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Items: 1 to 50 of 209

1.

Discovery of dihydroxyindole-2-carboxylic acid derivatives as dual allosteric HIV-1 Integrase and Reverse Transcriptase associated Ribonuclease H inhibitors.

Esposito F, Sechi M, Pala N, Sanna A, Koneru PC, Kvaratskhelia M, Naesens L, Corona A, Grandi N, di Santo R, D'Amore VM, Di Leva FS, Novellino E, Cosconati S, Tramontano E.

Antiviral Res. 2019 Dec 5:104671. doi: 10.1016/j.antiviral.2019.104671. [Epub ahead of print]

PMID:
31812637
2.

Superior inhibition of influenza virus hemagglutinin-mediated fusion by indole-substituted spirothiazolidinones.

Cihan-Üstündağ G, Zopun M, Vanderlinden E, Ozkirimli E, Persoons L, Çapan G, Naesens L.

Bioorg Med Chem. 2019 Nov 8:115130. doi: 10.1016/j.bmc.2019.115130. [Epub ahead of print]

PMID:
31753804
3.

Author Correction: A human immune dysregulation syndrome characterized by severe hyperinflammation with a homozygous nonsense Roquin-1 mutation.

Tavernier SJ, Athanasopoulos V, Verloo P, Behrens G, Staal J, Bogaert DJ, Naesens L, De Bruyne M, Van Gassen S, Parthoens E, Ellyard J, Cappello J, Morris LX, Van Gorp H, Van Isterdael G, Saeys Y, Lamkanfi M, Schelstraete P, Dehoorne J, Bordon V, Van Coster R, Lambrecht BN, Menten B, Beyaert R, Vinuesa CG, Heissmeyer V, Dullaers M, Haerynck F.

Nat Commun. 2019 Nov 20;10(1):5337. doi: 10.1038/s41467-019-13379-9.

4.

GATA2 deficiency and haematopoietic stem cell transplantation: challenges for the clinical practitioner.

Bogaert DJ, Laureys G, Naesens L, Mazure D, De Bruyne M, Hsu AP, Bordon V, Wouters E, Tavernier SJ, Lambrecht BN, De Baere E, Haerynck F, Kerre T.

Br J Haematol. 2019 Nov 11. doi: 10.1111/bjh.16247. [Epub ahead of print]

PMID:
31710708
5.

A human immune dysregulation syndrome characterized by severe hyperinflammation with a homozygous nonsense Roquin-1 mutation.

Tavernier SJ, Athanasopoulos V, Verloo P, Behrens G, Staal J, Bogaert DJ, Naesens L, De Bruyne M, Van Gassen S, Parthoens E, Ellyard J, Cappello J, Morris LX, Van Gorp H, Van Isterdael G, Saeys Y, Lamkanfi M, Schelstraete P, Dehoorne J, Bordon V, Van Coster R, Lambrecht BN, Menten B, Beyaert R, Vinuesa CG, Heissmeyer V, Dullaers M, Haerynck F.

Nat Commun. 2019 Oct 21;10(1):4779. doi: 10.1038/s41467-019-12704-6. Erratum in: Nat Commun. 2019 Nov 20;10(1):5337.

6.

Hemagglutinin Cleavability, Acid Stability, and Temperature Dependence Optimize Influenza B Virus for Replication in Human Airways.

Laporte M, Stevaert A, Raeymaekers V, Boogaerts T, Nehlmeier I, Chiu W, Benkheil M, Vanaudenaerde B, Pöhlmann S, Naesens L.

J Virol. 2019 Dec 12;94(1). pii: e01430-19. doi: 10.1128/JVI.01430-19. Print 2019 Dec 12.

PMID:
31597759
7.

Novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives as potent and selective influenza virus fusion inhibitors.

Göktaş F, Özbil M, Cesur N, Vanderlinden E, Naesens L, Cesur Z.

Arch Pharm (Weinheim). 2019 Nov;352(11):e1900028. doi: 10.1002/ardp.201900028. Epub 2019 Sep 18.

PMID:
31531897
8.

Synthesis and anti-coronavirus activity of a series of 1-thia-4-azaspiro[4.5]decan-3-one derivatives.

Apaydın ÇB, Cesur N, Stevaert A, Naesens L, Cesur Z.

Arch Pharm (Weinheim). 2019 Jun;352(6):e1800330. doi: 10.1002/ardp.201800330. Epub 2019 May 9.

PMID:
31073993
9.

