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428 results

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Page 1
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Lu T, Schubert C, Cummings MD, Bignan G, Connolly PJ, Smans K, Ludovici D, Parker MH, Meyer C, Rocaboy C, Alexander R, Grasberger B, De Breucker S, Esser N, Fraiponts E, Gilissen R, Janssens B, Peeters D, Van Nuffel L, Vermeulen P, Bischoff J, Meerpoel L. Lu T, et al. Among authors: bischoff j. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2159-2164. doi: 10.1016/j.bmcl.2018.05.014. Epub 2018 May 8. Bioorg Med Chem Lett. 2018. PMID: 29779975
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).
Zhang Z, Connolly PJ, Lim HK, Pande V, Meerpoel L, Teleha C, Branch JR, Ondrus J, Hickson I, Bush T, Luistro L, Packman K, Bischoff JR, Ibrahim S, Parrett C, Chong Y, Gottardis MM, Bignan G. Zhang Z, et al. Among authors: bischoff jr. J Med Chem. 2021 Jan 28;64(2):909-924. doi: 10.1021/acs.jmedchem.0c01563. Epub 2021 Jan 20. J Med Chem. 2021. PMID: 33470111
Spirocyclic Thiohydantoin Antagonists of F877L and Wild-Type Androgen Receptor for Castration-Resistant Prostate Cancer.
Zhang Z, Connolly PJ, Trabalón Escolar L, Rocaboy C, Pande V, Meerpoel L, Lim HK, Branch JR, Ondrus J, Hickson I, Bush TL, Bischoff JR, Bignan G. Zhang Z, et al. Among authors: bischoff jr. ACS Med Chem Lett. 2021 Jun 29;12(8):1245-1252. doi: 10.1021/acsmedchemlett.1c00032. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34422225 Free PMC article.
Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer.
Branch JR, Bush TL, Pande V, Connolly PJ, Zhang Z, Hickson I, Ondrus J, Jaensch S, Bischoff JR, Habineza G, Van Hecke G, Meerpoel L, Packman K, Parrett CJ, Chong YT, Gottardis MM, Bignan G. Branch JR, et al. Among authors: bischoff jr. Mol Cancer Ther. 2021 May;20(5):763-774. doi: 10.1158/1535-7163.MCT-20-0510. Epub 2021 Mar 1. Mol Cancer Ther. 2021. PMID: 33649102
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: bischoff jr. 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
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: bischoff jr. 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
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors.
Richters A, Doyle SK, Freeman DB, Lee C, Leifer BS, Jagannathan S, Kabinger F, Koren JV, Struntz NB, Urgiles J, Stagg RA, Curtin BH, Chatterjee D, Mathea S, Mikochik PJ, Hopkins TD, Gao H, Branch JR, Xin H, Westover L, Bignan GC, Rupnow BA, Karlin KL, Olson CM, Westbrook TF, Vacca J, Wilfong CM, Trotter BW, Saffran DC, Bischofberger N, Knapp S, Russo JW, Hickson I, Bischoff JR, Gottardis MM, Balk SP, Lin CY, Pop MS, Koehler AN. Richters A, et al. Among authors: bischoff jr. Cell Chem Biol. 2021 Feb 18;28(2):134-147.e14. doi: 10.1016/j.chembiol.2020.10.001. Epub 2020 Oct 20. Cell Chem Biol. 2021. PMID: 33086052 Free 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: bischoff jr. 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
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: bischoff jr. 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
Optimization of 6,6-dimethyl pyrrolo[3,4-c]pyrazoles: Identification of PHA-793887, a potent CDK inhibitor suitable for intravenous dosing.
Brasca MG, Albanese C, Alzani R, Amici R, Avanzi N, Ballinari D, Bischoff J, Borghi D, Casale E, Croci V, Fiorentini F, Isacchi A, Mercurio C, Nesi M, Orsini P, Pastori W, Pesenti E, Pevarello P, Roussel P, Varasi M, Volpi D, Vulpetti A, Ciomei M. Brasca MG, et al. Among authors: bischoff j. Bioorg Med Chem. 2010 Mar 1;18(5):1844-53. doi: 10.1016/j.bmc.2010.01.042. Epub 2010 Jan 25. Bioorg Med Chem. 2010. PMID: 20153204
428 results