Publications


Books and special issues of scientific journals


2022

García, M. M.; Molina-Álvarez, M.; Rodríguez-Rivera, C.; Paniagua, N.; Quesada, E.; Uranga, J. A.; Rodríguez-Franco, M. I.; Pascual, D.; Goicoechea, C. Antinociceptive and modulatory effect of pathoplastic changes in spinal glia of a TLR4 /CD14 blocking molecule in two models of pain in rat. Biomed. Pharmacother. 2022, 150, 112986
(10.1016/j.biopha.2022.112986)



Herrera-Arozamena, C.; Estrada-Valencia, M.; López-Caballero, P.; Pérez, C.; Morales-García, J.; Pérez-Castillo, A.; del Sastre, E.; Fernández-Mendívil, C.; Duarte, P.; Michalska, P.; Lombardía, J.; Senar, S.; León, R.; López, M.G.; Rodríguez-Franco, M. I. Resveratrol-based MTDLs to stimulate defensive and regenerative pathways and block early events in neurodegenerative cascades. J. Med. Chem. 2022, 000 (Online ahead of print: March 4,2022)
https://doi.org/10.1021/acs.jmedchem.1c01883.



Duarte, P.; Michalska, P.; Crisman, E.; Cuadrado, A.; León, R. Novel Series of Dual NRF2 Inducers and Selective MAO-B Inhibitors for the Treatment of Parkinson’s Disease. Antioxidants 2022, 11 (2), 247.
https://doi.org/10.3390/antiox11020247.



Cores, Á.; Michalska, P.; Pérez, J. M.; Crisman, E.; Gómez, C.; Villacampa, M.; Menéndez, J. C.; León, R. Enantioselective Synthesis and Pharmacological Evaluation of Aza-CGP37157–Lipoic Acid Hybrids for the Treatment of Alzheimer’s Disease. Antioxidants 2022, 11 (1), 112.
https://doi.org/10.3390/antiox11010112.



Cores, Á.; Carmona-Zafra, N.; Martín-Cámara, O.; Sánchez, J. D.; Duarte, P.; Villacampa, M.; Bermejo-Bescós, P.; Martín-Aragón, S.; León, R.; Menéndez, J. C. Curcumin-Piperlongumine Hybrids with a Multitarget Profile Elicit Neuroprotection in In Vitro Models of Oxidative Stress and Hyperphosphorylation. Antioxidants 2021, 11 (1), 28.
https://doi.org/10.3390/antiox11010028.


2021

Codony, S.; Calvó-Tusell, C.; Valverde, E.; Osuna, S.; Morisseau, C.; Loza, M. I.; Brea, J.; Pérez, C.; Rodríguez-Franco, M. I.; Pizarro-Delgado, J.; Corpas, R.; Griñán-Ferré, C.; Pallàs, M.; Sanfeliu, C.; Vázquez-Carrera, M.; Hammock, B. D.; Feixas, F.; Vázquez, S. From the Design to the In Vivo Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis. J. Med. Chem. 2021 , 64 (9), 5429–5446.
https://doi.org/10.1021/acs.jmedchem.0c01601.
This work received the 2021 Prize for the Best Publication, granted by the Spanish Society of Therapeutic Chemistry (SEQT).



Delogu, G. L.; Kumar, A.; Gatto, G.; Bustelo, F.; Saavedra, L. M.; Rodríguez-Franco, M. I.; Laguna, R.; Viña, D. Synthesis and in Vitro Study of Nitro- and Methoxy-2-Phenylbenzofurans as Human Monoamine Oxidase Inhibitors. Bioorg. Chem. 2021, 104616.
https://doi.org/10.1016/j.bioorg.2020.104616.



Nozal, V.; García‐Rubia, A.; Cuevas, E. P.; Pérez, C.; Tosat-Bitrián, C.; Bartolomé, F.; Carro, E.; Ramírez, D.; Palomo, V.; Martínez, A. From Kinase Inhibitors to Multitarget Ligands as Powerful Drug Leads for Alzheimer’s Disease Using Protein-Templated Synthesis. Angew. Chem. Int. Ed. 2021, 60 (35), 19344–19354.
https://doi.org/10.1002/anie.202106295.



Cores, Á.; Abril, S.; Michalska, P.; Duarte, P.; Olives, A. I.; Martín, M. A.; Villacampa, M.; León, R.; Menéndez, J. C. Bisavenathramide Analogues as Nrf2 Inductors and Neuroprotectors in In Vitro Models of Oxidative Stress and Hyperphosphorylation. Antioxidants 2021, 10 (6), 941.
https://doi.org/10.3390/antiox10060941.



Grieco, I.; Bissaro, M.; Tiz, D. B.; Perez, D. I.; Perez, C.; Martinez, A.; Redenti, S.; Mariotto, E.; Bortolozzi, R.; Viola, G.; Cozza, G.; Spalluto, G.; Moro, S.; Federico, S. Developing Novel Classes of Protein Kinase CK1δ Inhibitors by Fusing [1,2,4]Triazole with Different Bicyclic Heteroaromatic Systems. Eur. J. Med. Chem. 2021, 216, 113331.
https://doi.org/10.1016/j.ejmech.2021.113331.



Rojas-Prats, E.; Martinez-Gonzalez, L.; Gonzalo-Consuegra, C.; Liachko, N. F.; Perez, C.; Ramírez, D.; Kraemer, B. C.; Martin-Requero, Á.; Perez, D. I.; Gil, C.; de Lago, E.; Martinez, A. Targeting Nuclear Protein TDP-43 by Cell Division Cycle Kinase 7 Inhibitors: A New Therapeutic Approach for Amyotrophic Lateral Sclerosis. Eur. J. Med. Chem. 2021, 210.
https://doi.org/10.1016/j.ejmech.2020.112968.



Davies, M. P.; Benitez, R.; Perez, C.; Jakupovic, S.; Welsby, P.; Rzepecka, K.; Alder, J.; Davidson, C.; Martinez, A.; Hayes, J. M. Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3β. J. Med. Chem. 2021, 64 (3), 1497–1509.
https://doi.org/10.1021/acs.jmedchem.0c01568.



