Información general

Espinosa B., Christian
Profesor Asistente

Doctor en Química
Pontificia Universidad Católica de Chile, 2013.

Perfil en ORCID

Líneas de Investigación

Líneas de investigación:
Quimica medicinal
Síntesis de heterociclos 
Química Orgánica

Nuestro grupo de investigación está interesado en la síntesis de compuestos que actúen como antagonistas de dos subtipos de receptor de histamina H3 y H4.

La modulación del receptor de histamina 3 por antagonistas, tiene potencial utilidad terapéutica en trastornos neurodegenerativos como por ejemplo en la enfermedad de Alzheimer. Por otro lado, los antagonistas de los receptores de histamina 4 serían útiles en el tratamiento de enfermedades inflamatorias e inmunes, tales como rinitis alérgica, asma y dermatitis atópica.

Además, también nos interesa la obtención de compuestos que sean capaces de inhibir ambas isoformas de la enzima monoamino oxidasa (MAO-A y MAO-B) como también a la enzima acetilcolinesterasa, ambas involucradas en procesos neurodegenerativos.

Docencia

QIM201G  Química
QIF102A    Fármaco-Química II
QIF100B    Introducción a las ciencias farmacéuticas
QPG3280  Química Heterocíclica

Proyectos

2019 - 2022:
Development and evaluation of electrochemical hybrid platforms conformed by redox conducting polymers and transition metal dichalcogenides (MS2, M= Mo and W) and its application in the analysis and determination of amyloid peptides. CONICYT FONDECYT Regular 1190206.

2018 - 2021:
In the search for better therapies for neurodegenerative disorders: Pyrrolopyrimidines and derivatives as a new class of histamine 3 receptor antagonists. CONICYT FONDECYT de iniciación 11180292

2018 - 2019:
Synthesis, biological evaluation and computational studies of new pyrrolopyrimidines and purines derivatives as histamine 3 receptor antagonists. Proyecto de Investigación INICIO Nº I1707/2017, VRI-UC.

2014 - 2017:
Síntesis, evaluación biológica y estudios de acoplamiento molecular inducido de nuevos ligandos del receptor de histamina H4. Investigador responsable, CONICYT FONDECYT Postdoctorado.

Publicaciones

Espinosa-Bustos, C., Vázquez, K., Varela, J., Cerecetto, H., Paulino, M., Segura, R., Pizarro, J., Vera, B., González, M., Salas, C.O. New Aryloxy-Quinone Derivatives with Promising Activity on Trypanosoma cruzi. Archiv der Pharmazie, 2019, DOI: 10.1002/ardp.201900213

Bertrand, J., Dostálová, H., Kryštof, V., Jorda, R., Castro, A., Mella, J., Espinosa-Bustos, C., Zarate, A.M., Salas, C.O. New 2,6,9-trisubstituted purine derivatives as Bcr-Abl and Btk inhibitors and as promising agents against leukemia. Bioorganic Chemistry, 2019, https://doi.org/10.1016/j.bioorg.2019.103361

Del Valle, M.A. Gonzalez, B., Espinosa-Bustos, C., Ramirez, A., Gacitua, M. Hernandez, L. Ruthenium-Pyrrole and Thiophene Complexes for the Electrochemical Deposition of Metallopolymers with dsDNA Sensing Capabilities. International Journal of Electrochemical Science, 2019, 14: 8131-8140

Frank, A., Meza-Arriagada, F., Salas, C.O., Espinosa-Bustos, C., Stark, H. Nature-Inspired Pyrrolo[2,3-d]pyrimidines Targeting the Histamine H3 Receptor. Bioorganic & Medicinal Chemistry, 2019, 27: 3194-3200

Espinosa-Bustos, C., Mella, J., Soto-Delgado, J., Salas, C.O. State of the art of Smo antagonists for cancer therapy: Advances in the target receptor and new ligand structures. Future Medicinal Chemistry, 2019, 11(6), 617-638.

