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Items: 1 to 50 of 1213

1.

2-Amino-3-methylcarboxy-5-heptyl-thiophene (TJ191) is a selective anti-cancer small molecule that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells.

El-Gazzar A, Noppen S, Thomas J, Dehaen W, Balzarini J, Liekens S.

Oncotarget. 2017 Dec 15;9(5):6259-6269. doi: 10.18632/oncotarget.23501. eCollection 2018 Jan 19.

2.

2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition.

Romagnoli R, Kimatrai Salvador M, Schiaffino Ortega S, Baraldi PG, Oliva P, Baraldi S, Lopez-Cara LC, Brancale A, Ferla S, Hamel E, Balzarini J, Liekens S, Mattiuzzo E, Basso G, Viola G.

Eur J Med Chem. 2018 Jan 1;143:683-698. doi: 10.1016/j.ejmech.2017.11.096.

PMID:
29220790
3.

Surface Glycans: A Therapeutic Opportunity for Kinetoplastid Diseases: (Trends in Parasitology 2017).

Castillo-Acosta VM, Balzarini J, González-Pacanowska D.

Trends Parasitol. 2017 Dec;33(12):1003-1004. doi: 10.1016/j.pt.2017.09.005. Epub 2017 Oct 16. No abstract available.

PMID:
29050882
4.

Virtual Screening of Acyclovir Derivatives as Potential Antiviral Agents: Design, Synthesis, and Biological Evaluation of New Acyclic Nucleoside ProTides.

Derudas M, Vanpouille C, Carta D, Zicari S, Andrei G, Snoeck R, Brancale A, Margolis L, Balzarini J, McGuigan C.

J Med Chem. 2017 Sep 28;60(18):7876-7896. doi: 10.1021/acs.jmedchem.7b01009. Epub 2017 Sep 19.

5.

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

Mehellou Y, Rattan HS, Balzarini J.

J Med Chem. 2018 Mar 22;61(6):2211-2226. doi: 10.1021/acs.jmedchem.7b00734. Epub 2017 Aug 24.

PMID:
28792763
6.

Surface Glycans: A Therapeutic Opportunity for Kinetoplastid Diseases.

Castillo-Acosta VM, Balzarini J, González-Pacanowska D.

Trends Parasitol. 2017 Oct;33(10):775-787. doi: 10.1016/j.pt.2017.06.009. Epub 2017 Jul 28. Review. Erratum in: Trends Parasitol. 2017 Dec;33(12 ):1003-1004.

PMID:
28760415
7.

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

Krečmerová M, Dračínský M, Snoeck R, Balzarini J, Pomeisl K, Andrei G.

Bioorg Med Chem. 2017 Sep 1;25(17):4637-4648. doi: 10.1016/j.bmc.2017.06.046. Epub 2017 Jul 6.

PMID:
28757102
8.

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

Thomas J, Jana S, Sonawane M, Fiey B, Balzarini J, Liekens S, Dehaen W.

Org Biomol Chem. 2017 May 10;15(18):3892-3900. doi: 10.1039/c7ob00707h.

PMID:
28443928
9.

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

Djuidje EN, Dissette V, Bino A, Benetti S, Balzarini J, Liekens S, Manfredini S, Vertuani S, Baldisserotto A.

ChemMedChem. 2017 May 22;12(10):760-769. doi: 10.1002/cmdc.201700137. Epub 2017 May 3.

PMID:
28417557
10.

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.

Balzarini J, Menni M, Das K, van Berckelaer L, Ford A, Maguire NM, Liekens S, Boehmer PE, Arnold E, Götte M, Maguire AR.

Biochem Pharmacol. 2017 Jul 15;136:51-61. doi: 10.1016/j.bcp.2017.04.001. Epub 2017 Apr 6.

11.

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

Thomas J, Jecic A, Vanstreels E, van Berckelaer L, Romagnoli R, Dehaen W, Liekens S, Balzarini J.

Eur J Med Chem. 2017 May 26;132:219-235. doi: 10.1016/j.ejmech.2017.03.044. Epub 2017 Mar 23.

12.

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

Panda AK, Das U, Umemura N, Sakagami H, Kawase M, Balzarini J, De Clercq E, Dimmock SG, Roayapalley PK, Dimmock JR.

