Fluorescent 7-diethylaminocoumarin pyrrolobenzodiazepine conjugates: synthesis, DNA interaction, cytotoxicity and differential cellular localization

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2147-51. doi: 10.1016/j.bmcl.2008.01.083.

Geoffrey Wells ¹, Marie Suggitt, Marissa Coffils, Mirza A H Baig, Philip W Howard, Paul M Loadman, John A Hartley, Terence C Jenkins, David E Thurston

Affiliations

Affiliation

1 Cancer Research UK Gene Targeted Drug Design Research Group, School of Pharmacy, University of London, 29/39 Brunswick Square, London WC1N 1AX, UK.

PMID: 18280154 DOI: 10.1016/j.bmcl.2008.01.083

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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