Cell line-dependent activation and antiviral activity of T-1105, the non-fluorinated analogue of T-705 (favipiravir).

Huchting J, Vanderlinden E, Van Berwaer R, Meier C, Naesens L.

Antiviral Res. 2019 Jul;167:1-5. doi: 10.1016/j.antiviral.2019.04.002. Epub 2019 Apr 2.

PMID:
30951731
10.

Influenza virus entry via the GM3 ganglioside-mediated platelet-derived growth factor receptor β signalling pathway.

Vrijens P, Noppen S, Boogaerts T, Vanstreels E, Ronca R, Chiodelli P, Laporte M, Vanderlinden E, Liekens S, Stevaert A, Naesens L.

J Gen Virol. 2019 Apr;100(4):583-601. doi: 10.1099/jgv.0.001235. Epub 2019 Feb 14.

PMID:
30762518
11.

Pyrrolidine nucleoside bisphosphonates as antituberculosis agents targeting hypoxanthine-guanine phosphoribosyltransferase.

Eng WS, Rejman D, Pohl R, West NP, Woods K, Naesens LMJ, Keough DT, Guddat LW.

Eur J Med Chem. 2018 Nov 5;159:10-22. doi: 10.1016/j.ejmech.2018.09.039. Epub 2018 Sep 19.

PMID:
30265958
12.

Mediastinal Myeloid Sarcoma with TP53 Mutation Preceding Acute Myeloid Leukemia with a PICALM-MLLT10 Fusion Gene.

Naesens L, Devos H, Nollet F, Michaux L, Selleslag D.

Acta Haematol. 2018;140(2):97-104. doi: 10.1159/000491596. Epub 2018 Sep 18.

PMID:
30227397
13.

Structure-activity relationship studies of lipophilic teicoplanin pseudoaglycon derivatives as new anti-influenza virus agents.

Szűcs Z, Kelemen V, Le Thai S, Csávás M, Rőth E, Batta G, Stevaert A, Vanderlinden E, Naesens L, Herczegh P, Borbás A.

Eur J Med Chem. 2018 Sep 5;157:1017-1030. doi: 10.1016/j.ejmech.2018.08.058. Epub 2018 Aug 22.

PMID:
30170320
14.

Identification of influenza PA-Nter endonuclease inhibitors using pharmacophore- and docking-based virtual screening.

Ferro S, Gitto R, Buemi MR, Karamanou S, Stevaert A, Naesens L, De Luca L.

Bioorg Med Chem. 2018 Aug 15;26(15):4544-4550. doi: 10.1016/j.bmc.2018.07.046. Epub 2018 Jul 27.

PMID:
30082105
15.

Prodrugs of the Phosphoribosylated Forms of Hydroxypyrazinecarboxamide Pseudobase T-705 and Its De-Fluoro Analogue T-1105 as Potent Influenza Virus Inhibitors.

Huchting J, Vanderlinden E, Winkler M, Nasser H, Naesens L, Meier C.

J Med Chem. 2018 Jul 26;61(14):6193-6210. doi: 10.1021/acs.jmedchem.8b00617. Epub 2018 Jul 3.

PMID:
29906392
16.

Synthesis, biological evaluation and molecular modeling of novel azaspiro dihydrotriazines as influenza virus inhibitors targeting the host factor dihydrofolate reductase (DHFR).

Francesconi V, Giovannini L, Santucci M, Cichero E, Costi MP, Naesens L, Giordanetto F, Tonelli M.

Eur J Med Chem. 2018 Jul 15;155:229-243. doi: 10.1016/j.ejmech.2018.05.059. Epub 2018 Jun 2.

PMID:
29886325
17.

Aniline-Based Inhibitors of Influenza H1N1 Virus Acting on Hemagglutinin-Mediated Fusion.

Leiva R, Barniol-Xicota M, Codony S, Ginex T, Vanderlinden E, Montes M, Caffrey M, Luque FJ, Naesens L, Vázquez S.

J Med Chem. 2018 Jan 11;61(1):98-118. doi: 10.1021/acs.jmedchem.7b00908. Epub 2017 Dec 22.

PMID:
29220568
18.

Antiviral activity and metal ion-binding properties of some 2-hydroxy-3-methoxyphenyl acylhydrazones.

Carcelli M, Fisicaro E, Compari C, Contardi L, Rogolino D, Solinas C, Stevaert A, Naesens L.

