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Items: 1 to 50 of 189

1.

Cathepsin L Inhibitors with Activity against the Liver Fluke Identified From a Focus Library of Quinoxaline 1,4-di-N-Oxide Derivatives.

Ferraro F, Merlino A, Gil J, Cerecetto H, Corvo I, Cabrera M.

Molecules. 2019 Jun 26;24(13). pii: E2348. doi: 10.3390/molecules24132348.

2.

Formation of dendrimer-guest complexes as a strategy to increase the solubility of a phenazine N, N'-dioxide derivative with antitumor activity.

Dib N, Fernández L, Santo M, Otero L, Alustiza F, Liaudat AC, Bosch P, Lavaggi ML, Cerecetto H, González M.

Heliyon. 2019 Apr 23;5(4):e01528. doi: 10.1016/j.heliyon.2019.e01528. eCollection 2019 Apr.

3.

Identification of N-Oxide-Containing Aromatic Heterocycles as Pharmacophores for Rumen Fermentation Modifiers.

Bonifacino C, Rodríguez G, Pérez-Ruchel A, Repetto JL, Cerecetto H, Cajarville C, González M.

Metabolites. 2019 Apr 2;9(4). pii: E62. doi: 10.3390/metabo9040062.

4.

Chemosensitizer effect of cisplatin-treated bladder cancer cells by phenazine-5,10-dioxides.

Hernández P, Alem D, Nieves M, Cerecetto H, González M, Martínez-López W, Lavaggi ML.

Environ Toxicol Pharmacol. 2019 Jul;69:9-15. doi: 10.1016/j.etap.2019.03.015. Epub 2019 Mar 19.

PMID:
30921672
5.

Inhibition of LDL oxidation and inflammasome assembly by nitroaliphatic derivatives. Potential use as anti-inflammatory and anti-atherogenic agents.

Cataldo N, Musetti B, Celano L, Carabio C, Cassina A, Cerecetto H, González M, Thomson L.

Eur J Med Chem. 2018 Nov 5;159:178-186. doi: 10.1016/j.ejmech.2018.09.062. Epub 2018 Sep 26.

PMID:
30292895
6.

Novel and Selective Rhipicephalus microplus Triosephosphate Isomerase Inhibitors with Acaricidal Activity.

Saramago L, Gomes H, Aguilera E, Cerecetto H, González M, Cabrera M, Alzugaray MF, da Silva Vaz Junior I, Nunes da Fonseca R, Aguirre-López B, Cabrera N, Pérez-Montfort R, Merlino A, Moraes J, Álvarez G.

Vet Sci. 2018 Aug 23;5(3). pii: E74. doi: 10.3390/vetsci5030074.

7.

Synthesis of hydrophilic HYNIC-[1,2,4,5]tetrazine conjugates and their use in antibody pretargeting with 99mTc.

García MF, Gallazzi F, Junqueira MS, Fernández M, Camacho X, Mororó JDS, Faria D, Carneiro CG, Couto M, Carrión F, Pritsch O, Chammas R, Quinn T, Cabral P, Cerecetto H.

Org Biomol Chem. 2018 Jul 25;16(29):5275-5285. doi: 10.1039/c8ob01255e.

PMID:
29974915
8.

Polypharmacology in the treatment of Chagas disease.

Aguilera E, Alvarez G, Cerecetto H, Gonzalez M.

Curr Med Chem. 2018 Apr 9. doi: 10.2174/0929867325666180410101728. [Epub ahead of print]

PMID:
29637852
9.

Looking for combination of benznidazole and Trypanosoma cruzi-triosephosphate isomerase inhibitors for Chagas disease treatment.

Aguilera E, Varela J, Serna E, Torres S, Yaluff G, Bilbao NV, Cerecetto H, Alvarez G, González M.

Mem Inst Oswaldo Cruz. 2018 Mar;113(3):153-160. doi: 10.1590/0074-02760170267.

10.

Discovery of Potent EGFR Inhibitors through the Incorporation of a 3D-Aromatic-Boron-Rich-Cluster into the 4-Anilinoquinazoline Scaffold: Potential Drugs for Glioma Treatment.

Couto M, García MF, Alamón C, Cabrera M, Cabral P, Merlino A, Teixidor F, Cerecetto H, Viñas C.

Chemistry. 2018 Mar 2;24(13):3122-3126. doi: 10.1002/chem.201705181. Epub 2017 Dec 22.

PMID:
29194843
11.

