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Items: 1 to 50 of 96

1.

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.

2.

Novel Polyphenols That Inhibit Colon Cancer Cell Growth Affecting Cancer Cell Metabolism.

Gómez de Cedrón M, Vargas T, Madrona A, Jiménez A, Pérez-Pérez MJ, Quintela JC, Reglero G, San-Félix A, Ramírez de Molina A.

J Pharmacol Exp Ther. 2018 Aug;366(2):377-389. doi: 10.1124/jpet.118.248278. Epub 2018 Jun 5.

PMID:
29871992
3.

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.

4.

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
5.

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
6.

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.

7.

The viral capping enzyme nsP1: a novel target for the inhibition of chikungunya virus infection.

Delang L, Li C, Tas A, Quérat G, Albulescu IC, De Burghgraeve T, Guerrero NA, Gigante A, Piorkowski G, Decroly E, Jochmans D, Canard B, Snijder EJ, Pérez-Pérez MJ, van Hemert MJ, Coutard B, Leyssen P, Neyts J.

Sci Rep. 2016 Aug 22;6:31819. doi: 10.1038/srep31819.

8.

Blocking Blood Flow to Solid Tumors by Destabilizing Tubulin: An Approach to Targeting Tumor Growth.

Pérez-Pérez MJ, Priego EM, Bueno O, Martins MS, Canela MD, Liekens S.

J Med Chem. 2016 Oct 13;59(19):8685-8711. Epub 2016 Jun 27.

9.

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.

10.

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
11.

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
12.

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
13.

Thymidine phosphorylase participates in platelet signaling and promotes thrombosis.

Li W, Gigante A, Perez-Perez MJ, Yue H, Hirano M, McIntyre TM, Silverstein RL.

Circ Res. 2014 Dec 5;115(12):997-1006. doi: 10.1161/CIRCRESAHA.115.304591. Epub 2014 Oct 6.

14.

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
15.

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.

16.

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
17.

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
18.

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.

PMID:
24773591
19.

Binding of glutathione to enterovirus capsids is essential for virion morphogenesis.

Thibaut HJ, van der Linden L, Jiang P, Thys B, Canela MD, Aguado L, Rombaut B, Wimmer E, Paul A, Pérez-Pérez MJ, van Kuppeveld FJ, Neyts J.

PLoS Pathog. 2014 Apr 10;10(4):e1004039. doi: 10.1371/journal.ppat.1004039. eCollection 2014 Apr.

20.

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.

21.

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
22.

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
23.

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
24.

The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist.

Liekens S, Bronckaers A, Belleri M, Bugatti A, Sienaert R, Ribatti D, Nico B, Gigante A, Casanova E, Opdenakker G, Pérez-Pérez MJ, Balzarini J, Presta M.

Mol Cancer Ther. 2012 Apr;11(4):817-29. doi: 10.1158/1535-7163.MCT-11-0738. Epub 2012 Feb 1.

25.

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
26.

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
27.

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
28.

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
29.

The phthalocyanine prototype derivative Alcian Blue is the first synthetic agent with selective anti-human immunodeficiency virus activity due to its gp120 glycan-binding potential.

François KO, Pannecouque C, Auwerx J, Lozano V, Pérez-Pérez MJ, Schols D, Balzarini J.

Antimicrob Agents Chemother. 2009 Nov;53(11):4852-9. doi: 10.1128/AAC.00811-09. Epub 2009 Aug 31.

30.

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
31.

Microwave-assisted synthesis of 9-arylpurines.

Aguado L, Camarasa MJ, Pérez-Pérez MJ.

J Comb Chem. 2009 Mar 9;11(2):210-2. doi: 10.1021/cc800169d. No abstract available.

PMID:
19178290
32.

A novel organogelator incorporating tert-butyl esters of asparagines.

Lozano V, Hernández R, Mijangos C, Pérez-Pérez MJ.

Org Biomol Chem. 2009 Jan 21;7(2):364-9. doi: 10.1039/b817565a. Epub 2008 Nov 20.

PMID:
19109683
33.

Structure, physiological role, and specific inhibitors of human thymidine kinase 2 (TK2): present and future.

Pérez-Pérez MJ, Priego EM, Hernández AI, Familiar O, Camarasa MJ, Negri A, Gago F, Balzarini J.

Med Res Rev. 2008 Sep;28(5):797-820. doi: 10.1002/med.20124. Review.

PMID:
18459168
34.

Exploring acyclic nucleoside analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase.

Familiar O, Munier-Lehmann H, Negri A, Gago F, Douguet D, Rigouts L, Hernández AI, Camarasa MJ, Pérez-Pérez MJ.

