Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors

Harald Engelhardt(Boehringer Ingelheim (Austria)), Dietrich Böse(Boehringer Ingelheim (Austria)), Mark Petronczki(Boehringer Ingelheim (Austria)), Dirk Scharn(Boehringer Ingelheim (Austria)), Gerd Bader(Boehringer Ingelheim (Austria)), Anke Baum(Boehringer Ingelheim (Austria)), Andreas Bergner(Boehringer Ingelheim (Austria)), Eugene Chong(Boehringer Ingelheim (United States)), Sandra Döbel(Boehringer Ingelheim (Austria)), Georg Egger(Boehringer Ingelheim (Austria)), Christian Engelhardt(Boehringer Ingelheim (Austria)), Peter Ettmayer(Boehringer Ingelheim (Austria)), Julian E. Fuchs(Boehringer Ingelheim (Austria)), Thomas Gerstberger(Boehringer Ingelheim (Austria)), Nina C. Gonnella(Boehringer Ingelheim (United States)), Andreas Grimm(Boehringer Ingelheim (Austria)), Elisabeth Grondal(Boehringer Ingelheim (Austria)), Nizar Haddad(Boehringer Ingelheim (United States)), Barbara Hopfgartner(Boehringer Ingelheim (Austria)), Roland Kousek(Boehringer Ingelheim (Austria)), Mariusz Krawiec(Boehringer Ingelheim (United States)), Monika Kriz(Boehringer Ingelheim (Austria)), Lyne Lamarre(Boehringer Ingelheim (Austria)), Joyce C. Leung(Boehringer Ingelheim (United States)), Moriz Mayer(Boehringer Ingelheim (Austria)), Nitinchandra D. Patel(Boehringer Ingelheim (United States)), Biljana Peric Simov(Boehringer Ingelheim (Austria)), Jonathan T. Reeves(Boehringer Ingelheim (United States)), Renate Schnitzer(Boehringer Ingelheim (Austria)), Andreas Schrenk(Boehringer Ingelheim (Austria)), Bernadette Sharps(Boehringer Ingelheim (Austria)), Flavio Solca(Boehringer Ingelheim (Austria)), Heinz Stadtmüller(Boehringer Ingelheim (Austria)), Zhulin Tan(Boehringer Ingelheim (United States)), Tobias Wunberg(Boehringer Ingelheim (Austria)), Andreas Zoephel(Boehringer Ingelheim (Austria)), Darryl B. McConnell(Boehringer Ingelheim (Austria))
Journal of Medicinal Chemistry
November 5, 2019
Cited by 144Open Access
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Abstract

xenograft model. Key was the identification of a highly selective but moderately potent benzimidazole followed by complete rigidification of the molecule through macrocyclization.


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