Derivatizations of Sgc8-c aptamer to prepare metallic radiopharmaceuticals as imaging diagnostic agents: Syntheses, isolations, and physicochemical characterizations.

Sicco E, Báez J, Margenat J, García F, Ibarra M, Cabral P, Moreno M, Cerecetto H, Calzada V.

Chem Biol Drug Des. 2018 Mar;91(3):747-755. doi: 10.1111/cbdd.13135. Epub 2017 Nov 24.

PMID:
29080264
12.

Development, validation and application of a GC-MS method for the simultaneous detection and quantification of neutral lipid species in Trypanosoma cruzi.

Santivañez-Veliz M, Moreno-Viguri E, Pérez-Silanes S, Varela J, Cerecetto H, González M, Lizarraga E.

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Sep 1;1061-1062:225-232. doi: 10.1016/j.jchromb.2017.07.031. Epub 2017 Jul 19.

PMID:
28750236
13.

3-(Benzyloxy)-1-(5-[18F]fluoropentyl)-5-nitro-1H-indazole: a PET radiotracer to measure acetylcholinesterase in brain.

Fernández S, Giglio J, Reyes AL, Damián A, Pérez C, Pérez DI, González M, Oliver P, Rey A, Engler H, Cerecetto H.

Future Med Chem. 2017 Jun;9(10):983-994. doi: 10.4155/fmc-2017-0023. Epub 2017 Jun 20.

PMID:
28632402
14.

Small-Molecule Kinase-Inhibitors-Loaded Boron Cluster as Hybrid Agents for Glioma-Cell-Targeting Therapy.

Couto M, Mastandrea I, Cabrera M, Cabral P, Teixidor F, Cerecetto H, Viñas C.

Chemistry. 2017 Jul 12;23(39):9233-9238. doi: 10.1002/chem.201701965. Epub 2017 Jul 3.

PMID:
28605114
15.

Novel Imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides as antiproliferative trypanosoma cruzi drugs: Computational screening from neural network, synthesis and in vivo biological properties.

Guerra A, Gonzalez-Naranjo P, Campillo NE, Varela J, Lavaggi ML, Merlino A, Cerecetto H, González M, Gomez-Barrio A, Escario JA, Fonseca-Berzal C, Yaluf G, Paniagua-Solis J, Páez JA.

Eur J Med Chem. 2017 Aug 18;136:223-234. doi: 10.1016/j.ejmech.2017.04.075. Epub 2017 May 1.

PMID:
28499168
16.

Multi-Anti-Parasitic Activity of Arylidene Ketones and Thiazolidene Hydrazines against Trypanosoma cruzi and Leishmania spp.

Álvarez G, Perdomo C, Coronel C, Aguilera E, Varela J, Aparicio G, Zolessi FR, Cabrera N, Vega C, Rolón M, Rojas de Arias A, Pérez-Montfort R, Cerecetto H, González M.

Molecules. 2017 May 7;22(5). pii: E709. doi: 10.3390/molecules22050709.

17.

Tocilizumab Labeling with 99mTechnetium via HYNIC as a Molecular Diagnostic Agent for Multiple Myeloma.

Camacho X, Machado CL, García MF, Fernández M, Oddone N, Benech J, Gambini JP, Cerecetto H, Chammas R, Cabral P, Riva E.

Anticancer Agents Med Chem. 2017;17(9):1267-1277. doi: 10.2174/1871520617666170213144917.

PMID:
28270081
18.

Development of new PTK7-targeting aptamer-fluorescent and -radiolabelled probes for evaluation as molecular imaging agents: Lymphoma and melanoma in vivo proof of concept.

Calzada V, Moreno M, Newton J, González J, Fernández M, Gambini JP, Ibarra M, Chabalgoity A, Deutscher S, Quinn T, Cabral P, Cerecetto H.

Bioorg Med Chem. 2017 Feb 1;25(3):1163-1171. doi: 10.1016/j.bmc.2016.12.026. Epub 2016 Dec 24.

PMID:
28089349
19.

New hits as phase II enzymes inducers from a focused library with heteroatom-heteroatom and Michael-acceptor motives.

Cabrera M, de Ovalle S, Bollati-Fogolín M, Nascimento F, Corbelini P, Janarelli F, Kawano D, Eifler-Lima VL, González M, Cerecetto H.

Future Sci OA. 2015 Nov 1;1(3):FSO20. doi: 10.4155/fso.15.18. eCollection 2015 Nov.

20.

