Synthesis and Anticancer Properties of a Novel Bis-intercalator

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Synthesis and Anticancer Properties of a Novel Bis-intercalator

Anti-Cancer Agents in Medicinal Chemistry, 13(4): 632-638.

Author(s): Wei Shen, Huimin Deng and Zhiqiang Gao.

Affiliation: Department of Chemistry, National University of Singapore, Singapore 117543.


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.


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.

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Article Details

Volume: 13
Issue Number: 4
First Page: 632
Last Page: 638
Page Count: 7
DOI: 10.2174/1871520611313040011
Price: $58
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