nucleoside analogues.

ChemMedChem 2015 May 2;10(5):891-900. Epub 2015 Apr 2.

Organic Chemistry, Department of Chemistry, Faculty of Sciences, University of Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg (Germany); German Center of Infection Research (DZIF).

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http://dx.doi.org/10.1002/cmdc.201500063DOI Listing
May 2015

Design and synthesis of α-carboxy nucleoside phosphonate analogues and evaluation as HIV-1 reverse transcriptase-targeting agents.

J Org Chem 2015 Mar 9;80(5):2479-93. Epub 2015 Jan 9.

Department of Chemistry, Analytical and Biological Chemistry Research Facility, Synthesis and Solid State Pharmaceutical Centre, University College , Cork, Ireland.

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http://dx.doi.org/10.1021/jo502549yDOI Listing
March 2015

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.

Eur J Med Chem 2015 Mar 22;92:754-65. Epub 2015 Jan 22.

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Ji'nan, Shandong, PR China. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.01.042DOI Listing
March 2015

Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.

Bioorg Med Chem 2015 Mar 8;23(5):1069-81. Epub 2015 Jan 8.

Department of Pharmaceutical & Toxicological Chemistry, Volgograd State Medical University, Pavshikh Bortsov Sq., 1, Volgograd 400131, Russia.

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http://dx.doi.org/10.1016/j.bmc.2015.01.002DOI Listing
March 2015

Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity.

Bioorg Med Chem Lett 2015 Mar 30;25(6):1232-5. Epub 2015 Jan 30.

Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology & Science, Pilani 333031, India. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2015.01.058DOI Listing
March 2015

Alpha-carboxy nucleoside phosphonates as universal nucleoside triphosphate mimics.

Proc Natl Acad Sci U S A 2015 Mar 2;112(11):3475-80. Epub 2015 Mar 2.

Center for Advanced Biotechnology and Medicine and Department of Chemistry and Chemical Biology, Rutgers University, Piscataway, NJ 08854-8020;

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http://dx.doi.org/10.1073/pnas.1420233112DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4371953PMC
March 2015

Exposure of Trypanosoma brucei to an N-acetylglucosamine-binding lectin induces VSG switching and glycosylation defects resulting in reduced infectivity.

PLoS Negl Trop Dis 2015 Mar 6;9(3):e0003612. Epub 2015 Mar 6.

Instituto de Parasitología y Biomedicina "López-Neyra", Consejo Superior de Investigaciones Científicas, Parque Tecnológico de Ciencias de la Salud, Granada, Spain.

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http://dx.doi.org/10.1371/journal.pntd.0003612DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4351956PMC
March 2015

Novel 5-arylcarbamoyl-2-methylisoxazolidin-3-yl-3-phosphonates as nucleotide analogues.

Nucleosides Nucleotides Nucleic Acids 2014 ;33(8):552-82

a Bioorganic Chemistry Laboratory, Faculty of Pharmacy , Medical University of Łódź , Łódź , Muszyńskiego , Poland.

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http://dx.doi.org/10.1080/15257770.2014.909046DOI Listing
February 2015

Design, synthesis, and biological evaluation of unconventional aminopyrimidine, aminopurine, and amino-1,3,5-triazine methyloxynucleosides.

ChemMedChem 2015 Feb 24;10(2):321-35. Epub 2014 Nov 24.

Instituto de Química Médica (IQM-CSIC), Juan de la Cierva 3, 28006 Madrid (Spain).

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http://dx.doi.org/10.1002/cmdc.201402465DOI Listing
February 2015

Investigation of fatty acid conjugates of 3,5-bisarylmethylene-4-piperidone derivatives as antitumor agents and human topoisomerase-IIα inhibitors.

Bioorg Med Chem 2015 Feb 26;23(3):411-21. Epub 2014 Dec 26.

Department of Chemistry, Acadia University, Wolfville, Nova Scotia B4P 2R6, Canada. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2014.12.042DOI Listing
February 2015

Synthesis and biological evaluation of phosphoramidate prodrugs of two analogues of 2-deoxy-d-ribose-1-phosphate directed to the discovery of two carbasugars as new potential anti-HIV leads.

Bioorg Med Chem 2015 Feb 25;23(4):829-38. Epub 2014 Dec 25.

