| Structural highlights
Publication Abstract from PubMed
The concept of drug-likeness distills the physicochemical properties of small-molecule drugs to a set of rules. Macrocyclic drugs are known to break these rules. A structure-based macrocyclization strategy was applied to design new hepatitis C virus NS5B inhibitors with improved pharmocokinetic properties, exemplifying a rational strategy for overcoming the confines of standard "drug-like chemical space".
Structure-Based Macrocyclization Yields Hepatitis C Virus NS5B Inhibitors with Improved Binding Affinities and Pharmacokinetic Properties.,Cummings MD, Lin TI, Hu L, Tahri A, McGowan D, Amssoms K, Last S, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Van Emelen K, Nyanguile O, Simmen K, Raboisson P, Vendeville S Angew Chem Int Ed Engl. 2012 Mar 30. doi: 10.1002/anie.201200110. PMID:22473861[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
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References
- ↑ Cummings MD, Lin TI, Hu L, Tahri A, McGowan D, Amssoms K, Last S, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Van Emelen K, Nyanguile O, Simmen K, Raboisson P, Vendeville S. Structure-Based Macrocyclization Yields Hepatitis C Virus NS5B Inhibitors with Improved Binding Affinities and Pharmacokinetic Properties. Angew Chem Int Ed Engl. 2012 Mar 30. doi: 10.1002/anie.201200110. PMID:22473861 doi:10.1002/anie.201200110
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