Biometals. 2018 Feb;31(1):81-89. doi: 10.1007/s10534-017-0070-6. Epub 2017 Dec 5.

PMID:
29209895
19.

Amino acid and peptide prodrugs of diphenylpropanones positive allosteric modulators of α7 nicotinic receptors with analgesic activity.

Balsera B, Mulet J, Sala S, Sala F, de la Torre-Martínez R, González-Rodríguez S, Plata A, Naesens L, Fernández-Carvajal A, Ferrer-Montiel A, Criado M, Pérez de Vega MJ, González-Muñiz R.

Eur J Med Chem. 2018 Jan 1;143:157-165. doi: 10.1016/j.ejmech.2017.10.083. Epub 2017 Nov 2.

PMID:
29174812
20.

Design of Plasmodium vivax Hypoxanthine-Guanine Phosphoribosyltransferase Inhibitors as Potential Antimalarial Therapeutics.

Keough DT, Rejman D, Pohl R, Zborníková E, Hocková D, Croll T, Edstein MD, Birrell GW, Chavchich M, Naesens LMJ, Pierens GK, Brereton IM, Guddat LW.

ACS Chem Biol. 2018 Jan 19;13(1):82-90. doi: 10.1021/acschembio.7b00916. Epub 2017 Dec 5.

PMID:
29161011
21.

Synthesis and Evaluation of Asymmetric Acyclic Nucleoside Bisphosphonates as Inhibitors of Plasmodium falciparum and Human Hypoxanthine-Guanine-(Xanthine) Phosphoribosyltransferase.

Špaček P, Keough DT, Chavchich M, Dračínský M, Janeba Z, Naesens L, Edstein MD, Guddat LW, Hocková D.

J Med Chem. 2017 Sep 14;60(17):7539-7554. doi: 10.1021/acs.jmedchem.7b00926. Epub 2017 Aug 30.

PMID:
28813147
22.

Editorial overview: Antiviral strategies: Antiviral drug design: creating new ideas against old and new bugs.

Naesens L, Zoulim F.

Curr Opin Virol. 2017 Jun;24:v-vii. doi: 10.1016/j.coviro.2017.07.007. No abstract available.

PMID:
28743435
23.

Synthesis and evaluation of symmetric acyclic nucleoside bisphosphonates as inhibitors of the Plasmodium falciparum, Plasmodium vivax and human 6-oxopurine phosphoribosyltransferases and the antimalarial activity of their prodrugs.

Špaček P, Keough DT, Chavchich M, Dračínský M, Janeba Z, Naesens L, Edstein MD, Guddat LW, Hocková D.

Bioorg Med Chem. 2017 Aug 1;25(15):4008-4030. doi: 10.1016/j.bmc.2017.05.048. Epub 2017 May 24.

PMID:
28601510
24.

Host dihydrofolate reductase (DHFR)-directed cycloguanil analogues endowed with activity against influenza virus and respiratory syncytial virus.

Tonelli M, Naesens L, Gazzarrini S, Santucci M, Cichero E, Tasso B, Moroni A, Costi MP, Loddo R.

Eur J Med Chem. 2017 Jul 28;135:467-478. doi: 10.1016/j.ejmech.2017.04.070. Epub 2017 Apr 27.

PMID:
28477572
25.

Slow but Steady Wins the Race: Dissimilarities among New Dual Inhibitors of the Wild-Type and the V27A Mutant M2 Channels of Influenza A Virus.

Barniol-Xicota M, Gazzarrini S, Torres E, Hu Y, Wang J, Naesens L, Moroni A, Vázquez S.

J Med Chem. 2017 May 11;60(9):3727-3738. doi: 10.1021/acs.jmedchem.6b01758. Epub 2017 Apr 24.

26.

Airway proteases: an emerging drug target for influenza and other respiratory virus infections.

Laporte M, Naesens L.

Curr Opin Virol. 2017 Jun;24:16-24. doi: 10.1016/j.coviro.2017.03.018. Epub 2017 Apr 14. Review.

27.

Chelation Motifs Affecting Metal-dependent Viral Enzymes: N'-acylhydrazone Ligands as Dual Target Inhibitors of HIV-1 Integrase and Reverse Transcriptase Ribonuclease H Domain.

Carcelli M, Rogolino D, Gatti A, Pala N, Corona A, Caredda A, Tramontano E, Pannecouque C, Naesens L, Esposito F.

Front Microbiol. 2017 Mar 20;8:440. doi: 10.3389/fmicb.2017.00440. eCollection 2017.

