Back-Pocket Optimization of 2-Aminopyrimidine-Based Macrocycles Leads to Potent EPHA2/GAK Kinase Inhibitors

Author:

Gerninghaus Joshua12,Zhubi Rezart12,Krämer Andreas12,Karim Marwah3,Tran Do Hoang Nhu3,Joerger Andreas C.12ORCID,Schreiber Christian12,Berger Lena M.12ORCID,Berger Benedict-Tilman12ORCID,Ehret Theresa A.L.12,Elson Lewis12,Lenz Christopher12ORCID,Saxena Krishna12,Müller Susanne12ORCID,Einav Shirit34ORCID,Knapp Stefan12ORCID,Hanke Thomas12ORCID

Affiliation:

1. Institute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, Frankfurt am Main 60438, Germany

2. Structural Genomics Consortium (SGC), Buchmann Institute for Life Sciences, Max-von-Laue-Str. 15, Frankfurt am Main 60438, Germany

3. Department of Medicine, Division of Infectious Diseases and Geographic Medicine, and Department of Microbiology and Immunology, Stanford University School of Medicine, Stanford, California 94305, United States

4. Chan Zuckerberg Biohub, 499 Illinois St, San Francisco, California 94158, United States

Funder

European Commission

Deutschen Konsortium f?r Translationale Krebsforschung

National Institute of Allergy and Infectious Diseases

Deutsche Forschungsgemeinschaft

Congressionally Directed Medical Research Programs

Structural Genomics Consortium

Defense Threat Reduction Agency

Frankfurt Cancer Institute

Publisher

American Chemical Society (ACS)

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