González-Ruiz, V.; Cores, Á.; Martín-Cámara, O.; Orellana, K.; Cervera-Carrascón, V.; Michalska, P.; Olives, A. I.; León, R.; Martín, M. A.; Menéndez, J. C. Enhanced Stability and Bioactivity of Natural Anticancer Topoisomerase I Inhibitors through Cyclodextrin Complexation. Pharmaceutics 2021, 13 (10), 1609.
https://doi.org/10.3390/pharmaceutics13101609.



Gürbüz, P.; Dokumacı, A. H.; Gündüz, M. G.; Perez, C.; Göger, F.; Paksoy, M. Y.; Yerer, M. B.; Ömür Demirezer, L. In Vitro Biological Activity of Salvia Fruticosa Mill. Infusion against Amyloid β-Peptide-Induced Toxicity and Inhibition of GSK-3β, CK-1δ, and BACE-1 Enzymes Relevant to Alzheimer’s Disease. Saudi Pharm. J. 2021, 29 (3), 236–243.
https://doi.org/10.1016/j.jsps.2021.01.007.


2020

Herrera-Arozamena, C.; Estrada-Valencia, M.; Martí-Marí, O.; Pérez, C.; de la Fuente Revenga, M.; Villalba-Galea, C. A.; Rodríguez-Franco, M. I. Optical Control of Muscular Nicotinic Channels with Azocuroniums, Photoswitchable Azobenzenes Bearing Two N-Methyl-N-Carbocyclic Quaternary Ammonium Groups. Eur. J. Med. Chem. 2020, 200, 112403.
https://doi.org/10.1016/j.ejmech.2020.112403.



Herrera-Arozamena, C.; Estrada-Valencia, M.; Pérez, C.; Lagartera, L.; Morales-García, J. A.; Pérez-Castillo, A.; Franco-Gonzalez, J. F.; Michalska, P.; Duarte, P.; León, R.; López, M. G.; Mills, A.; Gago, F.; García-Yagüe, Á. J.; Fernández-Ginés, R.; Cuadrado, A.; Rodríguez-Franco, M. I. Tuning Melatonin Receptor Subtype Selectivity in Oxadiazolone-Based Analogues: Discovery of QR2 Ligands and NRF2 Activators with Neurogenic Properties. Eur. J. Med. Chem. 2020, 190, 112090.
https://doi.org/10.1016/j.ejmech.2020.112090.



Codony, S.; Pujol, E.; Pizarro, J.; Feixas, F.; Valverde, E.; Loza, M. I.; Brea, J. M.; Saez, E.; Oyarzabal, J.; Pineda-Lucena, A.; Pérez, B.; Pérez, C.; Rodríguez-Franco, M. I.; Leiva, R.; Osuna, S.; Morisseau, C.; Hammock, B. D.; Vázquez-Carrera, M.; Vázquez, S. 2-Oxaadamant-1-Yl Ureas as Soluble Epoxide Hydrolase Inhibitors: In Vivo Evaluation in a Murine Model of Acute Pancreatitis. J. Med. Chem. 2020, 63 (17), 9237–9257.
https://doi.org/10.1021/acs.jmedchem.0c00310.



Michalska, P.; Mayo, P.; Fernández-Mendívil, C.; Tenti, G.; Duarte, P.; Buendia, I.; Ramos, M. T.; López, M. G.; Menéndez, J. C.; León, R. Antioxidant, Anti-Inflammatory and Neuroprotective Profiles of Novel 1,4-Dihydropyridine Derivatives for the Treatment of Alzheimer’s Disease. Antioxidants 2020, 9 (8), 650.
https://doi.org/10.3390/antiox9080650.



Michalska, P.; Tenti, G.; Satriani, M.; Cores, A.; Ramos, M. T.; García, A. G.; Menéndez, J. C.; León, R. Aza-CGP37157-lipoic Hybrids Designed as Novel Nrf2-inducers and Antioxidants Exert Neuroprotection against Oxidative Stress and Show Neuroinflammation Inhibitory Properties. Drug Dev. Res. 2020, 81 (3), 283–294.
https://doi.org/10.1002/ddr.21618.



Espadinha, M.; Viejo, L.; Lopes, R. M. R. M.; Herrera-Arozamena, C.; Molins, E.; dos Santos, D. J. V. A.; Gonçalves, L.; Rodríguez-Franco, M. I.; Ríos, C. de los; Santos, M. M. M. Identification of Tetracyclic Lactams as NMDA Receptor Antagonists with Potential Application in Neurological Disorders. Eur. J. Med. Chem. 2020, 194, 112242.
https://doi.org/10.1016/j.ejmech.2020.112242.



Michalska, P.; Buendia, I.; Duarte, P.; FernandezMendivil, C.; Negredo, P.; Cuadrado, A.; López, M. G.; Leon, R. Melatonin-Sulforaphane Hybrid ITH12674 Attenuates Glial Response in Vivo by Blocking LPS Binding to MD2 and Receptor Oligomerization. Pharmacol. Res. 2020, 152, 104597.
https://doi.org/10.1016/j.phrs.2019.104597.



González-Naranjo, P.; Pérez, C.; Girón, R.; Sánchez-Robles, E. M.; Martín-Fontelles, M. I.; Carrillo-López, N.; Martín-Vírgala, J.; Naves, M.; Campillo, N. E.; Páez, J. A. New Cannabinoid Receptor Antagonists as Pharmacological Tool. Bioorg. Med. Chem. 2020, 28 (19), 115672.
https://doi.org/10.1016/j.bmc.2020.115672.



Campello, L.; Kutsyr, O.; Noailles, A.; Michalska, P.; Fernández-Sánchez, L.; Martínez-Gil, N.; Ortuño-Lizarán, I.; Sánchez-Sáez, X.; de Juan, E.; Lax, P.; León, R.; García, A. G.; Cuenca, N.; Maneu, V. New Nrf2-Inducer Compound ITH12674 Slows the Progression of Retinitis Pigmentosa in the Mouse Model Rd10. Cell. Physiol. Biochem. 2020 , 54 (1), 142–159.
https://doi.org/10.33594/000000210.



