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Items: 1 to 50 of 147

1.

(F)uridylylated Peptides Linked to VPg1 of Foot-and- Mouth Disease Virus (FMDV): Design, Synthesis and X-Ray Crystallography of the Complexes with FMDV RNA-Dependent RNA Polymerase.

de Castro S, Ferrer-Orta C, Mills A, Fernández-Cureses G, Gago F, Verdaguer N, Camarasa MJ.

Molecules. 2019 Jun 26;24(13). pii: E2360. doi: 10.3390/molecules24132360.

2.

Modifications in the branched arms of a class of dual inhibitors of HIV and EV71 replication expand their antiviral spectrum.

Martínez-Gualda B, Sun L, Martí-Marí O, Mirabelli C, Delang L, Neyts J, Schols D, Camarasa MJ, San-Félix A.

Antiviral Res. 2019 Aug;168:210-214. doi: 10.1016/j.antiviral.2019.06.006. Epub 2019 Jun 20.

PMID:
31228490
3.

Pyrrolopyrimidine vs Imidazole-Phenyl-Thiazole Scaffolds in Nonpeptidic Dimerization Inhibitors of Leishmania infantum Trypanothione Reductase.

Revuelto A, Ruiz-Santaquiteria M, de Lucio H, Gamo A, Carriles AA, Gutiérrez KJ, Sánchez-Murcia PA, Hermoso JA, Gago F, Camarasa MJ, Jiménez-Ruiz A, Velázquez S.

ACS Infect Dis. 2019 Jun 14;5(6):873-891. doi: 10.1021/acsinfecdis.8b00355. Epub 2019 Apr 23.

PMID:
30983322
4.

Galloyl Carbohydrates with Antiangiogenic Activity Mediated by Capillary Morphogenesis Gene 2 (CMG2) Protein Binding.

G-Doyagüez E, Carrero P, Madrona A, Rodriguez-Salamanca P, Martínez-Gualda B, Camarasa MJ, Jimeno ML, Bennallack PR, Finnell JG, Tsang TM, Christensen KA, San-Félix A, Rogers MS.

J Med Chem. 2019 Apr 25;62(8):3958-3970. doi: 10.1021/acs.jmedchem.8b01988. Epub 2019 Apr 9.

PMID:
30964669
5.

Diphenyl ether derivatives occupy the expanded binding site of cyclohexanedione compounds at the colchicine site in tubulin by movement of the αT5 loop.

Bueno O, Gargantilla M, Estévez-Gallego J, Martins S, Díaz JF, Camarasa MJ, Liekens S, Pérez-Pérez MJ, Priego EM.

Eur J Med Chem. 2019 Jun 1;171:195-208. doi: 10.1016/j.ejmech.2019.03.045. Epub 2019 Mar 21.

PMID:
30921759
6.
7.

A Novel Class of Cationic and Non-Peptidic Small Molecules as Hits for the Development of Antimicrobial Agents.

Jiménez A, García P, de la Puente S, Madrona A, Camarasa MJ, Pérez-Pérez MJ, Quintela JC, García-Del Portillo F, San-Félix A.

Molecules. 2018 Jun 22;23(7). pii: E1513. doi: 10.3390/molecules23071513.

8.

Polypharmacology in HIV inhibition: can a drug with simultaneous action against two relevant targets be an alternative to combination therapy?

de Castro S, Camarasa MJ.

Eur J Med Chem. 2018 Apr 25;150:206-227. doi: 10.1016/j.ejmech.2018.03.007. Epub 2018 Mar 5. Review.

9.

High-affinity ligands of the colchicine domain in tubulin based on a structure-guided design.

Bueno O, Estévez Gallego J, Martins S, Prota AE, Gago F, Gómez-SanJuan A, Camarasa MJ, Barasoain I, Steinmetz MO, Díaz JF, Pérez-Pérez MJ, Liekens S, Priego EM.

Sci Rep. 2018 Mar 9;8(1):4242. doi: 10.1038/s41598-018-22382-x.