The Effect of A Hexanoic Acid Linker Insertion on the Pharmacokinetics and Tumor Targeting Properties of the Melanoma Imaging Agent 99mTc-HYNIC-cycMSH.

Teixeira V, Fernández M, Oddone N, Zhang X, Gallazzi F, Cerecetto H, Gambini JP, Porcal W, Cabral P, Quinn TP.

Anticancer Agents Med Chem. 2017;17(8):1144-1152. doi: 10.2174/1871520616666161206144414.

PMID:
27924732
21.

Identification of Chalcones as Fasciola hepatica Cathepsin L Inhibitors Using a Comprehensive Experimental and Computational Approach.

Ferraro F, Merlino A, Dell Oca N, Gil J, Tort JF, Gonzalez M, Cerecetto H, Cabrera M, Corvo I.

PLoS Negl Trop Dis. 2016 Jul 27;10(7):e0004834. doi: 10.1371/journal.pntd.0004834. eCollection 2016 Jul.

22.

In vitro and in vivo uptake studies of PAMAM G4.5 dendrimers in breast cancer.

Oddone N, Lecot N, Fernández M, Rodriguez-Haralambides A, Cabral P, Cerecetto H, Benech JC.

J Nanobiotechnology. 2016 Jun 13;14(1):45. doi: 10.1186/s12951-016-0197-6.

23.

In vivo phase II-enzymes inducers, as potential chemopreventive agents, based on the chalcone and furoxan skeletons.

Cabrera M, Mastandrea I, Otero G, Cerecetto H, González M.

Bioorg Med Chem. 2016 Apr 15;24(8):1665-74. doi: 10.1016/j.bmc.2016.02.041. Epub 2016 Mar 2.

PMID:
26970663
24.

Radiopharmaceuticals in Tumor Hypoxia Imaging: A Review Focused on Medicinal Chemistry Aspects.

Cabral P, Cerecetto H.

Anticancer Agents Med Chem. 2017;17(3):318-332. doi: 10.2174/1871520616666160307142514. Review.

PMID:
26953234
25.

(99m)Tc-bioorthogonal click chemistry reagent for in vivo pretargeted imaging.

García MF, Zhang X, Shah M, Newton-Northup J, Cabral P, Cerecetto H, Quinn T.

Bioorg Med Chem. 2016 Mar 15;24(6):1209-15. doi: 10.1016/j.bmc.2016.01.046. Epub 2016 Jan 29.

26.

Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity.

Pérez-Silanes S, Torres E, Arbillaga L, Varela J, Cerecetto H, González M, Azqueta A, Moreno-Viguri E.

Bioorg Med Chem Lett. 2016 Feb 1;26(3):903-906. doi: 10.1016/j.bmcl.2015.12.070. Epub 2015 Dec 21.

27.

Potent and Selective Inhibitors of Trypanosoma cruzi Triosephosphate Isomerase with Concomitant Inhibition of Cruzipain: Inhibition of Parasite Growth through Multitarget Activity.

Aguilera E, Varela J, Birriel E, Serna E, Torres S, Yaluff G, de Bilbao NV, Aguirre-López B, Cabrera N, Díaz Mazariegos S, de Gómez-Puyou MT, Gómez-Puyou A, Pérez-Montfort R, Minini L, Merlino A, Cerecetto H, González M, Alvarez G.

ChemMedChem. 2016 Jun 20;11(12):1328-38. doi: 10.1002/cmdc.201500385. Epub 2015 Oct 23.

PMID:
26492824
28.

Analgesic and Anti-Inflammatory Properties of Arylnitroalkenes.

Celano L, Cupertino Da Silva YK, Cataldo N, Gabay M, Merlino A, Alexandre-Moreira MS, Lima LM, Cerecetto H, González M, Thomson L.

Inflamm Allergy Drug Targets. 2015;14(1):19-28.

PMID:
26490661
29.

3-H-[1,2]Dithiole as a New Anti-Trypanosoma cruzi Chemotype: Biological and Mechanism of Action Studies.

Couto M, Sánchez C, Dávila B, Machín V, Varela J, Álvarez G, Cabrera M, Celano L, Aguirre-López B, Cabrera N, de Gómez-Puyou MT, Gómez-Puyou A, Pérez-Montfort R, Cerecetto H, González M.

Molecules. 2015 Aug 12;20(8):14595-610. doi: 10.3390/molecules200814595.

30.

