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Title: Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor
Authors : Fischer, Thomas
Riedl, Rainer
Published in : ChemistryOpen
Volume(Issue) : 6
Issue : 2
Pages : 192
Pages to: 195
Publisher / Ed. Institution : Wiley
Issue Date: 2017
License (according to publishing contract) : CC BY-NC-ND 4.0: Namensnennung - Nicht kommerziell - Keine Bearbeitungen 4.0 International
Type of review: Peer review (Publication)
Language : English
Subjects : Medicinal chemistry; Drug discovery; Drug design
Subject (DDC) : 572: Biochemistry
615: Pharmacology and therapeutics
Abstract: The incorporation of fluorine atoms into functional molecules is of wide interest in synthetic organic chemistry as well as cognate disciplines. In particular, in medicinal chemistry, there is a strong desire to positively influence the physicochemical molecular properties of drug compounds by introducing fluorine into biologically active molecules. Here, we present targeted fluoro positioning as the key design principle of converting a weak matrix metalloproteinase-13 (MMP-13 ) inhibitor into a very potent (IC50 = 6nM) and highly selective (selectivity factors of > 1000 over MMP-1, 2, 3, 7, 8, 9, 10, 12, 14) inhibitor with excellent plasma and microsomal stability, and no binding to the hERG channel (hERG: human ether-a-go-go related gene).
Departement: Life Sciences und Facility Management
Organisational Unit: Institute of Chemistry and Biotechnology (ICBT)
Publication type: Article in scientific Journal
DOI : 10.1002/open.201600158
ISSN: 2191-1363
Appears in Collections:Publikationen Life Sciences und Facility Management

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