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.
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
Anti-Cancer Agents in Medicinal Chemistry
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.
Export Options
About this article
Cite this article as:
Shen Wei, Deng Huimin and Gao Zhiqiang, Synthesis and Anticancer Properties of a Novel Bis-intercalator, Anti-Cancer Agents in Medicinal Chemistry 2013; 13 (4) . https://dx.doi.org/10.2174/1871520611313040011
DOI https://dx.doi.org/10.2174/1871520611313040011 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Is There a Clinical Future for Spermatogonial Stem Cells?
Current Stem Cell Research & Therapy CNS Drug Development – Lost in Translation?
Mini-Reviews in Medicinal Chemistry Current Trends in the Application of Nanoparticles in Drug Delivery
Current Medicinal Chemistry The Immunohistochemical Expression of the E-Cadherin, Alpha-Catenin,Beta-Catenin and Gamma Catenin Proteins in Epithelial Ovarian Tumours: Relationship with Clinicopathologic Parameters and Patient Survival
Current Women`s Health Reviews Histone Deacetylase Inhibitors: New Promise in the Treatment of Immune and Inflammatory Diseases
Current Drug Targets Nanovehicle-based Small Interfering RNA (siRNA) Delivery for Therapeutic Purposes: A New Molecular Approach in Pharmacogenomics
Current Clinical Pharmacology The Need for Diagnostic Criteria in Systemic Vasculitis
Current Immunology Reviews (Discontinued) Design, Synthesis and Anticancer Evaluation of 1,2,4-Oxadiazole Bearing Isoxazole-Pyrazole Derivatives
Letters in Organic Chemistry Meet Our Editorial Board Member
Current Traditional Medicine 21-Hydroxy-6,19-epoxyprogesterone: A Promising Therapeutic Agent and a Molecular Tool for Deciphering Glucocorticoid Action
Mini-Reviews in Medicinal Chemistry Targeting FLT3 Kinase in Acute Myelogenous Leukemia: Progress, Perils, and Prospects
Mini-Reviews in Medicinal Chemistry Editorial
Current Nutrition & Food Science Exploring Promises of siRNA in Cancer Therapeutics
Current Cancer Therapy Reviews S100A8/A9 Proteins in Diseases of the Exocrine Pancreas
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Clinical Applications of Gene Therapy in Head and Neck Cancer
Current Gene Therapy New Insights into Chemistry and Anti-Infective Potential of Triazole Scaffold
Current Medicinal Chemistry Approaches to Gastrointestinal Cytoprotection: From Isolated Cells, Via Animal Experiments to Healthy Human Subjects and Patients with Different Gastrointestinal Disorders
Current Pharmaceutical Design Paving Roads for New Drugs in Oncology
Recent Patents on Anti-Cancer Drug Discovery Vitamin E and Prostate Cancer: Current Evidence and Future Directions
Current Nutrition & Food Science A Review of Chemotherapy and Photodynamic Therapy for Lung Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry