Abstract
Acridine derivatives are interesting chemotherapeutic agents that were first used as antibacterial and antiparasite agents. In this review we wish to concentrate our attention on the anticancer properties of acridines used in clinics since the 1970s. Based on recent results, an outlook on antitumour acridine chemotherapy will be proposed. The biological activity of acridines is mainly attributed to the planarity of these aromatic structures, which can intercalate within the double-stranded DNA structure, thus interfering with the cellular machinery. Recent understanding of the mode of action of acridines leads to continuous and exciting research in this heterocyclic family. Indeed, biological targets such as topoisomerases I and II, telomerase/telomere and protein kinases emerge and allow the design of novel acridine-based patterns. This review further pinpoints the latest progress in the development of anticancer agents based on naturally occurring and synthetic acridines (e.g. acridones, pyridoacridines); for this matter in vitro/in vivo studies and clinical trial results will be discussed. The DNA-affinic property of acridine is also useful to vectorise drugs into cell nuclei and some applications in hypoxia-selective treatment, platinum or N-mustard derived conjugates will be reported. Some other properties including inhibition of multidrug resistance or potential impact on Alzheimer disease will be treated. It is noteworthy that the position and the nature of the substituent on the heterocyclic core are determinants for the biological property and selectivity observed. So, we wish also to disclose a summary of recent synthetic methodologies developed for acridine synthesis.
Keywords: Acridine, acridone, alkaloid, anticancer, antitumour, topoisomerases, telomerase, hypoxia, organic synthesis
Anti-Cancer Agents in Medicinal Chemistry
Title: Acridine and Acridone Derivatives, Anticancer Properties and Synthetic Methods: Where Are We Now?
Volume: 7 Issue: 2
Author(s): Philippe Belmont, Johann Bosson, Thomas Godet and Martin Tiano
Affiliation:
Keywords: Acridine, acridone, alkaloid, anticancer, antitumour, topoisomerases, telomerase, hypoxia, organic synthesis
Abstract: Acridine derivatives are interesting chemotherapeutic agents that were first used as antibacterial and antiparasite agents. In this review we wish to concentrate our attention on the anticancer properties of acridines used in clinics since the 1970s. Based on recent results, an outlook on antitumour acridine chemotherapy will be proposed. The biological activity of acridines is mainly attributed to the planarity of these aromatic structures, which can intercalate within the double-stranded DNA structure, thus interfering with the cellular machinery. Recent understanding of the mode of action of acridines leads to continuous and exciting research in this heterocyclic family. Indeed, biological targets such as topoisomerases I and II, telomerase/telomere and protein kinases emerge and allow the design of novel acridine-based patterns. This review further pinpoints the latest progress in the development of anticancer agents based on naturally occurring and synthetic acridines (e.g. acridones, pyridoacridines); for this matter in vitro/in vivo studies and clinical trial results will be discussed. The DNA-affinic property of acridine is also useful to vectorise drugs into cell nuclei and some applications in hypoxia-selective treatment, platinum or N-mustard derived conjugates will be reported. Some other properties including inhibition of multidrug resistance or potential impact on Alzheimer disease will be treated. It is noteworthy that the position and the nature of the substituent on the heterocyclic core are determinants for the biological property and selectivity observed. So, we wish also to disclose a summary of recent synthetic methodologies developed for acridine synthesis.
Export Options
About this article
Cite this article as:
Belmont Philippe, Bosson Johann, Godet Thomas and Tiano Martin, Acridine and Acridone Derivatives, Anticancer Properties and Synthetic Methods: Where Are We Now?, Anti-Cancer Agents in Medicinal Chemistry 2007; 7 (2) . https://dx.doi.org/10.2174/187152007780058669
DOI https://dx.doi.org/10.2174/187152007780058669 |
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
-
Minocycline and Doxycycline: More Than Antibiotics
Current Molecular Pharmacology Recent Advances in Neuro-Endocrine-Immune Interactions in the Pathophysiology of Rheumatoid Arthritis
Current Rheumatology Reviews Novel Anti-Inflammatory and Neuroprotective Agents for Parkinsons Disease
CNS & Neurological Disorders - Drug Targets Cytokines as a Precipitant of Depressive Illness: Animal and Human Studies
Current Pharmaceutical Design The Role of Neuronal Insulin/Insulin-Like Growth Factor-1 Signaling for the Pathogenesis of Alzheimer’s Disease: Possible Therapeutic Implications
CNS & Neurological Disorders - Drug Targets Diversity Oriented p-TSA Catalyzed Efficient and Environmentally Benign Synthetic Protocol for the Synthesis of Structurally Diverse Heteroannulated Benzothiazolopyrimidines
Current Organocatalysis Immune Responses to Fungal Infections and Therapeutic Implications
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Janus Molecule I: Dichotomous Effects of COMT in Neuropathic vs Nociceptive Pain Modalities
CNS & Neurological Disorders - Drug Targets The Role of Immunosuppressive Medications in the Pathogenesis of Hypertension and Efficacy and Safety of Antihypertensive Agents in Kidney Transplant Recipients
Current Medicinal Chemistry Pharmaceutical Nanotechnology United States Patent Watch (October – December 2014)
Pharmaceutical Nanotechnology Postpartum Depression in Women with the FMR1 Premutation
Current Psychiatry Reviews Recent Advances in the Design and Synthesis of Prednisolone and Methylprednisolone Conjugates
Current Pharmaceutical Design Mesenchymal Stem Cells and their Exosomes: Promising Therapeutics for Chronic Pain
Current Stem Cell Research & Therapy Depression in Dementia or Dementia in Depression? Systematic Review of Studies and Hypotheses
Current Alzheimer Research One Special Question to Start with: Can HIF/NFkB be a Target in Inflammation?
Endocrine, Metabolic & Immune Disorders - Drug Targets Ubiquitin Ligases as Key Elements for the Modulation of the Immune Response: An Insight in the Pathogenesis of Autoimmunity
Current Rheumatology Reviews The Role of P-Glycoprotein in Psychiatric Disorders: A Reliable Guard of the Brain?
Central Nervous System Agents in Medicinal Chemistry 1,2,3-Triazine Scaffold as a Potent Biologically Active Moiety: A Mini Review
Mini-Reviews in Medicinal Chemistry The Potentials of Uncariae Ramulus Cum Uncis for the Treatment of Migraine: Targeting CGRP in the Trigeminovascular System
Current Neuropharmacology Start Small and Stay Small: Minimizing Attrition in the Clinic with a Focus on CNS Therapeutics
Current Topics in Medicinal Chemistry