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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: aguirre e. 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.
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.
Martínez González S, Hernández AI, Varela C, Rodríguez-Arístegui S, Lorenzo M, Rodríguez A, Rivero V, Martín JI, Saluste CG, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán M, Alfonso P, García-Serelde B, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Pastor J. Martínez González S, et al. Among authors: aguirre e. Bioorg Med Chem Lett. 2012 May 15;22(10):3460-6. doi: 10.1016/j.bmcl.2012.03.090. Epub 2012 Mar 29. Bioorg Med Chem Lett. 2012. PMID: 22520259
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.
Martínez González S, Hernández AI, Varela C, Lorenzo M, Ramos-Lima F, Cendón E, Cebrián D, Aguirre E, Gomez-Casero E, Albarrán MI, Alfonso P, García-Serelde B, Mateos G, Oyarzabal J, Rabal O, Mulero F, Gonzalez-Granda T, Link W, Fominaya J, Barbacid M, Bischoff JR, Pizcueta P, Blanco-Aparicio C, Pastor J. Martínez González S, et al. Among authors: aguirre e. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5208-14. doi: 10.1016/j.bmcl.2012.06.093. Epub 2012 Jul 4. Bioorg Med Chem Lett. 2012. PMID: 22819764
196 results