Bioorg Med Chem Lett. 2017 Apr 1;27(7):1611-1615. doi: 10.1016/j.bmcl.2017.02.016. Epub 2017 Feb 10.

PMID:
28238612
13.
14.
15.

Structure-activity relationship studies on a Trp dendrimer with dual activities against HIV and enterovirus A71. Modifications on the amino acid.

Martínez-Gualda B, Sun L, Rivero-Buceta E, Flores A, Quesada E, Balzarini J, Noppen S, Liekens S, Schols D, Neyts J, Leyssen P, Mirabelli C, Camarasa MJ, San-Félix A.

Antiviral Res. 2017 Mar;139:32-40. doi: 10.1016/j.antiviral.2016.12.010. Epub 2016 Dec 23.

16.

High mannose-specific lectin Msl mediates key interactions of the vaginal Lactobacillus plantarum isolate CMPG5300.

Malik S, Petrova MI, Imholz NC, Verhoeven TL, Noppen S, Van Damme EJ, Liekens S, Balzarini J, Schols D, Vanderleyden J, Lebeer S.

Sci Rep. 2016 Nov 17;6:37339. doi: 10.1038/srep37339.

17.

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

Kandil S, Balzarini J, Rat S, Brancale A, Westwell AD, McGuigan C.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5618-5623. doi: 10.1016/j.bmcl.2016.10.077. Epub 2016 Oct 27.

18.

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

Das K, Balzarini J, Miller MT, Maguire AR, DeStefano JJ, Arnold E.

ACS Chem Biol. 2016 Nov 18;11(11):3226. Epub 2016 Sep 26. No abstract available.

PMID:
27696816
19.

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

Castillo-Acosta VM, Ruiz-Pérez LM, Etxebarria J, Reichardt NC, Navarro M, Igarashi Y, Liekens S, Balzarini J, González-Pacanowska D.

PLoS Pathog. 2016 Sep 23;12(9):e1005851. doi: 10.1371/journal.ppat.1005851. eCollection 2016 Sep.

20.

Identification of an indol-based derivative as potent and selective varicella zoster virus (VZV) inhibitor.

Musella S, di Sarno V, Ciaglia T, Sala M, Spensiero A, Scala MC, Ostacolo C, Andrei G, Balzarini J, Snoeck R, Novellino E, Campiglia P, Bertamino A, Gomez-Monterrey IM.

Eur J Med Chem. 2016 Nov 29;124:773-781. doi: 10.1016/j.ejmech.2016.09.014. Epub 2016 Sep 7.

PMID:
27639368
21.

Lectin-Like Molecules of Lactobacillus rhamnosus GG Inhibit Pathogenic Escherichia coli and Salmonella Biofilm Formation.

Petrova MI, Imholz NC, Verhoeven TL, Balzarini J, Van Damme EJ, Schols D, Vanderleyden J, Lebeer S.

PLoS One. 2016 Aug 18;11(8):e0161337. doi: 10.1371/journal.pone.0161337. eCollection 2016.

22.

Niacin esters of chalcones with tumor-selective properties.

Panda AK, Das U, Roayapalley PK, Sakagami H, Kawase M, Balzarini J, De Clercq E, Dimmock JR.

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1451-6. doi: 10.3109/14756366.2016.1144595. Epub 2016 Jun 2.

PMID:
27251045
23.

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

Das K, Balzarini J, Miller MT, Maguire AR, DeStefano JJ, Arnold E.

ACS Chem Biol. 2016 Aug 19;11(8):2158-64. doi: 10.1021/acschembio.6b00187. Epub 2016 Jun 6. Erratum in: ACS Chem Biol. 2016 Nov 18;11(11):3226.

24.

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

Onnis V, Demurtas M, Deplano A, Balboni G, Baldisserotto A, Manfredini S, Pacifico S, Liekens S, Balzarini J.

Molecules. 2016 Apr 30;21(5). pii: E579. doi: 10.3390/molecules21050579.

25.

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

Hossain M, Das U, Umemura N, Sakagami H, Balzarini J, De Clercq E, Kawase M, Dimmock JR.

Bioorg Med Chem. 2016 May 15;24(10):2206-14. doi: 10.1016/j.bmc.2016.03.056. Epub 2016 Mar 30.

PMID:
27073056
26.

Membrane-permeable Triphosphate Prodrugs of Nucleoside Analogues.

