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Page 1
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor.
Bröker J, Waterson AG, Smethurst C, Kessler D, Böttcher J, Mayer M, Gmaschitz G, Phan J, Little A, Abbott JR, Sun Q, Gmachl M, Rudolph D, Arnhof H, Rumpel K, Savarese F, Gerstberger T, Mischerikow N, Treu M, Herdeis L, Wunberg T, Gollner A, Weinstabl H, Mantoulidis A, Krämer O, McConnell DB, W Fesik S. Bröker J, et al. Among authors: gollner a. J Med Chem. 2022 Nov 10;65(21):14614-14629. doi: 10.1021/acs.jmedchem.2c01120. Epub 2022 Oct 27. J Med Chem. 2022. PMID: 36300829 Free PMC article.
Discovery of Novel Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2-p53 Interaction.
Gollner A, Rudolph D, Arnhof H, Bauer M, Blake SM, Boehmelt G, Cockroft XL, Dahmann G, Ettmayer P, Gerstberger T, Karolyi-Oezguer J, Kessler D, Kofink C, Ramharter J, Rinnenthal J, Savchenko A, Schnitzer R, Weinstabl H, Weyer-Czernilofsky U, Wunberg T, McConnell DB. Gollner A, et al. J Med Chem. 2016 Nov 23;59(22):10147-10162. doi: 10.1021/acs.jmedchem.6b00900. Epub 2016 Nov 15. J Med Chem. 2016. PMID: 27775892
Targeted Synthesis of Complex Spiro[3H-indole-3,2'-pyrrolidin]-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors.
Gollner A, Weinstabl H, Fuchs JE, Rudolph D, Garavel G, Hofbauer KS, Karolyi-Oezguer J, Gmaschitz G, Hela W, Kerres N, Grondal E, Werni P, Ramharter J, Broeker J, McConnell DB. Gollner A, et al. ChemMedChem. 2019 Jan 8;14(1):88-93. doi: 10.1002/cmdc.201800617. Epub 2018 Dec 11. ChemMedChem. 2019. PMID: 30458062 Free PMC article.
KRAS Binders Hidden in Nature.
Bergner A, Cockcroft X, Fischer G, Gollner A, Hela W, Kousek R, Mantoulidis A, Martin LJ, Mayer M, Müllauer B, Siszler G, Wolkerstorfer B, Kessler D, McConnell DB. Bergner A, et al. Among authors: gollner a. Chemistry. 2019 Sep 18;25(52):12037-12041. doi: 10.1002/chem.201902810. Epub 2019 Jul 25. Chemistry. 2019. PMID: 31231840 Free PMC article.
36 results