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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
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, 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.
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
Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.
San José-Enériz E, Agirre X, Rabal O, Vilas-Zornoza A, Sanchez-Arias JA, Miranda E, Ugarte A, Roa S, Paiva B, Estella-Hermoso de Mendoza A, Alvarez RM, Casares N, Segura V, Martín-Subero JI, Ogi FX, Soule P, Santiveri CM, Campos-Olivas R, Castellano G, de Barrena MGF, Rodriguez-Madoz JR, García-Barchino MJ, Lasarte JJ, Avila MA, Martinez-Climent JA, Oyarzabal J, Prosper F. San José-Enériz E, et al. Nat Commun. 2017 May 26;8:15424. doi: 10.1038/ncomms15424. Nat Commun. 2017. PMID: 28548080 Free PMC article.
Impact of Scaffold Exploration on Novel Dual-Acting Histone Deacetylases and Phosphodiesterase 5 Inhibitors for the Treatment of Alzheimer's Disease.
Sánchez-Arias JA, Rabal O, Cuadrado-Tejedor M, de Miguel I, Pérez-González M, Ugarte A, Sáez E, Espelosin M, Ursua S, Haizhong T, Wei W, Musheng X, Garcia-Osta A, Oyarzabal J. Sánchez-Arias JA, et al. ACS Chem Neurosci. 2017 Mar 15;8(3):638-661. doi: 10.1021/acschemneuro.6b00370. Epub 2016 Dec 27. ACS Chem Neurosci. 2017. PMID: 27936591
34 results