Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833
In: ACS Medicinal Chemistry Letters, Jg. 11 (2020-10-28), S. 2519-2525
Online
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Zugriff:
[Image: see text] Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition of fluorine on the lipophilicity, permeability, and metabolism are discussed. Many of these changes were tolerated in terms of pharmacology and resulted in high quality molecules which reached advanced stages of profiling in the testing cascade.
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Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833
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| Autor/in / Beteiligte Person: | Tucker, Michael J. ; Moss, Thomas A. ; Scott, James S. ; Barlaam Bernard Christophe ; Davey, Paul R. J. ; Greenwood, Ryan ; Stokes, Stephen ; Fairley, Gary ; Polanski, Radoslaw ; Hatoum-Mokdad, Holia ; Longmire, David ; Gangl, Eric ; Yang, Bin ; Lister, Andrew ; Varnes, Jeffrey G. |
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| Zeitschrift: | ACS Medicinal Chemistry Letters, Jg. 11 (2020-10-28), S. 2519-2525 |
| Veröffentlichung: | American Chemical Society (ACS), 2020 |
| Medientyp: | unknown |
| ISSN: | 1948-5875 (print) |
| DOI: | 10.1021/acsmedchemlett.0c00505 |
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