Espinosa-Bustos, C., Frank, A., Arancibia-Opazo, S., Salas, C.O., Fierro, A., Stark, H. New lead elements for histamine H3 receptor ligands in the pyrrolo[2,3-d]pyrimidine class. Bioorganic and Medicinal Chemistry Letters. 2018. 10.1016/j.bmcl.2018.07.023

Espinosa-Bustos, C., Canales, C., Ramírez, G., Jaque, P., Salas, C.O. Unveiling interactions between DNA and cytotoxic 2-arylpiperidinyl-1,4-naphthoquinone derivatives: A combined electrochemical and computational study. Arabian Journal of Chemistry. 2018. 10.1016/j.arabjc.2018.04.008

Cabrera, A.R., Espinosa-Bustos, C., Faundez, M., Meléndez, J., Jaque, P., Daniliuc, C.G., Aguirre, A., Rojas, R.S., Salas, C.O. New imidoyl-indazole platinum (II) complexes as potential anticancer agents: synthesis, evaluation of cytotoxicity, cell death and experimental-theoretical DNA interaction studies. Journal of Inorganic Biochemistry. 2017, 174: 90-101.

Espinosa-Bustos, C., Cortés-Arriagada, D., Soto-Arriaza, M., Robinson-Duggon, J., Pizarro, N., Cabrera, A.R., Fuentealba, D., Salas, C.O. Fluorescence Properties of Aurone Derivatives: An Experimental and Theoretical Study with Some Preliminary Biological Applications. Photochemical and Photobiological Sciences. 2017, 16(8): 1268-1276.

Antilén, M., Valencia, C., Peralta, E., Canales, C., Espinosa-Bustos, C., Escudey, M. Enrofloxacin behavior in presence of soil extracted organic matter: An electrochemical approach. Electrochimica Acta. 2017, 244: 104–111.

Cañete-Molina, A., Espinosa-Bustos, C., Gonzalez-Castro, M., Faundez, M., Mella, J., Tapia, R.A., Cabrera, A.R., Brito, I., Aguirre, A., Salas, C.O. Design, synthesis, cytotoxicity and 3D-QSAR analysis of new 3,6-disubstituted-1,2,4,5-tetrazine derivatives as potential antitumor agents. Arabian Journal of Chemistry. 2017; http://dx.doi.org/10.1016/j.arabjc.2017.04.002.

Espinosa-Bustos, C., Villegas, A., Salas, C.O. A convenient and simple synthesis of N-arylpirrolopyrimidines using boronic acids and promoted by copper (II) acetate. Arkivoc. 2017; part iv, 63-73.

Gonzalez, B., del Valle, M.A., Diaz, F.R., Espinosa-Bustos, C., Ramirez, A.M., Hernandez, L.A. Synthesis, characterization, electropolymerization, and possible utilities of a new ruthenium–thiophene complex. Journal of Applied Polymer Science. 2016; DOI: 10.1002/APP.43559.

Vasquez, K., Espinosa-Bustos, C., Soto-Delgado, J., Tapia, R.A., Varela, J., Birriel, E., Segura, R., Pizarro, J., Cerecetto, H., Gonzalez, M., Paulino, M., Salas, C.O. New aryloxy-quinone derivatives as potential anti-Chagasic agents: synthesis, trypanosomicidal activity, electrochemical properties, pharmacophore elucidation and 3D-QSAR analysis. RSC Advances. 2015; 5: 65153-65166.

Gonzalez, B., del Valle, M.A., Diaz, F.R., Espinosa-Bustos, C., Ramirez, A.M., Hernandez, L.A. Synthesis and electrochemical characterization of new ruthenium–terthiophene complexes. Polyhedron. 2015; 89: 232–237.

Calderon-Arancibia, J., Espinosa-Bustos, C., Cañete-Molina, A., Tapia, R.A., Faundez, M., Torres, M.J., Aguirre, A., Paulino, M., Salas, C.O. Synthesis and pharmacophore modelling of 2,6,9-trisubstituted purine derivatives and their potential role as apoptosis-inducing agents in cancer cell lines. Molecules. 2015; 20: 6808-6826.