10.

Trypanothione reductase inhibition and anti-leishmanial activity of all-hydrocarbon stapled α-helical peptides with improved proteolytic stability.

Ruiz-Santaquiteria M, de Castro S, Toro MA, de Lucio H, Gutiérrez KJ, Sánchez-Murcia PA, Jiménez MÁ, Gago F, Jiménez-Ruiz A, Camarasa MJ, Velázquez S.

Eur J Med Chem. 2018 Apr 10;149:238-247. doi: 10.1016/j.ejmech.2018.02.071. Epub 2018 Feb 24.

PMID:
29501944
11.

Conformational mimetics of the α-methyl chalcone TUB091 binding tubulin: Design, synthesis and antiproliferative activity.

Bueno O, Tobajas G, Quesada E, Estévez-Gallego J, Noppen S, Camarasa MJ, Díaz JF, Liekens S, Priego EM, Pérez-Pérez MJ.

Eur J Med Chem. 2018 Mar 25;148:337-348. doi: 10.1016/j.ejmech.2018.02.019. Epub 2018 Feb 10.

PMID:
29471122
12.

Inhibition of the Replication of Different Strains of Chikungunya Virus by 3-Aryl-[1,2,3]triazolo[4,5- d]pyrimidin-7(6 H)-ones.

Gómez-SanJuan A, Gamo AM, Delang L, Pérez-Sánchez A, Amrun SN, Abdelnabi R, Jacobs S, Priego EM, Camarasa MJ, Jochmans D, Leyssen P, Ng LFP, Querat G, Neyts J, Pérez-Pérez MJ.

ACS Infect Dis. 2018 Apr 13;4(4):605-619. doi: 10.1021/acsinfecdis.7b00219. Epub 2018 Feb 14.

PMID:
29406692
13.

Improved proteolytic stability and potent activity against Leishmania infantum trypanothione reductase of α/β-peptide foldamers conjugated to cell-penetrating peptides.

de Lucio H, Gamo AM, Ruiz-Santaquiteria M, de Castro S, Sánchez-Murcia PA, Toro MA, Gutiérrez KJ, Gago F, Jiménez-Ruiz A, Camarasa MJ, Velázquez S.

Eur J Med Chem. 2017 Nov 10;140:615-623. doi: 10.1016/j.ejmech.2017.09.032. Epub 2017 Sep 21.

PMID:
29017116
14.

Antiviral activity of [1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-ones against chikungunya virus targeting the viral capping nsP1.

Gigante A, Gómez-SanJuan A, Delang L, Li C, Bueno O, Gamo AM, Priego EM, Camarasa MJ, Jochmans D, Leyssen P, Decroly E, Coutard B, Querat G, Neyts J, Pérez-Pérez MJ.

Antiviral Res. 2017 Aug;144:216-222. doi: 10.1016/j.antiviral.2017.06.003. Epub 2017 Jun 12.

15.

First example of peptides targeting the dimer interface of Leishmania infantum trypanothione reductase with potent in vitro antileishmanial activity.

Ruiz-Santaquiteria M, Sánchez-Murcia PA, Toro MA, de Lucio H, Gutiérrez KJ, de Castro S, Carneiro FAC, Gago F, Jiménez-Ruiz A, Camarasa MJ, Velázquez S.

Eur J Med Chem. 2017 Jul 28;135:49-59. doi: 10.1016/j.ejmech.2017.04.020. Epub 2017 Apr 13.

16.

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.

17.

Optimization of a Class of Tryptophan Dendrimers That Inhibit HIV Replication Leads to a Selective, Specific, and Low-Nanomolar Inhibitor of Clinical Isolates of Enterovirus A71.

Rivero-Buceta E, Sun L, Martínez-Gualda B, Doyagüez EG, Donckers K, Quesada E, Camarasa MJ, Delang L, San-Félix A, Neyts J, Leyssen P.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):5064-7. doi: 10.1128/AAC.00626-16. Print 2016 Aug.

18.

