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