Di Martino, R. M. C.; Pruccoli, L.; Bisi, A.; Gobbi, S.; Rampa, A.; Martinez, A.; Pérez, C.; Martinez-Gonzalez, L.; Paglione, M.; Di Schiavi, E.; Seghetti, F.; Tarozzi, A.; Belluti, F. Novel Curcumin-Diethyl Fumarate Hybrid as a Dualistic GSK-3β Inhibitor/Nrf2 Inducer for the Treatment of Parkinson’s Disease. ACS Chem. Neurosci. 2020 , 11 (17), 2728–2740.
https://doi.org/10.1021/acschemneuro.0c00363.



Cores, Á.; Piquero, M.; Villacampa, M.; León, R.; Menéndez, J. C. NRF2 Regulation Processes as a Source of Potential Drug Targets against Neurodegenerative Diseases.Biomolecules 2020, 10 (6), 904.
https://doi.org/10.3390/biom10060904.



Nuñez-Borque, E.; González-Naranjo, P.; Bartolomé, F.; Alquézar, C.; Reinares-Sebastián, A.; Pérez, C.; Ceballos, M. L.; Páez, J. A.; Campillo, N. E.; Martín-Requero, Á. Targeting Cannabinoid Receptor Activation and BACE-1 Activity Counteracts TgAPP Mice Memory Impairment and Alzheimer’s Disease Lymphoblast Alterations. Mol. Neurobiol. 2020, 57 (4), 1938–1951.
https://doi.org/10.1007/s12035-019-01813-4.



Michalska, P.; León, R. When It Comes to an End: Oxidative Stress Crosstalk with Protein Aggregation and Neuroinflammation Induce Neurodegeneration. Antioxidants 2020, 9 (8), 740.
https://doi.org/10.3390/antiox9080740.



DLassagne, F.; Duguépéroux, C.; Roca, C.; Perez, C.; Martinez, A.; Baratte, B.; Robert, T.; Ruchaud, S.; Bach, S.; Erb, W.; Roisnel, T.; Mongin, F. From Simple Quinoxalines to Potent Oxazolo[5,4- f ]Quinoxaline Inhibitors of Glycogen-Synthase Kinase 3 (GSK3). Org. Biomol. Chem. 2020, 18 (1), 154–162.
https://doi.org/10.1039/C9OB02002K.


2019

Estrada-Valencia, M.; Herrera-Arozamena, C.; Pérez, C.; Viña, D.; Morales-García, J. A.; Pérez-Castillo, A.; Ramos, E.; Romero, A.; Laurini, E.; Pricl, S.; Rodríguez-Franco, M. I. New Flavonoid – N,N-Dibenzyl(N-Methyl)Amine Hybrids: Multi-Target-Directed Agents for Alzheimer´s Disease Endowed with Neurogenic Properties. J. Enzyme Inhib. Med. Chem. 2019, 34 (1), 712–727.
https://doi.org/10.1080/14756366.2019.1581184.



González-Naranjo, P.; Pérez-Macias, N.; Pérez, C.; Roca, C.; Vaca, G.; Girón, R.; Sánchez-Robles, E.; Martín-Fontelles, M. I.; de Ceballos, M. L.; Martin-Requero, A.; Campillo, N. E.; Páez, J. A. Indazolylketones as New Multitarget Cannabinoid Drugs. Eur. J. Med. Chem. 2019, 166, 90–107.
https://doi.org/10.1016/j.ejmech.2019.01.030.



Gürbüz, P.; Martinez, A.; Pérez, C.; Martínez-González, L.; Göger, F.; Ayran, İ. Potential Anti-Alzheimer Effects of Selected Lamiaceae Plants through Polypharmacology on Glycogen Synthase Kinase-3β, β-Secretase, and Casein Kinase 1δ. Ind. Crops Prod. 2019, 138, 111431.
https://doi.org/10.1016/j.indcrop.2019.05.080.



Herrera-Arozamena, C.; Estrada-Valencia, M. H.; Villalba-Galea, C. A.; Rodriguez-Franco, M. I. Structure-Activity Relationship of Potent Photo-Switchable Neuromuscular Inhibitors. Biophys. J. 2019, 116 (3), 395a.
https://doi.org/10.1016/j.bpj.2018.11.2134.



Lassagne, F.; Duguépéroux, C.; Roca, C.; Perez, C.; Martinez, A.; Baratte, B.; Robert, T.; Ruchaud, S.; Bach, S.; Erb, W.; Roisnel, T.; Mongin, F. From Simple Quinoxalines to Potent Oxazolo[5,4- f ]Quinoxaline Inhibitors of Glycogen-Synthase Kinase 3 (GSK3). Org. Biomol. Chem. 2020, 18 (1), 154–162.
https://doi.org/10.1039/C9OB02002K.



Luengo, E.; Buendia, I.; Fernández‐Mendívil, C.; Trigo‐Alonso, P.; Negredo, P.; Michalska, P.; Hernández‐García, B.; Sánchez‐Ramos, C.; Bernal, J. A.; Ikezu, T.; León, R.; López, M. G. Pharmacological Doses of Melatonin Impede Cognitive Decline in Tau‐related Alzheimer Models, Once Tauopathy Is Initiated, by Restoring the Autophagic Flux. J. Pineal Res. 2019, e12578.
https://doi.org/10.1111/jpi.12578.



Páez, J. A.; Campillo, N. E. Innovative Therapeutic Potential of Cannabinoid Receptors as Targets in Alzheimer’s Disease and Less Well-Known Diseases. Curr. Med. Chem. 2019, 26 (18), 3300–3340.
https://doi.org/10.2174/0929867325666180226095132.



Ponzoni, I.; Sebastián-Pérez, V.; Martínez, M. J.; Roca, C.; De la Cruz Pérez, C.; Cravero, F.; Vazquez, G. E.; Páez, J. A.; Díaz, M. F.; Campillo, N. E. QSAR Classification Models for Predicting the Activity of Inhibitors of Beta-Secretase (BACE1) Associated with Alzheimer’s Disease. Sci. Rep. 2019, 9 (1), 9102.
https://doi.org/10.1038/s41598-019-45522-3.



