Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376850 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
The pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) are a class of DNA minor groove binding agents that react covalently with guanine bases, preferably at Pu-G-Pu sites. A series of three fluorescent PBD–coumarin conjugates with different linker architectures has been synthesized to probe correlations between DNA binding affinity, cellular localization and cytotoxicity. The results show that the linker structure plays a critical role for all three parameters.
Graphical abstractA series of three fluorescent PBD–coumarin conjugates with different linker architectures has been synthesized to probe correlations between DNA-binding affinity, cellular localization and cytotoxicity.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Geoffrey Wells, Marie Suggitt, Marissa Coffils, Mirza A.H. Baig, Philip W. Howard, Paul M. Loadman, John A. Hartley, Terence C. Jenkins, David E. Thurston,