Fluorescent 7-diethylaminocoumarin pyrrolobenzodiazepine conjugates: synthesis, DNA interaction, cytotoxicity and differential cellular localization |
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| Authors: | Wells Geoffrey Suggitt Marie Coffils Marissa Baig Mirza A H Howard Philip W Loadman Paul M Hartley John A Jenkins Terence C Thurston David E |
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| Affiliation: | Cancer Research UK Gene Targeted Drug Design Research Group, School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK. |
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| 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. |
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