Antivascular and antitumor properties of the tubulin-binding chalcone TUB091.

Canela MD, Noppen S, Bueno O, Prota AE, Bargsten K, Sáez-Calvo G, Jimeno ML, Benkheil M, Ribatti D, Velázquez S, Camarasa MJ, Díaz JF, Steinmetz MO, Priego EM, Pérez-Pérez MJ, Liekens S.

Oncotarget. 2017 Feb 28;8(9):14325-14342. doi: 10.18632/oncotarget.9527.

19.

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
20.

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
21.

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
22.

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

Velázquez S, de Castro S, Diez-Torrubia A, Balzarini J, Camarasa MJ.

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

PMID:
25620096
23.

Linear and branched alkyl-esters and amides of gallic acid and other (mono-, di- and tri-) hydroxy benzoyl derivatives as promising anti-HCV inhibitors.

Rivero-Buceta E, Carrero P, Doyagüez EG, Madrona A, Quesada E, Camarasa MJ, Peréz-Pérez MJ, Leyssen P, Paeshuyse J, Balzarini J, Neyts J, San-Félix A.

Eur J Med Chem. 2015 Mar 6;92:656-71. doi: 10.1016/j.ejmech.2015.01.033. Epub 2015 Jan 17.

PMID:
25617695
24.

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

Fernández-Cureses G, de Castro S, Jimeno ML, Balzarini J, Camarasa MJ.

ChemMedChem. 2015 Feb;10(2):321-35. doi: 10.1002/cmdc.201402465. Epub 2014 Nov 24.

PMID:
25420933
25.

Synthesis and antiproliferative activity of 6-phenylaminopurines.

Canela MD, Liekens S, Camarasa MJ, Priego EM, Pérez-Pérez MJ.

Eur J Med Chem. 2014 Nov 24;87:421-8. doi: 10.1016/j.ejmech.2014.09.093. Epub 2014 Sep 30.

PMID:
25282265
26.

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

de Castro S, Camarasa MJ, Balzarini J, Velázquez S.

Eur J Med Chem. 2014 Aug 18;83:174-89. doi: 10.1016/j.ejmech.2014.06.026. Epub 2014 Jun 13.

PMID:
24956554
27.

Microwave-assisted synthesis of C-8 aryl and heteroaryl inosines and determination of their inhibitory activities against Plasmodium falciparum purine nucleoside phosphorylase.

Gigante A, Priego EM, Sánchez-Carrasco P, Ruiz-Pérez LM, Vande Voorde J, Camarasa MJ, Balzarini J, González-Pacanowska D, Pérez-Pérez MJ.

Eur J Med Chem. 2014 Jul 23;82:459-65. doi: 10.1016/j.ejmech.2014.05.073. Epub 2014 Jun 2.

28.

Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1.

Flores A, Camarasa MJ, Pérez-Pérez MJ, San-Félix A, Balzarini J, Quesada E.

Org Biomol Chem. 2014 Jul 28;12(28):5278-94. doi: 10.1039/c4ob00445k.

PMID:
24927059
29.

Identification of [1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-ones as novel inhibitors of Chikungunya virus replication.

Gigante A, Canela MD, Delang L, Priego EM, Camarasa MJ, Querat G, Neyts J, Leyssen P, Pérez-Pérez MJ.

J Med Chem. 2014 May 22;57(10):4000-8. doi: 10.1021/jm401844c. Epub 2014 May 6.

PMID:
24800626
30.

Novel colchicine-site binders with a cyclohexanedione scaffold identified through a ligand-based virtual screening approach.

Canela MD, Pérez-Pérez MJ, Noppen S, Sáez-Calvo G, Díaz JF, Camarasa MJ, Liekens S, Priego EM.

J Med Chem. 2014 May 22;57(10):3924-38. doi: 10.1021/jm401939g. Epub 2014 May 9.

31.

Leishmania infantum EndoG is an endo/exo-nuclease essential for parasite survival.

