Abstract
A series of novel potential DNA bis-intercalators were designed and synthesized, in which two glucuronic acids were linked by ethylenediamine, and the glucuronic acid was coupled with various chromophores, including quinoline, acridine, indole and purine, at the C-1 position. The preliminary binding properties of these compounds to calf thymus DNA (CT-DNA) have been investigated by UV-absorption and fluorescence spectroscopy. The results indicated that all the target compounds can interact with CT-DNA, and the acridine derivative, 3b, showed the highest key selection vector (KSV) value, which suggested that compound 3b binds most strongly to CT-DNA.
Highlights
Numerous biological experiments have suggested that DNA is one of the primary cellular targets for many anticancer agents
We report the design and synthesis of four potential DNA bis-intercalators based on glucuronic acid (Figure 1)
The acetyl protected glucuronosyl donor was coupled with the derivatives of quinoline, acridine, purine and indole, respectively, to give the methyl-uronates
Summary
Numerous biological experiments have suggested that DNA is one of the primary cellular targets for many anticancer agents. The DNA interacting molecules are usually bound to DNA non-covalently by three modes: intercalation, groove binding and static electronic interactions. The targeting molecules interact with DNA in the base edges of the major groove or minor groove, which had been discussed by many groups [6,7,8,9,10]. The intercalation is another DNA binding mode that is closely related to the antitumor ability of many anticancer agents [11]
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