Synthesis and DNA binding properties of saturated distamycin analogues.
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.
Department of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550North Torrey Pines Road, CA 92037, La Jolla, USA.
Craig R
CR
Woods
Nicolas
N
Faucher
Bernd
B
Eschgfaller
Kenneth W
KW
Bair
Dale L
DL
Boger
D004247:DNA / Q000378:metabolism*; D004214:Distamycins / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism*
D004214:Distamycins; C030000:stallimycin; D004247:DNA