摘要
癌症是一个无声的杀手,仍然在全球造成重大的健康问题。在众多的生物靶点中,DNA是癌症化疗中最显著的靶点之一。由于其平面结构,菲及其衍生物通过插入DNA碱基对和抑制参与DNA合成的酶,表现出潜在的细胞毒性。然而,由于脱靶效应和耐药性,开发新型化疗药物将是值得称赞的。在这方面,我们对在过去五年内报道的发展菲基衍生物进行了详细的回顾。本文主要综述了融合菲衍生物的合成方面和策略,如(i)菲喹啉、菲喹啉、邻虫啉、邻酚毒素和二氢菲喹啉二氧衍生物,(ii)菲与其他具有药理意义的药效团结合物,以及(iii)菲-金属复合物。这篇综述还阐述了它们在亚微摩尔到纳摩尔范围内对各种癌细胞系的体外细胞毒性评价。此外,计算研究和构效关系(SARs)也已被提出,以突出所设计的同源物的基本特征。因此,本文综述将有助于今后在药物化学领域开发潜在的细胞毒性药物衍生物。
关键词: 抗癌,DNA插层,菲,分子对接,构效关系,药物化学。
Current Medicinal Chemistry
Title:The Syntheses and Medicinal Attributes of Phenanthrenes as Anticancer Agents: A Quinquennial Update
Volume: 29 Issue: 20
关键词: 抗癌,DNA插层,菲,分子对接,构效关系,药物化学。
摘要: Cancer is a silent killer and remains to pose major health problems globally. Amongst the several biological targets, DNA is one of the most striking targets in cancer chemotherapy. Owing to its planar structure, phenanthrene and its derivatives exhibit potential cytotoxicity by intercalating between the DNA base pairs and by inhibiting the enzymes that are involved in the synthesis of DNA. However, due to the off-target effects and resistance, the development of novel chemotherapeutic agents would be meritorious. In this regard, we present a detailed review on the development of phenanthrene-based derivatives reported in the last quinquennial. This review mainly focuses on the synthetic aspects and strategies to procure the fused phenanthrene derivatives such as (i) phenanthroindolizidines, phenanthroquinolizidine, phenanthroimidazoles, podophyllotoxin-based phenanthrenes, and dihydrophenanthrodioxine derivatives, (ii) phenanthrene conjugates with other pharmacologically significant pharmacophores, and (iii) phenanthrene-metal complexes. This review also edifies their potential in vitro cytotoxicity evaluation against various carcinoma cell lines in submicromolar to nanomolar ranges. Additionally, computational studies and structure-activity relationships (SARs) have also been presented to highlight the essential features of the designed congeners. Thus, this review would aid in the development of novel derivatives in future as potential cytotoxic agents in the field of medicinal chemistry.
Export Options
About this article
Cite this article as:
The Syntheses and Medicinal Attributes of Phenanthrenes as Anticancer Agents: A Quinquennial Update, Current Medicinal Chemistry 2022; 29 (20) . https://dx.doi.org/10.2174/0929867328666211018110223
DOI https://dx.doi.org/10.2174/0929867328666211018110223 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
![](/images/wayfinder.jpg)
- 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
- Announcements
Related Articles
-
QSAR Modeling for the Antimalarial Activity of 1,4-Naphthoquinonyl Derivatives as Potential Antimalarial Agents
Current Computer-Aided Drug Design Prevalence of Moderate to Severe Depressive Symptoms among Adults in the UAE: A Cross-sectional Study
New Emirates Medical Journal Predictive QSAR Modeling Workflow, Model Applicability Domains, and Virtual Screening
Current Pharmaceutical Design Revisiting Antipsychotic-induced Akathisia: Current Issues and Prospective Challenges
Current Neuropharmacology Melatonin and Its Therapeutic Potential in Neuroprotection
Central Nervous System Agents in Medicinal Chemistry Modulation of Protein-Protein Interactions by Stabilizing/Mimicking Protein Secondary Structure Elements
Current Topics in Medicinal Chemistry Synthesis and Evaluation of C-28 Oleanolic Acid Derivatives as Inhibitors of Glycogen Phosphorylase
Letters in Drug Design & Discovery Molecular Modeling Studies of Novel Fluoroquinolone Molecules
Current Drug Discovery Technologies An Insight into the Immunomodulatory Effects of Probiotics in the Prevention of COVID-19 Disease
Current Biotechnology Therapeutic Outlook of Pyrazole Analogs: A Mini Review
Mini-Reviews in Medicinal Chemistry Mycobacterial DNA GyrB Inhibitors: Ligand Based Pharmacophore Modelling and In Vitro Enzyme Inhibition Studies
Current Topics in Medicinal Chemistry The Type III Secretion System as a Source of Novel Antibacterial Drug Targets
Current Drug Targets Potential Polymorphic <i>CYP1A2</i> and <i>CYP2D6</i>-mediated Pharmacokinetic Interactions between Risperidone or Olanzapine and Selected Drugs Intended to Treat COVID-19
Drug Metabolism and Bioanalysis Letters Anti-Allergic Potential of Herbs and Herbal Natural Products - Activities and Patents
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Epidemiology of Coronavirus Disease Outbreak: The Italian Trends
Reviews on Recent Clinical Trials Management of Acute Aluminum Phosphide Poisoning: Has Anything Changed?
Drug Metabolism Letters Recent Advances in Medicinal Chemistry of Sulfonamides. Rational Design as Anti-Tumoral, Anti-Bacterial and Anti-Inflammatory Agents
Mini-Reviews in Medicinal Chemistry Induction of a Robust Humoral Response using HIV-1 VLP<sup>MPER-V3</sup> as a Novel Candidate Vaccine in BALB/c Mice
Current HIV Research Endothelin Receptor Antagonists: Another Potential Alternative for Cardiovascular Diseases
Current Drug Targets - Cardiovascular & Hematological Disorders Metabolism-based Drug-drug Interactions in Patients with Chronic Respiratory Diseases: A Review Focusing on Drugs Affecting the Respiratory System
Current Drug Metabolism