Redenti, S.; Marcovich, I.; De Vita, T.; Pérez, C.; De Zorzi, R.; Demitri, N.; Perez, D. I.; Bottegoni, G.; Bisignano, P.; Bissaro, M.; Moro, S.; Martinez, A.; Storici, P.; Spalluto, G.; Cavalli, A.; Federico, S. A Triazolotriazine‐Based Dual GSK‐3β/CK‐1δ Ligand as a Potential Neuroprotective Agent Presenting Two Different Mechanisms of Enzymatic Inhibition. ChemMedChem 2019, 14 (3), 310–314.
https://doi.org/10.1002/cmdc.201800778.



Rubio-Navarro, A.; Vázquez-Carballo, C.; Guerrero-Hue, M.; García-Caballero, C.; Herencia, C.; Gutiérrez, E.; Yuste, C.; Sevillano, Á.; Praga, M.; Egea, J.; Cannata, P.; Cortegano, I.; de Andrés, B.; Gaspar, M. L.; Cadenas, S.; Michalska, P.; León, R.; Ortiz, A.; Egido, J.; Moreno, J. A. Nrf2 Plays a Protective Role Against Intravascular Hemolysis-Mediated Acute Kidney Injury. Front. Pharmacol. 2019, 10.
https://doi.org/10.3389/fphar.2019.00740.



Romero, A.; San Hipólito-Luengo, Á.; Villalobos, L. A.; Vallejo, S.; Valencia, I.; Michalska, P.; Pajuelo‐Lozano, N.; Sánchez‐Pérez, I.; León, R.; Bartha, J. L.; Sanz, M. J.; Erusalimsky, J. D.; Sánchez-Ferrer, C. F.; Romacho, T.; Peiró, C. The Angiotensin-(1-7)/Mas Receptor Axis Protects from Endothelial Cell Senescence via Klotho and Nrf2 Activation. Aging Cell 2019, 18 (3), e12913.
https://doi.org/10.1111/acel.12913.



Sciú, M. L.; Sebastián-Pérez, V.; Martinez-Gonzalez, L.; Benitez, R.; Perez, D. I.; Pérez, C.; Campillo, N. E.; Martinez, A.; Moyano, E. L. Computer-Aided Molecular Design of Pyrazolotriazines Targeting Glycogen Synthase Kinase 3. J. Enzyme Inhib. Med. Chem. 2019, 34 (1), 87–96.
https://doi.org/10.1080/14756366.2018.1530223.



Venter, J.; Perez, C.; van Otterlo, W. A. L.; Martínez, A.; Blackie, M. A. L. 1-Aryl-3-(4-Methoxybenzyl)Ureas as Potentially Irreversible Glycogen Synthase Kinase 3 Inhibitors: Synthesis and Biological Evaluation. Bioorg. Med. Chem. Lett. 2019, 29 (13), 1597–1600.
https://doi.org/10.1016/j.bmcl.2019.04.049.


2018

Vera-Puente, O.; Rodriguez-Antolin, C.; Salgado-Figueroa, A.; Michalska, P.; Pernia, O.; Reid, B. M.; Rosas, R.; Garcia-Guede, A.; SacristÁn, S.; Jimenez, J.; Esteban-Rodriguez, I.; Martin, M. E.; Sellers, T. A.; León, R.; Gonzalez, Ví. M.; De Castro, J.; Ibanez de Caceres, I. MAFG Is a Potential Therapeutic Target to Restore Chemosensitivity in Cisplatin-Resistant Cancer Cells by Increasing Reactive Oxygen Species. Transl. Res. 2018, 200, 1–17.
https://doi.org/10.1016/j.trsl.2018.06.005.



Benek, O.; Hroch, L.; Aitken, L.; Gunn-Moore, F.; Vinklarova, L.; Kuca, K.; Perez, D. I.; Perez, C.; Martinez, A.; Fisar, Z.; Musilek, K. 1-(Benzo[ d ]Thiazol-2-Yl)-3-Phenylureas as Dual Inhibitors of Casein Kinase 1 and ABAD Enzymes for Treatment of Neurodegenerative Disorders. J. Enzyme Inhib. Med. Chem. 2018, 33 (1), 665–670.
https://doi.org/10.1080/14756366.2018.1445736.



Chierrito, T. P. C.; Pedersoli-Mantoani, S.; Roca, C.; Sebastian-Pérez, V.; Martínez-Gonzalez, L.; Pérez, D. I.; Perez, C.; Canales, A.; Cañada, F. J.; Campillo, N. E.; Carvalho, I.; Martinez, A. Chameleon-like Behavior of Indolylpiperidines in Complex with Cholinesterases Targets: Potent Butyrylcholinesterase Inhibitors. Eur. J. Med. Chem. 2018, 145, 431–444.
https://doi.org/10.1016/j.ejmech.2018.01.007.



Cuadrado, A.; Manda, G.; Hassan, A.; Alcaraz, M. J.; Barbas, C.; Daiber, A.; Ghezzi, P.; León, R.; López, M. G.; Oliva, B.; Pajares, M.; Rojo, A. I.; Robledinos-Antón, N.; Valverde, A. M.; Guney, E.; Schmidt, H. H. H. W. Transcription Factor NRF2 as a Therapeutic Target for Chronic Diseases: A Systems Medicine Approach. Pharmacol. Rev. 2018, 70 (2), 348–383.
https://doi.org/10.1124/pr.117.014753.



del Cerro, P.; Alquézar, C.; Bartolomé, F.; González-Naranjo, P.; Pérez, C.; Carro, E.; Páez, J. A.; Campillo, N. E.; Martín-Requero, Á. Activation of the Cannabinoid Type 2 Receptor by a Novel Indazole Derivative Normalizes the Survival Pattern of Lymphoblasts from Patients with Late-Onset Alzheimer’s Disease. CNS Drugs 2018 , 32 (6), 579–591.
https://doi.org/10.1007/s40263-018-0515-7.



Estrada Valencia, M.; Herrera-Arozamena, C.; de Andrés, L.; Pérez, C.; Morales-García, J. A.; Pérez-Castillo, A.; Ramos, E.; Romero, A.; Viña, D.; Yáñez, M.; Laurini, E.; Pricl, S.; Rodríguez-Franco, M. I. Neurogenic and Neuroprotective Donepezil-Flavonoid Hybrids with Sigma-1 Affinity and Inhibition of Key Enzymes in Alzheimer’s Disease. Eur. J. Med. Chem. 2018, 156, 534–553.
https://doi.org/10.1016/j.ejmech.2018.07.026.



Figueiro-Silva, J.; Antequera, D.; Pascual, C.; de la Fuente Revenga, M.; Volt, H.; Acuña-Castroviejo, D.; Rodríguez-Franco, M. I.; Carro, E. The Melatonin Analog IQM316 May Induce Adult Hippocampal Neurogenesis and Preserve Recognition Memories in Mice. Cell Transplant. 2018, 27 (3), 423–437.
https://doi.org/10.1177/0963689717721217.



Gandini, A.; Bartolini, M.; Tedesco, D.; Martinez-Gonzalez, L.; Roca, C.; Campillo, N. E.; Zaldivar-Diez, J.; Perez, C.; Zuccheri, G.; Miti, A.; Feoli, A.; Castellano, S.; Petralla, S.; Monti, B.; Rossi, M.; Moda, F.; Legname, G.; Martinez, A.; Bolognesi, M. L. Tau-Centric Multitarget Approach for Alzheimer’s Disease: Development of First-in-Class Dual Glycogen Synthase Kinase 3β and Tau-Aggregation Inhibitors. J. Med. Chem. 2018, 61 (17), 7640–7656.
https://doi.org/10.1021/acs.jmedchem.8b00610.



Herrera-Arozamena, C.; Martí-Marí, O.; Estrada, M.; Dela Fuente-Revenga, M.; Villalba-Galea, C. A.; Isabel Rodríguez-Franco, M. Functional Characterization of Novel Photo-Switchable Neuromuscular Blockers. Biophys. J. 2018, 114 (3), 297a.
https://doi.org/10.1016/j.bpj.2017.11.1696.



Martin-de-Saavedra, M. D.; Navarro, E.; Moreno-Ortega, A. J.; Cunha, M. P.; Buendia, I.; Hernansanz-Agustín, P.; León, R.; Cano-Abad, M. F.; Martínez-Ruiz, A.; Martínez-Murillo, R.; Duchen, M. R.; López, M. G. The APPswe/PS1A246E Mutations in an Astrocytic Cell Line Leads to Increased Vulnerability to Oxygen and Glucose Deprivation, Ca 2+ Dysregulation, and Mitochondrial Abnormalities. J. Neurochem. 2018, 145 (2), 170–182.
https://doi.org/10.1111/jnc.14293.



Reis, J.; Cagide, F.; Valencia, M. E.; Teixeira, J.; Bagetta, D.; Pérez, C.; Uriarte, E.; Oliveira, P. J.; Ortuso, F.; Alcaro, S.; Rodríguez-Franco, M. I.; Borges, F. Multi-Target-Directed Ligands for Alzheimer’s Disease: Discovery of Chromone-Based Monoamine Oxidase/Cholinesterase Inhibitors. Eur. J. Med. Chem. 2018, 158, 781–800.
https://doi.org/10.1016/j.ejmech.2018.07.056.



Roca, C.; Requena, C.; Sebastián-Pérez, V.; Malhotra, S.; Radoux, C.; Pérez, C.; Martinez, A.; Antonio Páez, J.; Blundell, T. L.; Campillo, N. E. Identification of New Allosteric Sites and Modulators of AChE through Computational and Experimental Tools. J. Enzyme Inhib. Med. Chem. 2018, 33 (1), 1034–1047.
https://doi.org/10.1080/14756366.2018.1476502.


2017

Barbado, M. V.; Medrano, M.; Caballero-Velázquez, T.; Álvarez-Laderas, I.; Sánchez-Abarca, L. I.; García-Guerrero, E.; Martín-Sánchez, J.; Rosado, I. V.; Piruat, J. I.; Gonzalez-Naranjo, P.; Campillo, N. E.; Páez, J. A.; Pérez-Simón, J. A. Cannabinoid Derivatives Exert a Potent Anti-Myeloma Activity Both in Vitro and in Vivo. Int. J. Cancer 2017, 140 (3), 674–685.
https://doi.org/10.1002/ijc.30483.



Chierrito, T. P. C.; Pedersoli-Mantoani, S.; Roca, C.; Requena, C.; Sebastian-Perez, V.; Castillo, W. O.; Moreira, N. C. S.; Pérez, C.; Sakamoto-Hojo, E. T.; Takahashi, C. S.; Jiménez-Barbero, J.; Cañada, F. J.; Campillo, N. E.; Martinez, A.; Carvalho, I. From Dual Binding Site Acetylcholinesterase Inhibitors to Allosteric Modulators: A New Avenue for Disease-Modifying Drugs in Alzheimer’s Disease. Eur. J. Med. Chem. 2017, 139, 773–791.
https://doi.org/10.1016/j.ejmech.2017.08.051.



Espadinha, M.; Dourado, J.; Lajarin-Cuesta, R.; Herrera-Arozamena, C.; Gonçalves, L. M. D.; Rodríguez-Franco, M. I.; de los Rios, C.; Santos, M. M. M. Optimization of Bicyclic Lactam Derivatives as NMDA Receptor Antagonists. ChemMedChem 2017 , 12 (7), 537–545.
https://doi.org/10.1002/cmdc.201700037.



Fernández, S.; Giglio, J.; Reyes, A. L.; Damián, A.; Pérez, C.; Pérez, D. I.; González, M.; Oliver, P.; Rey, A.; Engler, H.; Cerecetto, H. 3-(Benzyloxy)-1-(5-[ 18 F]Fluoropentyl)-5-Nitro-1 H -Indazole: A PET Radiotracer to Measure Acetylcholinesterase in Brain. Future Med. Chem. 2017, 9 (10), 983–994.
https://doi.org/10.4155/fmc-2017-0023.