Morales-Camilo, N., Salas, C., Sanhueza, C., Espinosa-Bustos, C., Sepúlveda-Boza, S., Reyes-Parada, M., González-Nilo, F., Caroli-Rezende, M., Fierro, A. Synthesis, biological evaluation, and molecular simulation of chalcones and aurones as selective MAO-B inhibitors. Chemical Biology & Drug Design. 2015; 85: 685–695.

Espinosa-Bustos, C., Lagos, C.F., Romero-Parra, J., Zárate, A.M., Mella-Raipán, J., Pessoa-Mahanna, H., Recabarren-Gajardo, G., Iturriaga-Vásquez, P., Tapia, R.A., Pessoa-Mahana, C.D. Design, synthesis, biological evaluation and binding mode modeling of benzimidazole derivatives targeting the cannabinoid receptor type 1. Archv. Der Pharmazie. 2015; 348, 1-8.

Sieveking, I., Thomas, P., Espinosa-Bustos, C., Fierro, A., Tapia, R., Salas, C., Quinones, N., Cuellar, M. et al. 2-phenylaminonaphthoquinones and related compounds: Synthesis, trypanocidal and cytotoxic activities. Bioorganic and Medicinal Chemistry. 2014; 22: 4609-4620.

Tapia, R., Salas, C., Vasquez, K., Espinosa-Bustos, C., Soto-Delgado, J, Varela, J., Birriel, E., Cerecetto, H., González, M., Paulino, M. Synthesis and biological characterization of nwe aryloxyindole-4,9-diones as potent trypanosomicidal agents. Bioorganic and Medicinal Chemistry Letters. 2014; 24: 3919-3922.

Mella-Raipán, J., Lagos, C., Recabarren-Gajardo, G, Espinosa-Bustos, C., Romero-Parra, J., Pessoa-Mahana, H., Iturriaga-Vasquez, P., Pessoa-Mahana, C. Design, Synthesis, Binding and Docking-Based 3D-QSAR Studies of 2-Pyridylbenzimidazoles-A New Family of High Affinity CB1 Cannabinoid Ligands. Molecules. 2013; 4, 18: 3972-4001.

Recabarren, G, Gacitúa, M., Murueva, I., Romero, J., Espinosa-Bustos, C., Mella, J., Del Valle, M., Pessoa, C., Tapia, R. Synthesis, characterization and electrochemical studies of new 5-and 6-nitro N-acyl-1H-indazoles. Journal of Physical Organic Chemistry. 2011; 24: 1179-1187.

Alvarez, M., Pessoa, C., Palavecino, M., Mella, J., Espinosa-Bustos, C, Lagos, M. Evaluation of the Membrane permeability (PAMPA and skin) of Benzimidazoles with potential cannabinoid activity and their relation with the biopharmaceutics classification system (BCS). Aaps Pharmscitech. 2011; 12: 573-578.

Pessoa-Mahana, D., Nuñez, A., Espinosa, C., Mella-Raipán, J., Pessoa-Mahana, H. Synthesis of a novel series of 4-Arylpiperazinyl Derivatives linked to a 2-(pyridin-3-yl)-1H-benzimidazole as new delavirdine analogues. Journal of the Brazilian Chemical Society. 2010; 21: 63-70.

Pessoa-Mahana, D., Espinosa-Bustos, C., Mella-Raipán, J., Canales-Pacheco, J., Pessoa-Mahana, H. Microwave-assisted synthesis and regioisomeric structural elucidation of novel benzimidazo[1,2d][1,4]benzodiazepinone derivatives. Arkivoc. 2009; Part 12: 131-140.

Redes

UC:
Cristian Salas S, Facultad de Química y de Farmacia.
Angélica Fierro, Facultad de Química y de Farmacia.
Mario Faúndez, Facultad de Química y de Farmacia.
Alan Cabrera, Facultad de Química y de Farmacia
Francisco Armijo, Facultad de Química y de Farmacia

Otras redes:
Holger Stark, Heinrich-Heine-University (Alemania)
José Antonio Arias-Montaño, Centro de Investigación y de Estudios Avanzados (Cinvestav) (México)
Ramón Estévez, Universidad de Santiago de Compostela (España)
Pablo Jaque, Universidad de Chile (Chile)

Premios y Distinciones

Premio Docente joven destacado de la Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Julio 2018.