Gollnest T, Dinis de Oliveira T, Rath A, Hauber I, Schols D, Balzarini J, Meier C.

Angew Chem Int Ed Engl. 2016 Apr 18;55(17):5255-8. doi: 10.1002/anie.201511808. Epub 2016 Mar 23.

PMID:
27008042
27.

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

Hulpia F, Balzarini J, Schols D, Andrei G, Snoeck R, Van Calenbergh S.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1970-2. doi: 10.1016/j.bmcl.2016.03.005. Epub 2016 Mar 3.

PMID:
26965865
28.

Resistance to the nucleotide analogue cidofovir in HPV(+) cells: a multifactorial process involving UMP/CMP kinase 1.

Topalis D, Nogueira TC, De Schutter T, El Amri C, Krečmerová M, Naesens L, Balzarini J, Andrei G, Snoeck R.

Oncotarget. 2016 Mar 1;7(9):10386-401. doi: 10.18632/oncotarget.7006.

29.

The Cellular Thioredoxin-1/Thioredoxin Reductase-1 Driven Oxidoreduction Represents a Chemotherapeutic Target for HIV-1 Entry Inhibition.

Reiser K, Mathys L, Curbo S, Pannecouque C, Noppen S, Liekens S, Engman L, Lundberg M, Balzarini J, Karlsson A.

PLoS One. 2016 Jan 27;11(1):e0147773. doi: 10.1371/journal.pone.0147773. eCollection 2016.

30.

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

Mullins ND, Maguire NM, Ford A, Das K, Arnold E, Balzarini J, Maguire AR.

Org Biomol Chem. 2016 Feb 28;14(8):2454-65. doi: 10.1039/c5ob02507a.

31.

Screening Platform toward New Anti-HIV Aptamers Set on Molecular Docking and Fluorescence Quenching Techniques.

Oliviero G, Stornaiuolo M, D'Atri V, Nici F, Yousif AM, D'Errico S, Piccialli G, Mayol L, Novellino E, Marinelli L, Grieco P, Carotenuto A, Noppen S, Liekens S, Balzarini J, Borbone N.

Anal Chem. 2016 Feb 16;88(4):2327-34. doi: 10.1021/acs.analchem.5b04268. Epub 2016 Feb 5.

PMID:
26810800
32.

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

Karki SS, Das U, Umemura N, Sakagami H, Iwamoto S, Kawase M, Balzarini J, De Clercq E, Dimmock SG, Dimmock JR.

J Med Chem. 2016 Jan 28;59(2):763-9. doi: 10.1021/acs.jmedchem.5b01706. Epub 2016 Jan 7.

PMID:
26727215
33.

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

Sobotta L, Wierzchowski M, Mierzwicki M, Gdaniec Z, Mielcarek J, Persoons L, Goslinski T, Balzarini J.

J Inorg Biochem. 2016 Feb;155:76-81. doi: 10.1016/j.jinorgbio.2015.11.006. Epub 2015 Nov 14.

PMID:
26638008
34.

Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD(+)/NADH Ratio and SIRT1.

Tikhomirov AS, Shchekotikhin AE, Lee YH, Chen YA, Yeh CA, Tatarskiy VV Jr, Dezhenkova LG, Glazunova VA, Balzarini J, Shtil AA, Preobrazhenskaya MN, Chueh PJ.

J Med Chem. 2015 Dec 24;58(24):9522-34. doi: 10.1021/acs.jmedchem.5b00859. Epub 2015 Dec 15.

PMID:
26633734
35.

Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers.

Rivero-Buceta E, Carrero P, Casanova E, Doyagüez EG, Madrona A, Quesada E, Peréz-Pérez MJ, Mateos R, Bravo L, Mathys L, Noppen S, Kiselev E, Marchand C, Pommier Y, Liekens S, Balzarini J, Camarasa MJ, San-Félix A.

Eur J Med Chem. 2015 Dec 1;106:132-43. doi: 10.1016/j.ejmech.2015.10.027. Epub 2015 Oct 21.

PMID:
26540494
36.

Tryptophan dendrimers that inhibit HIV replication, prevent virus entry and bind to the HIV envelope glycoproteins gp120 and gp41.

Rivero-Buceta E, Doyagüez EG, Colomer I, Quesada E, Mathys L, Noppen S, Liekens S, Camarasa MJ, Pérez-Pérez MJ, Balzarini J, San-Félix A.

Eur J Med Chem. 2015 Dec 1;106:34-43. doi: 10.1016/j.ejmech.2015.10.031. Epub 2015 Oct 21.

PMID:
26513643
37.

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

Gollnest T, de Oliveira TD, Schols D, Balzarini J, Meier C.

Nat Commun. 2015 Oct 27;6:8716. doi: 10.1038/ncomms9716.

38.

Curcumin-inspired cytotoxic 3,5-bis(arylmethylene)-1-(N-(ortho-substituted aryl)maleamoyl)-4-piperidones: A novel group of topoisomerase II alpha inhibitors.

Jha A, Duffield KM, Ness MR, Ravoori S, Andrews G, Bhullar KS, Rupasinghe HP, Balzarini J.

Bioorg Med Chem. 2015 Oct 1;23(19):6404-17. doi: 10.1016/j.bmc.2015.08.023. Epub 2015 Aug 20.

PMID:
26456623
39.

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

John J, Kim Y, Bennett N, Das K, Liekens S, Naesens L, Arnold E, Maguire AR, Götte M, Dehaen W, Balzarini J.

J Med Chem. 2015 Oct 22;58(20):8110-27. doi: 10.1021/acs.jmedchem.5b01180. Epub 2015 Oct 9.

40.

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

Gu SX, Qiao H, Zhu YY, Shu QC, Liu H, Ju XL, De Clercq E, Balzarini J, Pannecouque C.

Bioorg Med Chem. 2015 Oct 15;23(20):6587-93. doi: 10.1016/j.bmc.2015.09.020. Epub 2015 Sep 11.

PMID:
26385446
41.

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

Domínguez-Pérez B, Ferrer É, Figueredo M, Maréchal JD, Balzarini J, Alibés R, Busqué F.

J Org Chem. 2015 Oct 2;80(19):9495-505. doi: 10.1021/acs.joc.5b01413.

PMID:
26376319
42.

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

Vande Voorde J, Vervaeke P, Liekens S, Balzarini J.

FEBS Open Bio. 2015 Aug 3;5:634-9. doi: 10.1016/j.fob.2015.07.007. eCollection 2015.

43.

Rational Development of Nucleoside Diphosphate Prodrugs: DiPPro-Compounds.

Meier C, Jessen HJ, Schulz T, Weinschenk L, Pertenbreiter F, Balzarini J.

Curr Med Chem. 2015;22(34):3933-50. Review.

PMID:
26303175
44.

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

de Castro S, Fernández-Cureses G, Andrei G, Snoeck R, Sánchez-Murcia PA, Korba B, Gago F, Balzarini J, Camarasa MJ.

Antiviral Res. 2015 Oct;122:64-8. doi: 10.1016/j.antiviral.2015.08.006. Epub 2015 Aug 11.

PMID:
26275802
45.

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

Mathys L, Balzarini J.

Expert Opin Ther Targets. 2016;20(1):123-43. doi: 10.1517/14728222.2015.1068760. Epub 2015 Jul 15. Review.

PMID:
26178644
46.

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.

Romagnoli R, Baraldi PG, Prencipe F, Balzarini J, Liekens S, Estévez F.

Eur J Med Chem. 2015 Aug 28;101:205-17. doi: 10.1016/j.ejmech.2015.06.042. Epub 2015 Jun 25.

PMID:
26141911
47.

Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides.

Weinschenk L, Schols D, Balzarini J, Meier C.

J Med Chem. 2015 Aug 13;58(15):6114-30. doi: 10.1021/acs.jmedchem.5b00737. Epub 2015 Jul 22.

PMID:
26125628
48.

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

Temburnikar KW, Ross CR, Wilson GM, Balzarini J, Cawrse BM, Seley-Radtke KL.

Bioorg Med Chem. 2015 Aug 1;23(15):4354-63. doi: 10.1016/j.bmc.2015.06.025. Epub 2015 Jun 16.

49.
50.

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

Kaur H, Balzarini J, de Kock C, Smith PJ, Chibale K, Singh K.

Eur J Med Chem. 2015 Aug 28;101:52-62. doi: 10.1016/j.ejmech.2015.06.024. Epub 2015 Jun 12.

PMID:
26114811

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