Gameiro, I.; Michalska, P.; Tenti, G.; Cores, Á.; Buendia, I.; Rojo, A. I.; Georgakopoulos, N. D.; Hernández-Guijo, J. M.; Teresa Ramos, M.; Wells, G.; López, M. G.; Cuadrado, A.; Menéndez, J. C.; León, R. Discovery of the First Dual GSK3β Inhibitor/Nrf2 Inducer. A New Multitarget Therapeutic Strategy for Alzheimer’s Disease. Sci. Rep. 2017, 7 (1), 45701.
https://doi.org/10.1038/srep45701.



García, A.; Brea, J.; González-García, A.; Pérez, C.; Cadavid, M. I.; Loza, M. I.; Martinez, A.; Gil, C. Targeting PDE10A GAF Domain with Small Molecules: A Way for Allosteric Modulation with Anti-Inflammatory Effects. Molecules 2017, 22 (9), 1472.
https://doi.org/10.3390/molecules22091472.



Guerra, A.; Gonzalez-Naranjo, P.; Campillo, N. E.; Varela, J.; Lavaggi, M. L.; Merlino, A.; Cerecetto, H.; González, M.; Gomez-Barrio, A.; Escario, J. A.; Fonseca-Berzal, C.; Yaluf, G.; Paniagua-Solis, J.; Páez, J. A. 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. Eur. J. Med. Chem. 2017 , 136, 223–234.
https://doi.org/10.1016/j.ejmech.2017.04.075.



Herrera-Arozamena, C.; Martí-Marí, O.; de la Fuente Revenga, M.; Villalba-Galea, C. A.; Rodríguez-Franco, M. I. New Photoswitchable Neuromuscular Blockers: Design, Synthesis, and Physicochemical / Biological Evaluation. J. Neurochem. 2017, 142, 123.
https://doi.org/10.1111/jnc.14093.



Mansilla, A.; Chaves-Sanjuan, A.; Campillo, N. E.; Semelidou, O.; Martínez-González, L.; Infantes, L.; González-Rubio, J. M.; Gil, C.; Conde, S.; Skoulakis, E. M. C.; Ferrús, A.; Martínez, A.; Sánchez-Barrena, M. J. Interference of the Complex between NCS-1 and Ric8a with Phenothiazines Regulates Synaptic Function and Is an Approach for Fragile X Syndrome. Proc. Natl. Acad. Sci. 2017, 114 (6), E999–E1008.
https://doi.org/10.1073/pnas.1611089114.



Monjas, L.; Arce, M. P.; León, R.; Egea, J.; Pérez, C.; Villarroya, M.; López, M. G.; Gil, C.; Conde, S.; Rodríguez-Franco, M. I. Enzymatic and Solid-Phase Synthesis of New Donepezil-Based L- and d -Glutamic Acid Derivatives and Their Pharmacological Evaluation in Models Related to Alzheimer’s Disease and Cerebral Ischemia. Eur. J. Med. Chem. 2017, 130, 60–72.
https://doi.org/10.1016/j.ejmech.2017.02.034.



Morales-García, J. A.; de la Fuente Revenga, M.; Alonso-Gil, S.; Rodríguez-Franco, M. I.; Feilding, A.; Perez-Castillo, A.; Riba, J. The Alkaloids of Banisteriopsis Caapi, the Plant Source of the Amazonian Hallucinogen Ayahuasca, Stimulate Adult Neurogenesis in Vitro. Sci. Rep. 2017, 7 (1), 5309. https://doi.org/10.1038/s41598-017-05407-9. Altmetric score (which calculates a score based on the attention given to an article): 176. This article is in the 98th percentile (ranked 4,254th) of the 279,324 tracked articles of a similar age in all journals and the 97th percentile (ranked 13th) of the 499 tracked articles of a similar age in Scientific Reports,( https://www.nature.com/articles/s41598-017-05407-9/metrics, accessed January 13, 2022).



Palomo, V.; Perez, D. I.; Roca, C.; Anderson, C.; Rodríguez-Muela, N.; Perez, C.; Morales-Garcia, J. A.; Reyes, J. A.; Campillo, N. E.; Perez-Castillo, A. M.; Rubin, L. L.; Timchenko, L.; Gil, C.; Martinez, A. Subtly Modulating Glycogen Synthase Kinase 3 β: Allosteric Inhibitor Development and Their Potential for the Treatment of Chronic Diseases. J. Med. Chem. 2017, 60 (12), 4983–5001.
https://doi.org/10.1021/acs.jmedchem.7b00395.



Ponzoni, I.; Sebastián-Pérez, V.; Requena-Triguero, C.; Roca, C.; Martínez, M. J.; Cravero, F.; Díaz, M. F.; Páez, J. A.; Arrayás, R. G.; Adrio, J.; Campillo, N. E. Hybridizing Feature Selection and Feature Learning Approaches in QSAR Modeling for Drug Discovery. Sci. Rep. 2017, 7 (1), 2403.
https://doi.org/10.1038/s41598-017-02114-3.



Punzón, E.; García-Alvarado, F.; Maroto, M.; Fernández-Mendívil, C.; Michalska, P.; García-Álvarez, I.; Arranz-Tagarro, J. A.; Buendia, I.; López, M. G.; León, R.; Gandía, L.; Fernández-Mayoralas, A.; García, A. G. Novel Sulfoglycolipid IG20 Causes Neuroprotection by Activating the Phase II Antioxidant Response in Rat Hippocampal Slices. Neuropharmacology 2017, 116, 110–121.
https://doi.org/10.1016/j.neuropharm.2016.12.016.



Efentakis, P.; Rizakou, A.; Christodoulou, E.; Chatzianastasiou, A.; López, M. G.; León, R.; Balafas, E.; Kadoglou, N. P. E.; Tseti, I.; Skaltsa, H.; Kostomitsopoulos, N.; Iliodromitis, E. K.; Valsami, G.; Andreadou, I. Saffron (Crocus sativus) intake provides nutritional preconditioning against myocardial ischemia-reperfusion injury in wild type and Apo-E(-/-) mice: Involvement of Nrf2 activation. Nut., Met. & Card. Dis., 2017, 27, 919-929.
https://doi.org/10.1016/j.numecd.2017.08.005.



