Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor

Fischer, Thomas; Riedl, Rainer

doi:10.1002/open.201600158

Please use this identifier to cite or link to this item: https://doi.org/10.21256/zhaw-1690

Full metadata record

DC Field	Value	Language
dc.contributor.author	Fischer, Thomas	-
dc.contributor.author	Riedl, Rainer	-
dc.date.accessioned	2018-02-16T14:54:11Z	-
dc.date.available	2018-02-16T14:54:11Z	-
dc.date.issued	2017	-
dc.identifier.issn	2191-1363	de_CH
dc.identifier.uri	https://digitalcollection.zhaw.ch/handle/11475/2857	-
dc.description.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).	de_CH
dc.language.iso	en	de_CH
dc.publisher	Wiley	de_CH
dc.relation.ispartof	ChemistryOpen	de_CH
dc.rights	http://creativecommons.org/licenses/by-nc-nd/4.0/	de_CH
dc.subject	Medicinal chemistry	de_CH
dc.subject	Drug discovery	de_CH
dc.subject	Drug design	de_CH
dc.subject.ddc	572: Biochemie	de_CH
dc.subject.ddc	615: Pharmakologie und Therapeutik	de_CH
dc.title	Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor	de_CH
dc.type	Beitrag in wissenschaftlicher Zeitschrift	de_CH
dcterms.type	Text	de_CH
zhaw.departement	Life Sciences und Facility Management	de_CH
zhaw.organisationalunit	Institut für Chemie und Biotechnologie (ICBT)	de_CH
dc.identifier.doi	10.1002/open.201600158	de_CH
dc.identifier.doi	10.21256/zhaw-1690	-
zhaw.funding.eu	No	de_CH
zhaw.issue	2	de_CH
zhaw.originated.zhaw	Yes	de_CH
zhaw.pages.end	195	de_CH
zhaw.pages.start	192	de_CH
zhaw.publication.status	publishedVersion	de_CH
zhaw.volume	6	de_CH
zhaw.publication.review	Peer review (Publikation)	de_CH
zhaw.webfeed	CC Drug Discovery	de_CH
Appears in collections:	Publikationen Life Sciences und Facility Management

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Fischer, T., & Riedl, R. (2017). Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor. ChemistryOpen, 6(2), 192–195. https://doi.org/10.1002/open.201600158

Fischer, T. and Riedl, R. (2017) ‘Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor’, ChemistryOpen, 6(2), pp. 192–195. Available at: https://doi.org/10.1002/open.201600158.

T. Fischer and R. Riedl, “Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor,” ChemistryOpen, vol. 6, no. 2, pp. 192–195, 2017, doi: 10.1002/open.201600158.

FISCHER, Thomas und Rainer RIEDL, 2017. Targeted fluoro positioning for the discovery of a potent and highly selective matrix metalloproteinase inhibitor. ChemistryOpen. 2017. Bd. 6, Nr. 2, S. 192–195. DOI 10.1002/open.201600158

Fischer, Thomas, and Rainer Riedl. 2017. “Targeted Fluoro Positioning for the Discovery of a Potent and Highly Selective Matrix Metalloproteinase Inhibitor.” ChemistryOpen 6 (2): 192–95. https://doi.org/10.1002/open.201600158.

Fischer, Thomas, and Rainer Riedl. “Targeted Fluoro Positioning for the Discovery of a Potent and Highly Selective Matrix Metalloproteinase Inhibitor.” ChemistryOpen, vol. 6, no. 2, 2017, pp. 192–95, https://doi.org/10.1002/open.201600158.