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Halogen-enriched fragment libraries as chemical probes for harnessing halogen bonding in fragment-based lead discovery

Zimmermann, MO and Lange, A and Wilcken, R and Cieslik, MB and Exner, TE and Joerger, AC and Koch, P and Boeckler, FM (2014) Halogen-enriched fragment libraries as chemical probes for harnessing halogen bonding in fragment-based lead discovery. Future Medicinal Chemistry. pp. 617-639.

Abstract

Halogen bonding has recently experienced a renaissance, gaining increased recognition as a useful molecular interaction in the life sciences. Halogen bonds are favorable, fairly directional interactions between an electropositive region on the halogen (the -hole) and a number of different nucleophilic interaction partners. Some aspects of halogen bonding are not yet understood well enough to take full advantage of its potential in drug discovery. We describe and present the concept of halogen-enriched fragment libraries. These libraries consist of unique chemical probes, facilitating the identification of favorable halogen bonds by sharing the advantages of classical fragment-based screening. Besides providing insights into the nature and applicability of halogen bonding, halogen-enriched fragment libraries provide smart starting points for hit-to-lead evolution. 2014 Future Science Ltd

Item Type: Article
Additional Information: NIBR author: Wilcken, R institute: NIBR contributor address: (Zimmermann, Lange, Wilcken, Cieslik, Exner, Koch, Boeckler) Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmaceutical Sciences, Eberhard-Karls-University Tuebingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany (Wilcken, Joerger) MRC Laboratory of Molecular Biology, Cambridge Biomedical Campus, Francis Crick Avenue, Cambridge CB2 0QH, United Kingdom (Wilcken) Novartis Institutes for BioMedical Research, CH-4002 Basel, Switzerland
Date Deposited: 13 Oct 2015 13:12
Last Modified: 13 Oct 2015 13:12
URI: https://oak.novartis.com/id/eprint/22748

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