Development of bis-thiazoles as inhibitors of triosephosphate isomerase from Trypanosoma cruzi. Identification of new non-mutagenic agents that are active in vivo.

Álvarez G, Martínez J, Varela J, Birriel E, Cruces E, Gabay M, Leal SM, Escobar P, Aguirre-López B, Cabrera N, Tuena de Gómez-Puyou M, Gómez Puyou A, Pérez-Montfort R, Yaluff G, Torres S, Serna E, Vera de Bilbao N, González M, Cerecetto H.

Eur J Med Chem. 2015 Jul 15;100:246-56. doi: 10.1016/j.ejmech.2015.06.018. Epub 2015 Jun 12.

PMID:
26094151
31.

Design, synthesis and in vitro trypanocidal and leishmanicidal activities of novel semicarbazone derivatives.

Alves MA, de Queiroz AC, Alexandre-Moreira MS, Varela J, Cerecetto H, González M, Doriguetto AC, Landre IM, Barreiro EJ, Lima LM.

Eur J Med Chem. 2015 Jul 15;100:24-33. doi: 10.1016/j.ejmech.2015.05.046. Epub 2015 Jun 2.

PMID:
26069927
32.

Searching phase II enzymes inducers, from Michael acceptor-[1,2]dithiolethione hybrids, as cancer chemopreventive agents.

Couto M, de Ovalle S, Cabrera M, Cerecetto H, González M.

Future Med Chem. 2015;7(7):857-71. doi: 10.4155/fmc.15.32.

PMID:
26061105
33.

Molecular docking and molecular dynamics simulation studies of Trypanosoma cruzi triosephosphate isomerase inhibitors. Insights into the inhibition mechanism and selectivity.

Minini L, Álvarez G, González M, Cerecetto H, Merlino A.

J Mol Graph Model. 2015 May;58:40-9. doi: 10.1016/j.jmgm.2015.02.002. Epub 2015 Feb 21.

PMID:
25829097
34.

Expanding the family of heteroleptic oxidovanadium(IV) compounds with salicylaldehyde semicarbazones and polypyridyl ligands showing anti-Trypanosoma cruzi activity.

Scalese G, Benítez J, Rostán S, Correia I, Bradford L, Vieites M, Minini L, Merlino A, Coitiño EL, Birriel E, Varela J, Cerecetto H, González M, Pessoa JC, Gambino D.

J Inorg Biochem. 2015 Jun;147:116-25. doi: 10.1016/j.jinorgbio.2015.03.002. Epub 2015 Mar 12.

PMID:
25824466
35.

Spin trapping: an essential tool for the study of diseases caused by oxidative stress.

Barriga-González G, Olea-Azar C, Zuñiga-López MC, Folch-Cano C, Aguilera-Venegas B, Porcal W, González M, Cerecetto H.

Curr Top Med Chem. 2015;15(5):484-95. Review.

PMID:
25658802
36.

Development, characterization, and in vitro biological performance of fluconazole-loaded microemulsions for the topical treatment of cutaneous leishmaniasis.

Oliveira MB, Calixto G, Graminha M, Cerecetto H, González M, Chorilli M.

Biomed Res Int. 2015;2015:396894. doi: 10.1155/2015/396894. Epub 2015 Jan 12.

37.

Identification of a new amide-containing thiazole as a drug candidate for treatment of Chagas' disease.

Álvarez G, Varela J, Cruces E, Fernández M, Gabay M, Leal SM, Escobar P, Sanabria L, Serna E, Torres S, Figueredo Thiel SJ, Yaluff G, Vera de Bilbao NI, Cerecetto H, González M.

Antimicrob Agents Chemother. 2015 Mar;59(3):1398-404. doi: 10.1128/AAC.03814-14. Epub 2014 Dec 15.

38.

Anaerobic metabolism of the agro-pesticide nitroxinil by bovine ruminal fluid.

Irazoqui I, Rodriguez A, Birriel E, Gabay M, Lavaggi ML, Repetto JL, Cajarville C, Gonzalez M, Cerecetto H.

Drug Metab Lett. 2014;8(2):101-8.

PMID:
25496284
39.

Preparation and biological evaluation of (99m)Tc-labelled phenazine dioxides as potential tracers for hypoxia imaging.

Fernández S, Berchesi A, Tejeria E, Sanz I, Cerecetto H, González M, Lavaggi ML, Rey A.

Curr Radiopharm. 2015;8(1):56-61.

PMID:
25440318
40.

Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents.

