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Nucleic Acids Research, Vol 25, Issue 11 2121-2128, Copyright © 1997 by Oxford University Press

ARTICLES

Synthesis and binding properties of conjugates between oligodeoxynucleotides and daunorubicin derivatives

A Garbesi, S Bonazzi, S Zanella, ML Capobianco, G Giannini and F Arcamone
I.Co.CEA-CNR, Via P.Gobetti 101, 40129 Bologna, Italy. garbesi@area.bo.cnr.it

Conjugation of an anthracycline to a triplex-forming oligonucleotide (TFO) allows delivery of this drug to a specific DNA site, preserving the intercalation geometry of this class of anticancer agents. Conjugate 11, in which the TFO is linked via a hexamethylene bridge to the O-4 on the D ring of the anthraquinone moiety, affords the most stable triple helix, through intercalation of the planar chromophore between DNA bases and binding of both the TFO and the amino sugar to the major and the minor groove respectively.
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