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Page 1
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. 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.
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. 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
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. 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
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. 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
Discovery of novel triazolo[4,3-b]pyridazin-3-yl-quinoline derivatives as PIM inhibitors.
Martínez-González S, Rodríguez-Arístegui S, Gómez de la Oliva CA, Hernández AI, González Cantalapiedra E, Varela C, García AB, Rabal O, Oyarzabal J, Bischoff JR, Klett J, Albarrán MI, Cebriá A, Ajenjo N, García-Serelde B, Gómez-Casero E, Cuadrado-Urbano M, Cebrián D, Blanco-Aparicio C, Pastor J. Martínez-González S, et al. Eur J Med Chem. 2019 Apr 15;168:87-109. doi: 10.1016/j.ejmech.2019.02.022. Epub 2019 Feb 19. Eur J Med Chem. 2019. PMID: 30802730
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
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. Among authors: martinez gonzalez s. 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.
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. 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. 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
Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors.
Martínez-González S, García AB, Albarrán MI, Cebriá A, Amezquita-Alves A, García-Campos FJ, Martínez-Gago J, Martínez-Torrecuadrada J, Muñoz IG, Blanco-Aparicio C, Pastor J. Martínez-González S, et al. Eur J Med Chem. 2020 Sep 1;201:112443. doi: 10.1016/j.ejmech.2020.112443. Epub 2020 Jun 20. Eur J Med Chem. 2020. PMID: 32599324
58 results