Fluorescent 7-Diethylaminocoumarin Pyrrolobenzodiazepine conjugates: Synthesis, DNA-Interaction, Cytotoxicity and Differential Cellular Localization.

Description

No / 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 abstract
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.

Links & Downloads

1. Wells, G., Suggitt, M., Coffils, M., Baig, M.A.H., Howard, P.W., Loadman, P.M., Hartley, J.A., Jenkins, T.C. and Thurston, D.E. (2008). Fluorescent 7-diethylaminocoumarin pyrrolobenzodiazepine conjugates: Synthesis, DNA interaction, cytotoxicity and differential cellular localization. Bioorganic & Medicinal Chemistry Letters, Vol. 18, No. 6, pp. 2147-2151.
2. http://hdl.handle.net/10454/4569
3. https://doi.org/10.1016/j.bmcl.2008.01.083

Tags

Pyrrolobenzodiazepine

PBDs

DNA-binding

DNA sequence-selective

Fluorescence conjugates

Nuclear penetration

Anticancer agents

Antitumour agents

Additional Fields

Identifer	oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/4569
Date	January 2008
Creators	Wells, G., Suggitt, Marie, Coffils, M., Baig, M.A.H., Howard, P.W., Loadman, Paul, Hartley, J.A., Jenkins, Terence C., Thurston, D.E.
Source Sets	Bradford Scholars
Language	English
Detected Language	English
Type	Article, No full-text in the repository