Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19-Reference-Cited by-同舟云学术

Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19

Published:2022-11-16 Issue:23 Volume:65 Page:15679-15697
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Amrhein Jennifer A.¹²,Beyett Tyler S.³^ORCID,Feng William W.⁴^ORCID,Krämer Andreas¹²,Weckesser Janik¹²,Schaeffner Ilse K.³,Rana Jaimin K.³,Jänne Pasi A.⁴,Eck Michael J.³,Knapp Stefan¹²^ORCID,Hanke Thomas¹²^ORCID

Affiliation:

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

2. Structural Genomics Consortium, Buchman Institute for Molecular Life Science (BMLS), Max-von-Laue-Straße 15, 60438 Frankfurt, Germany

3. Department of Cancer Biology, Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02215, United States

4. Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute, Department of Medical Oncology, Department of Medicine, Harvard Medical School, Boston, Massachusetts 02215, United States

Funder

Bayer

Merck KGaA

Genentech

Pfizer

Innovative Medicines Initiative

Genome Canada

Wellcome Trust

AbbVie

Funda??o de Amparo ? Pesquisa do Estado de S?o Paulo

National Institutes of Health

Boehringer Ingelheim