ChemMedChem. 2008 Jul;3(7):1083-93. doi: 10.1002/cmdc.200800060.

PMID:
18418833
35.

Novel N-3 substituted TSAO-T derivatives: synthesis and anti-HIV-evaluation.

Bonache MC, Quesada E, Sheen CW, Balzarini J, Sluis-Cremer N, Pérez-Pérez MJ, Camarasa MJ, San-Félix A.

Nucleosides Nucleotides Nucleic Acids. 2008 Apr;27(4):351-67. doi: 10.1080/15257770801943990.

PMID:
18404570
36.

7,5'-O-dibenzylinosines: synthesis and studies on their conformational properties.

Casanova E, Aguado L, Jimeno ML, Gago F, Camarasa MJ, Pérez-Pérez MJ.

Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):695-9.

PMID:
18066882
37.

Selective human adenosine A3 antagonists based on pyrido[2,1-f]purine-2,4-diones: novel features of hA3 antagonist binding.

Priego EM, Pérez-Pérez MJ, von Frijtag Drabbe Kuenzel JK, de Vries H, Ijzerman AP, Camarasa MJ, Martín-Santamaría S.

ChemMedChem. 2008 Jan;3(1):111-9.

PMID:
18000937
38.

Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy.

Liekens S, Bronckaers A, Pérez-Pérez MJ, Balzarini J.

Biochem Pharmacol. 2007 Dec 3;74(11):1555-67. Epub 2007 May 16. Review.

PMID:
17572389
39.

N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.

Hernandez AI, Familiar O, Negri A, Rodríguez-Barrios F, Gago F, Karlsson A, Camarasa MJ, Balzarini J, Pérez-Pérez MJ.

J Med Chem. 2006 Dec 28;49(26):7766-73.

PMID:
17181158
40.

Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds.

Liekens S, Balzarini J, Hernández AI, De Clercq E, Priego EM, Camarasa MJ, Pérez-Pérez MJ.

Nucleosides Nucleotides Nucleic Acids. 2006;25(9-11):975-80.

PMID:
17065049
41.

5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.

Casanova E, Hernandez AI, Priego EM, Liekens S, Camarasa MJ, Balzarini J, Pérez-Pérez MJ.

J Med Chem. 2006 Sep 7;49(18):5562-70.

PMID:
16942029
42.

Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: a single mode of inhibition for the three HIV enzymes?

Camarasa MJ, Velázquez S, San-Félix A, Pérez-Pérez MJ, Gago F.

Antiviral Res. 2006 Sep;71(2-3):260-7. Epub 2006 Jun 28. Review.

PMID:
16872687
43.

Structural basis for non-competitive product inhibition in human thymidine phosphorylase: implications for drug design.

El Omari K, Bronckaers A, Liekens S, Pérez-Pérez MJ, Balzarini J, Stammers DK.

Biochem J. 2006 Oct 15;399(2):199-204.

44.

TSAO derivatives, inhibitors of HIV-1 reverse transcriptase dimerization: recent progress.

Camarasa MJ, Velázquez S, San-Félix A, Pérez-Pérez MJ, Bonache MC, De Castro S.

Curr Pharm Des. 2006;12(15):1895-907. Review.

PMID:
16724955
45.

5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis.

Liekens S, Bronckaers A, Hernández AI, Priego EM, Casanova E, Camarasa MJ, Pérez-Pérez MJ, Balzarini J.

Mol Pharmacol. 2006 Aug;70(2):501-9. Epub 2006 May 4.

46.

Bromovinyl-deoxyuridine: A selective substrate for mitochondrial thymidine kinase in cell extracts.

Franzolin E, Rampazzo C, Pérez-Pérez MJ, Hernández AI, Balzarini J, Bianchi V.

Biochem Biophys Res Commun. 2006 May 26;344(1):30-6.

PMID:
16630572
47.
48.

Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications.

Pérez-Pérez MJ, Priego EM, Hernández AI, Camarasa MJ, Balzarini J, Liekens S.

Mini Rev Med Chem. 2005 Dec;5(12):1113-23. Review.

PMID:
16375757
49.

Mitochondrial thymidine kinase inhibitors.

Pérez-Pérez MJ, Hernández AI, Priego EM, Rodríguez-Barrios F, Gago F, Camarasa MJ, Balzarini J.

Curr Top Med Chem. 2005;5(13):1205-19. Review.

PMID:
16305527
50.

TSAO derivatives the first non-peptide inhibitors of HIV-1 RT dimerization.

Camarasa MJ, Velázquez S, San-Félix A, Pérez-Pérez MJ.

Antivir Chem Chemother. 2005;16(3):147-53. Review.

PMID:
16004078

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