Synthesis of MDM2-p53 Inhibitor BI-0282 via a Dipolar Cycloaddition and Late-Stage Davis–Beirut Reaction

por Ramharter, Juergen, Kulhanek, Michael, Dettling, Maike, Gmaschitz, Gerhard, Karolyi-Oezguer, Jale, Weinstabl, Harald, Gollner, Andreas
Publicado 2022

Targeted Synthesis of Complex Spiro[3H‐indole‐3,2′‐pyrrolidin]‐2(1H)‐ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2–p53 Inhibitors

por Gollner, Andreas, Weinstabl, Harald, Fuchs, Julian E., Rudolph, Dorothea, Garavel, Geraldine, Hofbauer, Karin S., Karolyi‐Oezguer, Jale, Gmaschitz, Gerhard, Hela, Wolfgang, Kerres, Nina, Grondal, Elisabeth, Werni, Patrick, Ramharter, Juergen, Broeker, Joachim, McConnell, Darryl B.
Publicado 2018

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS(G12C) Inhibitor

por Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Publicado 2022

A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo

por Kofink, Christiane, Trainor, Nicole, Mair, Barbara, Wöhrle, Simon, Wurm, Melanie, Mischerikow, Nikolai, Roy, Michael J., Bader, Gerd, Greb, Peter, Garavel, Géraldine, Diers, Emelyne, McLennan, Ross, Whitworth, Claire, Vetma, Vesna, Rumpel, Klaus, Scharnweber, Maximilian, Fuchs, Julian E., Gerstberger, Thomas, Cui, Yunhai, Gremel, Gabriela, Chetta, Paolo, Hopf, Stefan, Budano, Nicole, Rinnenthal, Joerg, Gmaschitz, Gerhard, Mayer, Moriz, Koegl, Manfred, Ciulli, Alessio, Weinstabl, Harald, Farnaby, William
Publicado 2022