Tapia RA, Salas CO, Vázquez K, Espinosa-Bustos C, Soto-Delgado J, Varela J, Birriel E, Cerecetto H, González M, Paulino M.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3919-22. doi: 10.1016/j.bmcl.2014.06.044. Epub 2014 Jun 24.

PMID:
25008454
41.

In vivo anti-Trypanosoma cruzi activity of hydro-ethanolic extract and isolated active principles from Aristeguietia glutinosa and mechanism of action studies.

Varela J, Serna E, Torres S, Yaluff G, de Bilbao NI, Miño P, Chiriboga X, Cerecetto H, González M.

Molecules. 2014 Jun 23;19(6):8488-502. doi: 10.3390/molecules19068488.

42.

Mutagenicity of N-oxide containing heterocycles and related compounds: experimental and theoretical studies.

Gabay M, Cabrera M, Maio RD, Paez JA, Campillo N, Lavaggi ML, Cerecetto H, González M.

Curr Top Med Chem. 2014;14(11):1374-87.

PMID:
24805062
43.

Optimization of antitrypanosomatid agents: identification of nonmutagenic drug candidates with in vivo activity.

Álvarez G, Varela J, Márquez P, Gabay M, Arias Rivas CE, Cuchilla K, Echeverría GA, Piro OE, Chorilli M, Leal SM, Escobar P, Serna E, Torres S, Yaluff G, Vera de Bilbao NI, González M, Cerecetto H.

J Med Chem. 2014 May 22;57(10):3984-99. doi: 10.1021/jm500018m. Epub 2014 May 2.

PMID:
24749923
44.

Synthesis and evaluation of a new 99mTc(I)-tricarbonyl complex bearing the 5-nitroimidazol-1-yl moiety as potential hypoxia imaging agent.

Giglio J, Dematteis S, Fernández S, Cerecetto H, Rey A.

J Labelled Comp Radiopharm. 2014 May 30;57(6):403-9. doi: 10.1002/jlcr.3195. Epub 2014 Apr 1.

PMID:
24692093
45.

Trypanosoma cruzi chemical proteomics using immobilized benznidazole.

Trochine A, Alvarez G, Corre S, Faral-Tello P, Durán R, Batthyany CI, Cerecetto H, González M, Robello C.

Exp Parasitol. 2014 May;140:33-8. doi: 10.1016/j.exppara.2014.03.013. Epub 2014 Mar 13.

PMID:
24632192
46.

Initial studies on mechanism of action and cell death of active N-oxide-containing heterocycles in Trypanosoma cruzi epimastigotes in vitro.

Benítez D, Casanova G, Cabrera G, Galanti N, Cerecetto H, González M.

Parasitology. 2014 Apr;141(5):682-96. doi: 10.1017/S003118201300200X. Epub 2014 Jan 27.

PMID:
24476762
47.

Arylnitroalkenes as scavengers of macrophage-generated oxidants.

Celano L, Carabio C, Frache R, Cataldo N, Cerecetto H, González M, Thomson L.

Eur J Med Chem. 2014 Mar 3;74:31-40. doi: 10.1016/j.ejmech.2013.12.029. Epub 2014 Jan 3.

PMID:
24440380
48.

A serendipitous one-step conversion of 3H-1,2-dithiole-3-thione to (E)-3-[1-(alkylthio)alkylidene]-3H-1,2-dithiole: an experimental and theoretical study.

Couto M, Cabrera M, Echeverría GA, Piro OE, González M, Cerecetto H.

Mol Divers. 2014 May;18(2):285-94. doi: 10.1007/s11030-013-9499-x. Epub 2014 Jan 14.

PMID:
24420794
49.

Identification of novel benzimidazole derivatives as anti-Trypanosoma cruzi agents: solid-phase synthesis, structure-activity relationships and molecular docking studies.

Ríos N, Varela J, Birriel E, González M, Cerecetto H, Merlino A, Porcal W.

Future Med Chem. 2013 Oct;5(15):1719-32. doi: 10.4155/fmc.13.160.

PMID:
24144409
50.

Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents.

Torres E, Moreno-Viguri E, Galiano S, Devarapally G, Crawford PW, Azqueta A, Arbillaga L, Varela J, Birriel E, Di Maio R, Cerecetto H, González M, Aldana I, Monge A, Pérez-Silanes S.

Eur J Med Chem. 2013 Aug;66:324-34. doi: 10.1016/j.ejmech.2013.04.065. Epub 2013 May 30.

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