Michalska, P.; Buendia, I.; Del Barrio, L.; León, R. Novel multitarget hybrid compounds for the treatment of Alzheimer’s disease. Curr. Top. Med. Chem. 2017, 19, 1027-1043.
https://doi.org/10.2174/1568026616666160927154116.



Rieger, D. K.; Navarro, E.; Buendia, I.; Parada, E.; González-Lafuente, L.; León, R.; Costa, A. P.; Heinrich, I. A.; Nascimento, K. S.; Cavada, B. S.; López, M. G.; Egea, J.; Leal, R. B. ConBr, a lectin purified from the seeds of Canavalia brasileiensis, protects against ischemia in organotypic culture of rat hippocampus: Potential implication of voltage gated calcium channels. Neurochemical Research, 2017, 42, 347-359.
https://doi.org/10.1007/s11064-016-2078-7



Buendia, I.; Tenti, G.; Michalska, P.; Méndez-López, I.; Luengo, E.; Satriani, M.; Padín-Nogueira, F.; López, M. G.; Ramos, M. T.; García, A. G.; Menéndez, J. C.; León, R. ITH14001, a CGP37157-nimodipine hybrid designed to regulate calcium homeostasis and oxidative stress, exerts neuroprotection in cerebral ischemia. ACS Chem. Neurosci. 2017, 8, 67-81.
https://doi.org/10.1021/acschemneuro.6b00181



Michalska, P.; Wojnicz, A.; Ruiz-Nuño, A.; Abril, S.; Buendia, I.; León, R. Inclusion complex of ITH12674 with 2-hydroxypropyl--cyclodextrin: Preparation, physical characterization and pharmacological effect. Carbohydrate Polymers, 2017, 157, 94-104.
https://doi.org/10.1016/j.carbpol.2016.09.072


2016

Benchekroun, M.; Romero, A.; Egea, J.; León, R.; Michalska, P.; Buendía, I.; Jimeno, M. L.; Jun, D.; Janockova, J.; Sepsova, V.; Soukup, O.; Bautista-Aguilera, O. M.; Refouvelet, B.; Ouari, O.; Marco-Contelles, J.; Ismaili, L. The Antioxidant Additive Approach for Alzheimer’s Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. J. Med. Chem. 2016, 59 (21), 9967–9973.
https://doi.org/10.1021/acs.jmedchem.6b01178.



Chlebek, J.; De Simone, A.; Hošťálková, A.; Opletal, L.; Pérez, C.; Pérez, D. I.; Havlíková, L.; Cahlíková, L.; Andrisano, V. Application of BACE1 Immobilized Enzyme Reactor for the Characterization of Multifunctional Alkaloids from Corydalis Cava (Fumariaceae) as Alzheimer’s Disease Targets. Fitoterapia 2016, 109, 241–247.
https://doi.org/10.1016/j.fitote.2016.01.008.



Chlebek, J.; Novák, Z.; Kassemová, D.; Šafratová, M.; Kostelník, J.; Malý, L.; Ločárek, M.; Opletal, L.; Hošt’álková, A.; Hrabinová, M.; Kuneš, J.; Novotná, P.; Urbanová, M.; Nováková, L.; Macáková, K.; Hulcová, D.; Solich, P.; Pérez Martín, C.; Jun, D.; Cahlíková, L. Isoquinoline Alkaloids from Fumaria Officinalis L. and Their Biological Activities Related to Alzheimer ’s Disease. Chem. Biodivers. 2016, 13 (1), 91–99.
https://doi.org/10.1002/cbdv.201500033.



Estrada, M.; Herrera-Arozamena, C.; Pérez, C.; Viña, D.; Romero, A.; Morales-García, J. A.; Pérez-Castillo, A.; Rodríguez-Franco, M. I. New Cinnamic – N-Benzylpiperidine and Cinnamic – N,N-Dibenzyl(N-Methyl)Amine Hybrids as Alzheimer-Directed Multitarget Drugs with Antioxidant, Cholinergic, Neuroprotective and Neurogenic Properties. Eur. J. Med. Chem.2016, 121, 376–386.
https://doi.org/10.1016/j.ejmech.2016.05.055.



Estrada, M.; Pérez, C.; Soriano, E.; Laurini, E.; Romano, M.; Pricl, S.; Morales-García, J. A.; Pérez-Castillo, A.; Rodríguez-Franco, M. I. New Neurogenic Lipoic-Based Hybrids as Innovative Alzheimer’s Drugs with σ-1 Agonism and β-Secretase Inhibition. Future Med. Chem. 2016, 8 (11), 1191–1207.
https://doi.org/10.4155/fmc-2016-0036.



Herrera-Arozamena, C.; Martí-Marí, O.; Estrada, M.; de la Fuente Revenga, M.; Rodríguez-Franco, M. Recent Advances in Neurogenic Small Molecules as Innovative Treatments for Neurodegenerative Diseases. Molecules 2016, 21 (9), 1165.
https://doi.org/10.3390/molecules21091165.



Buendia, I.; Parada, E.; Navarro, E.; León, R.; Negredo, P.; Egea. J.; López, M. G. Subthreshold concentrations of melatonin and galantamine improves pathological AD-hallmarks in hippocampal organotypic cultures. Mol. Neurobiol. 2016, 53, 3338-3348.
https://doi.org/10.1007/s12035-015-9272-5.



Buendia, I.; Michalska, P.; Navarro, E.; Gameiro, I.; Egea, J.; León, R. Nrf2-ARE pathway: an emerging target against oxidative stress and neuroinflammation in neurodegenerative diseases. Pharmacol. Ther. 2016, 157, 84-104.
https://doi.org/10.1016/j.pharmthera.2015.11.003.


2015

Benchekroun, M.; Bartolini, M.; Egea, J.; Romero, A.; Soriano, E.; Pudlo, M.; Luzet, V.; Andrisano, V.; Jimeno, M.-L.; López, M. G.; Wehle, S.; Gharbi, T.; Refouvelet, B.; de Andrés, L.; Herrera-Arozamena, C.; Monti, B.; Bolognesi, M. L.; Rodríguez-Franco, M. I.; Decker, M.; Marco-Contelles, J.; Ismaili, L. Novel Tacrine-Grafted Ugi Adducts as Multipotent Anti-Alzheimer Drugs: A Synthetic Renewal in Tacrine-Ferulic Acid Hybrids. ChemMedChem 2015, 10 (3), 523–539.
https://doi.org/10.1002/cmdc.201402409.