Rico E, Oliva C, Gutierrez KJ, Alzate JF, Genes CM, Moreno D, Casanova E, Gigante A, Pérez-Pérez MJ, Camarasa MJ, Clos J, Gago F, Jiménez-Ruiz A.

PLoS One. 2014 Feb 26;9(2):e89526. doi: 10.1371/journal.pone.0089526. eCollection 2014.

32.

Novel water-soluble prodrugs of acyclovir cleavable by the dipeptidyl-peptidase IV (DPP IV/CD26) enzyme.

Diez-Torrubia A, Cabrera S, de Castro S, García-Aparicio C, Mulder G, De Meester I, Camarasa MJ, Balzarini J, Velázquez S.

Eur J Med Chem. 2013;70:456-68. doi: 10.1016/j.ejmech.2013.10.001. Epub 2013 Oct 9.

PMID:
24185376
33.

Probing the dimerization interface of Leishmania infantum trypanothione reductase with site-directed mutagenesis and short peptides.

Toro MA, Sánchez-Murcia PA, Moreno D, Ruiz-Santaquiteria M, Alzate JF, Negri A, Camarasa MJ, Gago F, Velázquez S, Jiménez-Ruiz A.

Chembiochem. 2013 Jul 8;14(10):1212-7. doi: 10.1002/cbic.201200744. Epub 2013 Jun 6.

PMID:
23744811
34.

5'-Trityl-substituted thymidine derivatives as a novel class of antileishmanial agents: Leishmania infantum EndoG as a potential target.

Casanova E, Moreno D, Gigante A, Rico E, Genes CM, Oliva C, Camarasa MJ, Gago F, Jiménez-Ruiz A, Pérez-Pérez MJ.

ChemMedChem. 2013 Jul;8(7):1161-74. doi: 10.1002/cmdc.201300129. Epub 2013 Apr 26.

PMID:
23625887
35.

Dipeptidyl peptidase IV-activated prodrugs of anti-varicella zoster virus bicyclic nucleoside analogues containing different self-cleavage spacer systems.

Diez-Torrubia A, Cabrera S, De Meester I, Camarasa MJ, Balzarini J, Velázquez S.

ChemMedChem. 2012 Sep;7(9):1612-22. doi: 10.1002/cmdc.201200295. Epub 2012 Aug 6.

PMID:
22887971
36.

Recent advances in thymidine kinase 2 (TK2) inhibitors and new perspectives for potential applications.

Priego EM, Karlsson A, Gago F, Camarasa MJ, Balzarini J, Pérez-Pérez MJ.

Curr Pharm Des. 2012;18(20):2981-94. Review.

PMID:
22571666
37.

Dipeptidyl peptidase IV (DPPIV/CD26)-based prodrugs of hydroxy-containing drugs.

Diez-Torrubia A, Cabrera S, Lambeir AM, Balzarini J, Camarasa MJ, Velázquez S.

ChemMedChem. 2012 Apr;7(4):618-28. doi: 10.1002/cmdc.201100504. Epub 2012 Feb 3.

PMID:
22307932
38.

Efficient synthesis and anti-enteroviral activity of 9-arylpurines.

Aguado L, Canela MD, Thibaut HJ, Priego EM, Camarasa MJ, Leyssen P, Neyts J, Pérez-Pérez MJ.

Eur J Med Chem. 2012 Mar;49:279-88. doi: 10.1016/j.ejmech.2012.01.022. Epub 2012 Jan 17.

PMID:
22305341
39.

Targeting HIV entry through interaction with envelope glycoprotein 120 (gp120): synthesis and antiviral evaluation of 1,3,5-triazines with aromatic amino acids.

Lozano V, Aguado L, Hoorelbeke B, Renders M, Camarasa MJ, Schols D, Balzarini J, San-Félix A, Pérez-Pérez MJ.

J Med Chem. 2011 Aug 11;54(15):5335-48. doi: 10.1021/jm200560r. Epub 2011 Jul 13.

PMID:
21749165
40.

Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides.

