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Page 1
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-d]pyrimidine RET Inhibitors.
Mathison CJN, Yang Y, Nelson J, Huang Z, Jiang J, Chianelli D, Rucker PV, Roland J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE. Mathison CJN, et al. Among authors: epple r. ACS Med Chem Lett. 2021 Nov 6;12(12):1912-1919. doi: 10.1021/acsmedchemlett.1c00450. eCollection 2021 Dec 9. ACS Med Chem Lett. 2021. PMID: 34917254 Free PMC article.
Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma.
Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE. Mathison CJN, et al. Among authors: epple r. ACS Med Chem Lett. 2020 Feb 12;11(4):558-565. doi: 10.1021/acsmedchemlett.0c00015. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292564 Free PMC article.
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.
Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Lelais G, et al. Among authors: epple r. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. Epub 2016 Jul 19. J Med Chem. 2016. PMID: 27433829
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Velcicky J, Mathison CJN, Nikulin V, Pflieger D, Epple R, Azimioara M, Cow C, Michellys PY, Rigollier P, Beisner DR, Bodendorf U, Guerini D, Liu B, Wen B, Zaharevitz S, Brandl T. Velcicky J, et al. Among authors: epple r. ACS Med Chem Lett. 2019 May 23;10(6):887-892. doi: 10.1021/acsmedchemlett.9b00044. eCollection 2019 Jun 13. ACS Med Chem Lett. 2019. PMID: 31223443 Free PMC article.
1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
Epple R, Azimioara M, Russo R, Bursulaya B, Tian SS, Gerken A, Iskandar M. Epple R, et al. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. doi: 10.1016/j.bmcl.2006.02.079. Epub 2006 Mar 20. Bioorg Med Chem Lett. 2006. PMID: 16546385
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
Epple R, Urbina HD, Russo R, Liu H, Mason D, Bursulaya B, Tumanut C, Li J, Harris JL. Epple R, et al. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1254-9. doi: 10.1016/j.bmcl.2006.12.014. Epub 2006 Dec 9. Bioorg Med Chem Lett. 2007. PMID: 17196818
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Epple R, Azimioara M, Russo R, Xie Y, Wang X, Cow C, Wityak J, Karanewsky D, Bursulaya B, Kreusch A, Tuntland T, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS. Epple R, et al. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5488-92. doi: 10.1016/j.bmcl.2006.08.052. Epub 2006 Aug 22. Bioorg Med Chem Lett. 2006. PMID: 16931011
EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.
Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S. Jia Y, et al. Among authors: epple r. Cancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. Epub 2016 Jan 29. Cancer Res. 2016. PMID: 26825170
41 results