Extensión y Divulgación

57° Congresso Brasileiro de Química. Título ponencia: Synthesis and cytotoxicity of 2,6,9-trisubstituted purines derivatives. Christian Espinosa-Bustos, Cristian Salas, Mario Faundez, Carlos Gallardo. Brasil, 2017.

18th Tetrahedron Symposium. Título ponencia: New 2,4,7-trisusbtituted pyrrolo[2,3-d]pyrimidine derivatives as histamine 3 receptor ligands. Christian Espinosa-Bustos, Cristian Salas, Annika Frank, Holger Stark. Hungría, 2017.

16th BMOS - Brazilian Meeting on Organic Synthesis. Título ponencia: Design and synthesis of new ligands for Hedgehog (Hh) receptors and their potential role as anti-cancer agents. A preliminary study. Ana María Zárate-Méndez, Christian Espinosa-Bustos, Marcos González-Castro, Matías González-Quiroz, Jaime Meléndez, Cristian O. Salas. Brasil, 2015.

44th National Organic Symposium. Título ponencia: Synthesis of 9-Benzyl-N-alkyl-9H-purin-6-amine Derivatives Designed as Ligands of the Histamine H4 Receptor. Christian Espinosa-Bustos, Cristian O. Salas. Estados Unidos, 2015.

Mechanisms of Hedgehog Signalling in Development, Tissue repair and Cancer. Título: Design and synthesis of new ligands for Hedgehog (Hh) receptors and their potential role as anti-cancer agents. A preliminary study. Ana María Zárate-Méndez, Matías González-Quiroz, Christian Espinosa-Bustos, Marcos González-Castro, Jaime Meléndez, Cristian O. Salas. Chile, 2015.

IUPAC World Chemistry Congress. Título: Synthesis and docking studies of new aryloxy heterocyclic quinones as potential trypanosomicidal agents. Ricardo A. Tapia, Cristian O. Salas, Karina Vázquez, Christian Espinosa, Javier Varela, Mercedes González, Hugo Cerecetto, Margot Paulino. Turquía, 2013.

NERM 2012, American Chemical Society 38th Northeast Regional Meeting. Título: Preliminary CB1 Binding Assays of a Novel Series of N-Acyl-2,5 Dimethoxyphenyl-1H-Benzimidazoles. Christian Espinosa-Bustos, Javier Romero-Parra, Carlos, F. Lagos, Ana Zárate, Jaime Mella-Raipán, Patricio Iturriaga-Vásquez, Ricardo A. Tapia, C. David Pessoa-Mahana. Estados Unidos, 2012.

VII Simposio Internacional de Química de Productos Naturales y sus Aplicaciones. Título: Estudio de Síntesis de Fenoxi-Indoloquinonas. Christian Espinosa-Bustos, C. D. Pessoa Mahana, Ricardo A. Tapia. Chile, 2012.

14TH Brazilian Meeting on Organic Synthesis. Título: Synthesis and Docking of New (2-(2,5-Dimethoxyphenyl)-1H-Benzo[d]Imidazol-1-yl)(Aryl)Methanone Derivatives Designed as Novel Cannabinoid CB1 Receptor Antagonists. Christian Espinosa-Bustos, Carlos Lagos, Javier Romero-Parra, Jaime Mella-Raipán, Hernán Pessoa-Mahana, Gonzalo Recabarren-Gajardo, C. David Pessoa-Mahana. Brasil, 2011.

13TH Brazilian Meeting on Organic Synthesis. Título: Novel Synthesis of 3-(2-aryl-1H-benzo[d]imidazolyl)-1,4-naphtoquinones using Molecular Iodine under Ultrasonic Irradiation. Christian Espinosa-Bustos, Edmundo Saéz, Ricardo Tapia, C. David Pessoa-Mahana, Gonzalo Recabarren-Gajardo. Brasil, 2009.