School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Cardiff, King Edward VII Avenue, Cardiff CF10 3NB, UK. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2014.12.039DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127161PMC
February 2015

Nucleoside mono- and diphosphate prodrugs of 2',3'-dideoxyuridine and 2',3'-dideoxy-2',3'-didehydrouridine.

ChemMedChem 2015 Jan 10;10(1):94-106. Epub 2014 Sep 10.

Organic Chemistry, Department of Chemistry, Faculty of Sciences, University of Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg (Germany).

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http://dx.doi.org/10.1002/cmdc.201402295DOI Listing
January 2015

Norbornane-based nucleoside and nucleotide analogues locked in North conformation.

Bioorg Med Chem 2015 Jan 15;23(1):184-91. Epub 2014 Nov 15.

Gilead Sciences & IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., 166 10 Prague 6, Czech Republic.

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http://dx.doi.org/10.1016/j.bmc.2014.11.011DOI Listing
January 2015

Hairpin oligonucleotides forming G-quadruplexes: new aptamers with anti-HIV activity.

Eur J Med Chem 2015 Jan 14;89:51-8. Epub 2014 Oct 14.

Department of Chemical Sciences, University of Napoli 'Federico II', Via Cintia 4, I-80126 Napoli, Italy. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.10.030DOI Listing
January 2015

Design, synthesis, and biological evaluation of novel 2H-pyran-2-one derivatives as potential HIV-1 reverse transcriptase inhibitors.

Arch Pharm (Weinheim) 2015 Jan 19;348(1):23-33. Epub 2014 Dec 19.

Dipartimento di Fisica, Università degli studi di Trento, Povo, Trento, Italy.

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http://doi.wiley.com/10.1002/ardp.201400235
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January 2015

Structure-activity relationship of tumor-selective 5-substituted 2-amino-3-carboxymethylthiophene derivatives.

ChemMedChem 2014 Dec 18;9(12):2744-53. Epub 2014 Sep 18.

Department of Chemistry, KU Leuven, 3001Heverlee (Belgium).

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http://dx.doi.org/10.1002/cmdc.201402274DOI Listing
December 2014

The role of N-glycans of HIV-1 gp41 in virus infectivity and susceptibility to the suppressive effects of carbohydrate-binding agents.

Retrovirology 2014 Dec 11;11:107. Epub 2014 Dec 11.

Rega Institute for Medical Research, KU Leuven, Minderbroedersstraat 10, B-3000, Leuven, Belgium.

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http://dx.doi.org/10.1186/s12977-014-0107-7DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4269863PMC
December 2014

Discovery of a nanomolar inhibitor of lung adenocarcinoma in vitro.

Bioorg Med Chem Lett 2014 Nov 3;24(21):5107-10. Epub 2014 Sep 3.

Department of Chemistry and Biochemistry, Brigham Young University, Provo, UT 84602, United States.

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http://dx.doi.org/10.1016/j.bmcl.2014.08.044DOI Listing
November 2014

All trans 1-(3-arylacryloyl)-3,5-bis(pyridin-4-ylmethylene)piperidin-4-ones as curcumin-inspired antineoplastics.

Eur J Med Chem 2014 Nov 30;87:461-70. Epub 2014 Sep 30.

Department of Chemistry, Acadia University, Wolfville, Nova Scotia, Canada B4P 2R6. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.09.090DOI Listing
November 2014

Design and synthesis of a new series of cyclopropylamino-linking diarylpyrimidines as HIV non-nucleoside reverse transcriptase inhibitors.

Eur J Pharm Sci 2014 Oct 20;62:334-41. Epub 2014 Jun 20.

Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium.

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http://dx.doi.org/10.1016/j.ejps.2014.06.003DOI Listing
October 2014

Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.

Bioorg Med Chem 2014 Oct 7;22(19):5290-7. Epub 2014 Aug 7.

Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012 Jinan, Shandong, PR China. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2014.08.001DOI Listing
October 2014

Discovery and SAR studies of a novel class of cytotoxic 1,4-disubstituted piperidines via Ugi reaction.

Eur J Med Chem 2014 Aug 13;83:174-89. Epub 2014 Jun 13.

Instituto de Química Médica (C.S.I.C.), Juan de la Cierva 3, E-28006 Madrid, Spain. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S02235234140054
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http://dx.doi.org/10.1016/j.ejmech.2014.06.026DOI Listing
August 2014