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Page 1
Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy.
Rabal O, San José-Enériz E, Agirre X, Sánchez-Arias JA, Vilas-Zornoza A, Ugarte A, de Miguel I, Miranda E, Garate L, Fraga M, Santamarina P, Fernandez Perez R, Ordoñez R, Sáez E, Roa S, García-Barchino MJ, Martínez-Climent JA, Liu Y, Wu W, Xu M, Prosper F, Oyarzabal J. Rabal O, et al. Among authors: sanchez arias ja. J Med Chem. 2018 Aug 9;61(15):6518-6545. doi: 10.1021/acs.jmedchem.7b01926. Epub 2018 Jul 19. J Med Chem. 2018. PMID: 29953809
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with In Vivo Efficacy in Multiple Myeloma.
Rabal O, San José-Enériz E, Agirre X, Sánchez-Arias JA, de Miguel I, Ordoñez R, Garate L, Miranda E, Sáez E, Vilas-Zornoza A, Pineda-Lucena A, Estella A, Zhang F, Wu W, Xu M, Prosper F, Oyarzabal J. Rabal O, et al. Among authors: sanchez arias ja. J Med Chem. 2021 Mar 25;64(6):3392-3426. doi: 10.1021/acs.jmedchem.0c02255. Epub 2021 Mar 4. J Med Chem. 2021. PMID: 33661013
Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.
Rabal O, Sánchez-Arias JA, San José-Enériz E, Agirre X, de Miguel I, Garate L, Miranda E, Sáez E, Roa S, Martínez-Climent JA, Liu Y, Wu W, Xu M, Prosper F, Oyarzabal J. Rabal O, et al. Among authors: sanchez arias ja. J Med Chem. 2018 Aug 9;61(15):6546-6573. doi: 10.1021/acs.jmedchem.7b01925. Epub 2018 Jul 19. J Med Chem. 2018. PMID: 29890830
Discovery and safety profiling of a potent preclinical candidate, (4-[4-[[(3R)-3-(hydroxycarbamoyl)-8-azaspiro[4.5]decan-3-yl]sulfonyl]phenoxy]-N-methylbenzamide) (CM-352), for the prevention and treatment of hemorrhage.
Orbe J, Rodríguez JA, Sánchez-Arias JA, Salicio A, Belzunce M, Ugarte A, Chang HC, Rabal O, Oyarzabal J, Páramo JA. Orbe J, et al. J Med Chem. 2015 Apr 9;58(7):2941-57. doi: 10.1021/jm501939z. Epub 2015 Feb 25. J Med Chem. 2015. PMID: 25686022
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
Rabal O, Sánchez-Arias JA, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, García-Barroso C, Ugarte A, Estella-Hermoso de Mendoza A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J. Rabal O, et al. J Med Chem. 2016 Oct 13;59(19):8967-9004. doi: 10.1021/acs.jmedchem.6b00908. Epub 2016 Sep 27. J Med Chem. 2016. PMID: 27606546
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
Rabal O, Sánchez-Arias JA, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, García-Barroso C, Ugarte A, Estella-Hermoso de Mendoza A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J. Rabal O, et al. Eur J Med Chem. 2018 Apr 25;150:506-524. doi: 10.1016/j.ejmech.2018.03.005. Epub 2018 Mar 20. Eur J Med Chem. 2018. PMID: 29549837
Phenotypic Screening To Discover Novel Chemical Series as Efficient Antihemorrhagic Agents.
de Miguel I, Orbe J, Sánchez-Arias JA, Rodríguez JA, Salicio A, Rabal O, Belzunce M, Sáez E, Xu M, Wu W, Tan H, Ma H, Páramo JA, Oyarzabal J. de Miguel I, et al. ACS Med Chem Lett. 2018 Apr 16;9(5):428-433. doi: 10.1021/acsmedchemlett.7b00549. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795754 Free PMC article.
A First-in-Class Small-Molecule that Acts as a Dual Inhibitor of HDAC and PDE5 and that Rescues Hippocampal Synaptic Impairment in Alzheimer's Disease Mice.
Cuadrado-Tejedor M, Garcia-Barroso C, Sánchez-Arias JA, Rabal O, Pérez-González M, Mederos S, Ugarte A, Franco R, Segura V, Perea G, Oyarzabal J, Garcia-Osta A. Cuadrado-Tejedor M, et al. Neuropsychopharmacology. 2017 Jan;42(2):524-539. doi: 10.1038/npp.2016.163. Epub 2016 Aug 23. Neuropsychopharmacology. 2017. PMID: 27550730 Free PMC article.
34 results