28.

Diclofenac-Based Hydrazones and Spirothiazolidinones: Synthesis, Characterization, and Antimicrobial Properties.

Kocabalkanlı A, Cihan-Üstündağ G, Naesens L, Mataracı-Kara E, Nassozi M, Çapan G.

Arch Pharm (Weinheim). 2017 May;350(5). doi: 10.1002/ardp.201700010. Epub 2017 Mar 30.

PMID:
28370198
29.

Synthesis and in vitro antiviral evaluation of 4-substituted 3,4-dihydropyrimidinones.

Kumarasamy D, Roy BG, Rocha-Pereira J, Neyts J, Nanjappan S, Maity S, Mookerjee M, Naesens L.

Bioorg Med Chem Lett. 2017 Jan 15;27(2):139-142. doi: 10.1016/j.bmcl.2016.12.010. Epub 2016 Dec 5.

PMID:
27979594
30.

Crystal structures and inhibition of Trypanosoma brucei hypoxanthine-guanine phosphoribosyltransferase.

Terán D, Hocková D, Česnek M, Zíková A, Naesens L, Keough DT, Guddat LW.

Sci Rep. 2016 Oct 27;6:35894. doi: 10.1038/srep35894.

31.

First discovery of novel 3-hydroxy-quinazoline-2,4(1H,3H)-diones as specific anti-vaccinia and adenovirus agents via 'privileged scaffold' refining approach.

Kang D, Zhang H, Zhou Z, Huang B, Naesens L, Zhan P, Liu X.

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5182-5186. doi: 10.1016/j.bmcl.2016.09.071. Epub 2016 Sep 29.

PMID:
27742238
32.

Antiviral therapies on the horizon for influenza.

Naesens L, Stevaert A, Vanderlinden E.

Curr Opin Pharmacol. 2016 Oct;30:106-115. doi: 10.1016/j.coph.2016.08.003. Epub 2016 Aug 26. Review.

33.

The Influenza Virus Polymerase Complex: An Update on Its Structure, Functions, and Significance for Antiviral Drug Design.

Stevaert A, Naesens L.

Med Res Rev. 2016 Nov;36(6):1127-1173. doi: 10.1002/med.21401. Epub 2016 Aug 29. Review.

34.

Distinct Effects of T-705 (Favipiravir) and Ribavirin on Influenza Virus Replication and Viral RNA Synthesis.

Vanderlinden E, Vrancken B, Van Houdt J, Rajwanshi VK, Gillemot S, Andrei G, Lemey P, Naesens L.

Antimicrob Agents Chemother. 2016 Oct 21;60(11):6679-6691. doi: 10.1128/AAC.01156-16. Print 2016 Nov.

35.

Inhibitory Effect of 2,3,5,6-Tetrafluoro-4-[4-(aryl)-1H-1,2,3-triazol-1-yl]benzenesulfonamide Derivatives on HIV Reverse Transcriptase Associated RNase H Activities.

Pala N, Esposito F, Rogolino D, Carcelli M, Sanna V, Palomba M, Naesens L, Corona A, Grandi N, Tramontano E, Sechi M.

Int J Mol Sci. 2016 Aug 20;17(8). pii: E1371. doi: 10.3390/ijms17081371.

36.

N-acylhydrazone inhibitors of influenza virus PA endonuclease with versatile metal binding modes.

Carcelli M, Rogolino D, Gatti A, De Luca L, Sechi M, Kumar G, White SW, Stevaert A, Naesens L.

Sci Rep. 2016 Aug 11;6:31500. doi: 10.1038/srep31500.

37.

Synthesis and biological evaluation of lipophilic teicoplanin pseudoaglycon derivatives containing a substituted triazole function.

Szűcs Z, Csávás M, Rőth E, Borbás A, Batta G, Perret F, Ostorházi E, Szatmári R, Vanderlinden E, Naesens L, Herczegh P.

J Antibiot (Tokyo). 2017 Feb;70(2):152-157. doi: 10.1038/ja.2016.80. Epub 2016 Jun 29.

PMID:
27353163
38.

Cidofovir is active against human papillomavirus positive and negative head and neck and cervical tumor cells by causing DNA damage as one of its working mechanisms.

Mertens B, Nogueira T, Stranska R, Naesens L, Andrei G, Snoeck R.

Oncotarget. 2016 Jul 26;7(30):47302-47318. doi: 10.18632/oncotarget.10100.

39.

1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.