Bonache MC, Cordeiro A, Quesada E, Vanstreels E, Daelemans D, Camarasa MJ, Balzarini J, San-Félix A.

Antiviral Res. 2011 Oct;92(1):37-44. doi: 10.1016/j.antiviral.2011.05.002. Epub 2011 May 12.

PMID:
21600933
41.

Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket.

Das K, Bauman JD, Rim AS, Dharia C, Clark AD Jr, Camarasa MJ, Balzarini J, Arnold E.

J Med Chem. 2011 Apr 28;54(8):2727-37. doi: 10.1021/jm101536x. Epub 2011 Mar 29.

42.

From β-amino-γ-sultone to unusual bicyclic pyridine and pyrazine heterocyclic systems: synthesis and cytostatic and antiviral activities.

de Castro S, Familiar O, Andrei G, Snoeck R, Balzarini J, Camarasa MJ, Velázquez S.

ChemMedChem. 2011 Apr 4;6(4):686-97. doi: 10.1002/cmdc.201000546. Epub 2011 Mar 2.

PMID:
21370477
43.

Dipeptidyl peptidase IV dependent water-soluble prodrugs of highly lipophilic bicyclic nucleoside analogues.

Diez-Torrubia A, Balzarini J, Andrei G, Snoeck R, De Meester I, Camarasa MJ, Velázquez S.

J Med Chem. 2011 Mar 24;54(6):1927-42. doi: 10.1021/jm101624e. Epub 2011 Feb 18.

PMID:
21332170
44.

Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone.

Familiar O, Munier-Lehmann H, Aínsa JA, Camarasa MJ, Pérez-Pérez MJ.

Eur J Med Chem. 2010 Dec;45(12):5910-8. doi: 10.1016/j.ejmech.2010.09.056. Epub 2010 Oct 15.

PMID:
20951473
45.

Intramolecular cation-pi interactions as the driving force to restrict the conformation of certain nucleosides.

Casanova E, Priego EM, Jimeno ML, Aguado L, Negri A, Gago F, Camarasa MJ, Pérez-Pérez MJ.

J Org Chem. 2010 Mar 19;75(6):1974-81. doi: 10.1021/jo902677s.

PMID:
20192191
46.

Application of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to different amine-containing drugs.

Diez-Torrubia A, García-Aparicio C, Cabrera S, De Meester I, Balzarini J, Camarasa MJ, Velázquez S.

J Med Chem. 2010 Jan 28;53(2):559-72. doi: 10.1021/jm901590f.

PMID:
20000418
47.

9-Arylpurines as a novel class of enterovirus inhibitors.

Aguado L, Thibaut HJ, Priego EM, Jimeno ML, Camarasa MJ, Neyts J, Pérez-Pérez MJ.

J Med Chem. 2010 Jan 14;53(1):316-24. doi: 10.1021/jm901240p.

PMID:
19924996
48.

One-pot synthesis of polycyclic nucleosides with unusual molecular skeletons.

Bonache MC, Cordeiro A, Carrero P, Quesada E, Camarasa MJ, Jimeno ML, San-Félix A.

J Org Chem. 2009 Dec 4;74(23):9071-81. doi: 10.1021/jo9019144.

PMID:
19888745
49.

Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59).

Bronckaers A, Aguado L, Negri A, Camarasa MJ, Balzarini J, Pérez-Pérez MJ, Gago F, Liekens S.

Biochem Pharmacol. 2009 Aug 1;78(3):231-40. doi: 10.1016/j.bcp.2009.04.011. Epub 2009 Apr 21.

PMID:
19389384
50.

4-Benzyloxy-gamma-sultone derivatives: discovery of a novel family of non-nucleoside inhibitors of human cytomegalovirus and varicella zoster virus.

De Castro S, García-Aparicio C, Andrei G, Snoeck R, Balzarini J, Camarasa MJ, Velázquez S.

J Med Chem. 2009 Mar 26;52(6):1582-91. doi: 10.1021/jm8014662. Erratum in: J Med Chem. 2009 May 14;52(9):3121.

PMID:
19226140

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