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Synthesis and DNA binding properties of saturated distamycin analogues
Craig R Woods1, Nicolas Faucher, Bernd Eschgfaller
1Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, CA 92037, La Jolla, USA.
Bioorganic & Medicinal Chemistry Letters
|August 17, 2002
Abstract:
A series of saturated heterocyclic analogues of distamycin were prepared and examined. A fluorescent intercalator displacement (FID) assay conducted on p[dA]-p[dT] DNA to obtain C(50) values and a hairpin deoxyoligonucleotide containing an A/T-rich binding site was used to evaluate DNA binding affinity. It is observed that saturated heterocycles greatly reduce the DNA binding relative to distamycin.