Buendia, I.; Egea, J.; Parada, E.; Navarro, E.; León, R.; Rodríguez-Franco, M. I.; López, M. G. The Melatonin–N,N-Dibenzyl(N-Methyl)Amine Hybrid ITH91/IQM157 Affords Neuroprotection in an in Vitro Alzheimer’s Model via Hemo-Oxygenase-1 Induction. ACS Chem. Neurosci. 2015, 6 (2), 288–296.
https://doi.org/10.1021/cn5002073.



de la Fuente Revenga, M.; Balle, T.; Jensen, A. A.; Frølund, B. Conformationally Restrained Carbamoylcholine Homologues. Synthesis, Pharmacology at Neuronal Nicotinic Acetylcholine Receptors and Biostructural Considerations. Eur. J. Med. Chem. 2015, 102, 352–362.
https://doi.org/10.1016/j.ejmech.2015.07.029.



de la Fuente Revenga, M.; Fernández-Sáez, N.; Herrera-Arozamena, C.; Morales-García, J. A.; Alonso-Gil, S.; Pérez-Castillo, A.; Caignard, D.-H.; Rivara, S.; Rodríguez-Franco, M. I. Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential. J. Med. Chem. 2015 , 58 (12), 4998–5014.
https://doi.org/10.1021/acs.jmedchem.5b00245.
This work received the honour of being the subject of the Cover of the Journal of Medicinal Chemistry for its issue of July 23, 2015 (http://pubs.acs.org/toc/jmcmar/58/14)



de la Fuente Revenga, M.; Herrera-Arozamena, C.; Fernández-Sáez, N.; Barco, G.; García-Orue, I.; Sugden, D.; Rivara, S.; Rodríguez-Franco, M. I. New Coumarin-Based Fluorescent Melatonin Ligands. Design, Synthesis and Pharmacological Characterization. Eur. J. Med. Chem. 2015, 103, 370–373.
https://doi.org/10.1016/j.ejmech.2015.09.003.



de la Fuente Revenga, M.; Pérez, C.; Morales-García, J. A.; Alonso-Gil, S.; Pérez-Castillo, A.; Caignard, D.-H.; Yáñez, M.; Gamo, A. M.; Rodríguez-Franco, M. I. Neurogenic Potential Assessment and Pharmacological Characterization of 6-Methoxy-1,2,3,4-Tetrahydro-β-Carboline (Pinoline) and Melatonin–Pinoline Hybrids. ACS Chem. Neurosci. 2015, 6 (5), 800–810.
https://doi.org/10.1021/acschemneuro.5b00041.
This work received the honour of being the Cover of ACS Chemical Neuroscience in its issue of May 2015 (http://pubs.acs.org/toc/acncdm/6/5).



Matos, M. J.; Rodríguez-Enríquez, F.; Borges, F.; Santana, L.; Uriarte, E.; Estrada, M.; Rodríguez-Franco, M. I.; Laguna, R.; Viña, D. 3-Amidocoumarins as Potential Multifunctional Agents against Neurodegenerative Diseases. ChemMedChem 2015, 10 (12), 2071–2079.
https://doi.org/10.1002/cmdc.201500408.



Matos, M. J.; Rodríguez-Enríquez, F.; Vilar, S.; Santana, L.; Uriarte, E.; Hripcsak, G.; Estrada, M.; Rodríguez-Franco, M. I.; Viña, D. Potent and Selective MAO-B Inhibitory Activity: Amino- versus Nitro-3-Arylcoumarin Derivatives. Bioorg. Med. Chem. Lett. 2015, 25 (3), 642–648.
https://doi.org/10.1016/j.bmcl.2014.12.001.



Pérez, C.; Ruiz del Castillo, M. L.; Gil, C.; Blanch, G. P.; Flores, G. Supercritical Fluid Extraction of Grape Seeds: Extract Chemical Composition, Antioxidant Activity and Inhibition of Nitrite Production in LPS-Stimulated Raw 264.7 Cells. Food Funct. 2015, 6 (8), 2607–2613.
https://doi.org/10.1039/C5FO00325C.



Silva, T.; Bravo, J.; Summavielle, T.; Remião, F.; Pérez, C.; Gil, C.; Martínez, A.; Borges, F. Biology-Oriented Development of Novel Lipophilic Antioxidants with Neuroprotective Activity. RSC Adv. 2015, 5 (21), 15800–15811.
https://doi.org/10.1039/C4RA15164J.



Egea, J.; Buendia, I.; Parada, E.; Navarro, E.; Rada, P.; Cuadrado, A.; López, M. G.; García, A. G. León, R. Melatonin-sulforaphane hybrid ITH12674 induces neuroprotection in oxidative stress conditions by a “Drug-Prodrug” mechanism of action. Brit. J. Pharmacol. 2015, 172, 1807-1821.
https://doi.org/10.1111/bph.13025.



Buendia, I.; Gomez-Rangel, V.; Gonzalez-Lafuente, L.; Parada, E.; León, R.; Gameiro, I.; Michalska, P.; Laudon, M.; Egea, J.; López, M. G. Neuroprotective mechanism of the novel melatonin derivative Neu-P11 in brain ischemia related models. Neuropharmacol. 2015, 99, 187-195.
https://doi.org/10.1016/j.neuropharm.2015.07.014



Navarro, E.; Buendia, I.; Parada, E.; León, R.; Jansen-Duerr, P.; Pircher, H.; Egea, J.; López, M. G. Alpha7 nicotinic receptor activation protects against oxidative stress via heme-oxygenase I induction. Biochem. Pharmacol. 2015, 97 (4), 473-81.
https://doi.org/10.1016/j.bcp.2015.07.022



Egea, J.; Buendia, I.; Parada, E.; Navarro, E.; León, R.; López, M. G. Anti-inflammatory role of microglial 7 nAChRs and its role in neuroprotection. Biochem. Pharmacol. 2015, 97 (4), 463-72.
https://doi.org/10.1016/j.bcp.2015.07.032