Title:Synthesis and Anticancer Properties of a Novel Bis-intercalator
Volume: 13
Issue: 4
Author(s): Wei Shen, Huimin Deng and Zhiqiang Gao
Affiliation:
Keywords:
Anticancer, Bis-intercalator, C6 cell, Cancer, Circular dichroism spectroscopy, Cytotoxicity, DNA, Fluorometry, Hela cell,
Intercalator, MDA-435S cell, Naphthalene diimide, Threading intercalation, UV-Vis spectrometry, Viscometry
Abstract: A series of naphthalene diimide (ND)-based mono-, bis-, and tris-intercalators are synthesized and evaluated for their
anticancer activities. All compounds show anticancer activities in the micromolar range. Among them the bis-intercalator is the most
promising. Experimental results indicate that (i) target compounds intercalate DNA and (ii) the bis-intercalator with the optimal linker
shows considerably more affinity to DNA than corresponding mono-and tris-intercalators. Spectroscopic measurements indicate that the
ND groups bind to the double-stranded DNA (ds-DNA) in a classical threading intercalation mode, while the cationic linker reinforces
the intercalation via electrostatic interaction with ds-DNA. In vitro cytotoxicity of the bis-intercalator towards a number of cancer cells,
such as C6, HeLa, and MDA-435S, is tested and compared to that of normal cells. Attractive anticancer activity is observed with the bisintercalator,
which provides a new lead in the anticancer drug design strategy.