Geisman AN, Valuev-Elliston VT, Ozerov AA, Khandazhinskaya AL, Chizhov AO, Kochetkov SN, Pannecouque C, Naesens L, Seley-Radtke KL, Novikov MS.

Bioorg Med Chem. 2016 Jun 1;24(11):2476-85. doi: 10.1016/j.bmc.2016.04.010. Epub 2016 Apr 5.

PMID:
27112451
40.

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.

41.

Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones.

Cihan-Üstündağ G, Gürsoy E, Naesens L, Ulusoy-Güzeldemirci N, Çapan G.

Bioorg Med Chem. 2016 Jan 15;24(2):240-6. doi: 10.1016/j.bmc.2015.12.008. Epub 2015 Dec 8.

PMID:
26707844
42.

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.

43.

Investigation of the salicylaldehyde thiosemicarbazone scaffold for inhibition of influenza virus PA endonuclease.

Rogolino D, Bacchi A, De Luca L, Rispoli G, Sechi M, Stevaert A, Naesens L, Carcelli M.

J Biol Inorg Chem. 2015 Oct;20(7):1109-21. doi: 10.1007/s00775-015-1292-0. Epub 2015 Sep 1.

PMID:
26323352
44.

Virtual Screening and Biological Validation of Novel Influenza Virus PA Endonuclease Inhibitors.

Pala N, Stevaert A, Dallocchio R, Dessì A, Rogolino D, Carcelli M, Sanna V, Sechi M, Naesens L.

ACS Med Chem Lett. 2015 Jun 18;6(8):866-71. doi: 10.1021/acsmedchemlett.5b00109. eCollection 2015 Aug 13.

45.

Antimalarial activity of prodrugs of N-branched acyclic nucleoside phosphonate inhibitors of 6-oxopurine phosphoribosyltransferases.

Hocková D, Janeba Z, Naesens L, Edstein MD, Chavchich M, Keough DT, Guddat LW.

Bioorg Med Chem. 2015 Sep 1;23(17):5502-10. doi: 10.1016/j.bmc.2015.07.038. Epub 2015 Jul 27.

PMID:
26275679
46.

What kind of prostate cancers do we miss on multiparametric magnetic resonance imaging?

De Visschere PJ, Naesens L, Libbrecht L, Van Praet C, Lumen N, Fonteyne V, Pattyn E, Villeirs G.

Eur Radiol. 2016 Apr;26(4):1098-107. doi: 10.1007/s00330-015-3894-x. Epub 2015 Jul 3.

PMID:
26135002
47.

A versatile salicyl hydrazonic ligand and its metal complexes as antiviral agents.

Rogolino D, Carcelli M, Bacchi A, Compari C, Contardi L, Fisicaro E, Gatti A, Sechi M, Stevaert A, Naesens L.

J Inorg Biochem. 2015 Sep;150:9-17. doi: 10.1016/j.jinorgbio.2015.05.013. Epub 2015 May 27.

PMID:
26047528
48.

Synthesis and Biological Evaluation of N-Alkyl-3-(alkylamino)-pyrazine-2-carboxamides.

Semelkova L, Konecna K, Paterova P, Kubicek V, Kunes J, Novakova L, Marek J, Naesens L, Pesko M, Kralova K, Dolezal M, Zitko J.

Molecules. 2015 May 14;20(5):8687-711. doi: 10.3390/molecules20058687.

49.

First Crystal Structures of Mycobacterium tuberculosis 6-Oxopurine Phosphoribosyltransferase: Complexes with GMP and Pyrophosphate and with Acyclic Nucleoside Phosphonates Whose Prodrugs Have Antituberculosis Activity.

Eng WS, Hocková D, Špaček P, Janeba Z, West NP, Woods K, Naesens LM, Keough DT, Guddat LW.

J Med Chem. 2015 Jun 11;58(11):4822-38. doi: 10.1021/acs.jmedchem.5b00611. Epub 2015 May 13.

PMID:
25915781
50.

New polycyclic dual inhibitors of the wild type and the V27A mutant M2 channel of the influenza A virus with unexpected binding mode.

Rey-Carrizo M, Gazzarrini S, Llabrés S, Frigolé-Vivas M, Juárez-Jiménez J, Font-Bardia M, Naesens L, Moroni A, Luque FJ, Vázquez S.

Eur J Med Chem. 2015;96:318-29. doi: 10.1016/j.ejmech.2015.04.030. Epub 2015 Apr 14.

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