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Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.
Martínez González S, Rodríguez-Arístegui S, Hernández AI, Varela C, González Cantalapiedra E, Álvarez RM, Rodríguez Hergueta A, Bischoff JR, Albarrán MI, Cebriá A, Cendón E, Cebrián D, Alfonso P, Pastor J. Martínez González S, et al. Among authors: alvarez rm. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2536-2543. doi: 10.1016/j.bmcl.2017.03.090. Epub 2017 Apr 2. Bioorg Med Chem Lett. 2017. PMID: 28404374
Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.
Pastor J, Oyarzabal J, Saluste G, Alvarez RM, Rivero V, Ramos F, Cendón E, Blanco-Aparicio C, Ajenjo N, Cebriá A, Albarrán MI, Cebrián D, Corrionero A, Fominaya J, Montoya G, Mazzorana M. Pastor J, et al. Among authors: alvarez rm. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1591-7. doi: 10.1016/j.bmcl.2011.12.130. Epub 2012 Jan 5. Bioorg Med Chem Lett. 2012. PMID: 22266039
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.
Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Alvarez RM, García AB, Lorenzo M, Rivero V, Oyarzabal J, Rabal O, Bischoff JR, Albarrán M, Cebriá A, Alfonso P, Link W, Fominaya J, Pastor J. Martínez González S, et al. Among authors: alvarez rm. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. doi: 10.1016/j.bmcl.2012.01.074. Epub 2012 Jan 28. Bioorg Med Chem Lett. 2012. PMID: 22325943
Identification of novel PI3K inhibitors through a scaffold hopping strategy.
Martínez González S, Hernández AI, Álvarez RM, Rodríguez A, Ramos-Lima F, Bischoff JR, Albarrán MI, Cebriá A, Hernández-Encinas E, García-Arocha J, Cebrián D, Blanco-Aparicio C, Pastor J. Martínez González S, et al. Among authors: alvarez rm. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4794-4799. doi: 10.1016/j.bmcl.2017.09.059. Epub 2017 Sep 30. Bioorg Med Chem Lett. 2017. PMID: 29017786
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.
Álvarez RM, García AB, Riesco-Fagundo C, Martín JI, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Oyarzabal J, Di Geronimo B, Lorenzo M, Albarrán MI, Cebriá A, Cebrián D, Martínez-González S, Blanco-Aparicio C, Pastor J. Álvarez RM, et al. Eur J Med Chem. 2021 Feb 5;211:113109. doi: 10.1016/j.ejmech.2020.113109. Epub 2020 Dec 18. Eur J Med Chem. 2021. PMID: 33360802
Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors.
Martínez-González S, Alvarez RM, Martín JI, García AB, Riesco-Fagundo C, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Albarrán MI, Gómez-Casero E, Cebriá A, Aguirre E, Ajenjo N, Cebrián D, Di Geronimo B, Cunningham D, O'Neill M, Dave HPG, Blanco-Aparicio C, Pastor J. Martínez-González S, et al. Among authors: alvarez rm. ACS Med Chem Lett. 2021 Nov 2;12(11):1794-1801. doi: 10.1021/acsmedchemlett.1c00412. eCollection 2021 Nov 11. ACS Med Chem Lett. 2021. PMID: 34795869 Free PMC article.
Corrigendum to <' Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors' [Eur. J. Med. Chem. 211 (2021), 113109].
Alvarez RM, García AB, Riesco-Fagundo C, Martín JI, Varela C, Rodríguez Hergueta A, González Cantalapiedra E, Oyarzabal J, Di Geronimo B, Lorenzo M, Albarrán MI, Cebriá A, Cebrián D, Martínez-González S, Blanco-Aparicio C, Pastor J. Alvarez RM, et al. Eur J Med Chem. 2021 Nov 15;224:113703. doi: 10.1016/j.ejmech.2021.113703. Epub 2021 Jul 17. Eur J Med Chem. 2021. PMID: 34284231 No abstract available.
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and alpha2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety.
Pastor J, Alcázar J, Alvarez RM, Andrés JI, Cid JM, De Lucas AI, Díaz A, Fernández J, Font LM, Iturrino L, Lafuente C, Martínez S, Bakker MH, Biesmans I, Heylen LI, Megens AA. Pastor J, et al. Among authors: alvarez rm. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2917-22. doi: 10.1016/j.bmcl.2004.03.031. Bioorg Med Chem Lett. 2004. PMID: 15125959
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Drinkenburg W, Fernández J, Font LM, Iturrino L, Langlois X, Lenaerts I, Martínez S, Megens AA, Pastor J, Pullan S, Steckler T. Andrés JI, et al. Among authors: alvarez rm. Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. doi: 10.1016/j.bmc.2007.03.053. Epub 2007 Mar 21. Bioorg Med Chem. 2007. PMID: 17407815
104 results