Abstract
Background: Phenstatin and their derivatives display remarkable antiproliferative activity toward a wide variety of preclinical tumor models. Structural simplicity and excellent stability of phenstatins offer a stimulating premise for developing various derivatives with profound antimitotic activity and excellent cytotoxicity.
Objective: To do analysis of literature that phenstatins derivatives inhibit tubulin polymerization through their interaction at the colchicine binding site of microtubules and arrest the G2/M phase of the cell cycle. In addition, phenstatin derivatives are undergoing clinical evaluation as vascular targeting/disrupting agents and also exhibit direct antiangiogenic properties.
Methods: An organised well designed and appropriately managed search of bibliographic databases for peer-reviewed research literature using a focused review question and inclusion/ exclusion criteria has been done for this article.
Conclusion: In this review article, the synthesis and structure-activity relationships of phenstatin and a wide number of their reported analogues with modifications to ring A, ring B, and to the keto position are discussed in the perspective of medicinal chemistry with proper conclusion.
Keywords: Structure-activity relationship, Cytotoxic activity, Antimitotic activity, Tubulin polymerization inhibition, Colchicine binding site, phenstatins.
Current Medicinal Chemistry
Title:Recent Developments on Phenstatins as Potent Antimitotic Agents
Volume: 25 Issue: 20
Author(s): Xing Chen , Shi-Meng Wang , Gajjela Bharath Kumar, Grant A.L. Bare, Jing Leng, Syed Nasir Abbas Bukhari*Hua-Li Qin*
Affiliation:
- Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070,China
- Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, 205 Luoshi Road, Wuhan, 430070,China
Keywords: Structure-activity relationship, Cytotoxic activity, Antimitotic activity, Tubulin polymerization inhibition, Colchicine binding site, phenstatins.
Abstract: Background: Phenstatin and their derivatives display remarkable antiproliferative activity toward a wide variety of preclinical tumor models. Structural simplicity and excellent stability of phenstatins offer a stimulating premise for developing various derivatives with profound antimitotic activity and excellent cytotoxicity.
Objective: To do analysis of literature that phenstatins derivatives inhibit tubulin polymerization through their interaction at the colchicine binding site of microtubules and arrest the G2/M phase of the cell cycle. In addition, phenstatin derivatives are undergoing clinical evaluation as vascular targeting/disrupting agents and also exhibit direct antiangiogenic properties.
Methods: An organised well designed and appropriately managed search of bibliographic databases for peer-reviewed research literature using a focused review question and inclusion/ exclusion criteria has been done for this article.
Conclusion: In this review article, the synthesis and structure-activity relationships of phenstatin and a wide number of their reported analogues with modifications to ring A, ring B, and to the keto position are discussed in the perspective of medicinal chemistry with proper conclusion.
Export Options
About this article
Cite this article as:
Chen Xing , Wang Shi-Meng, Kumar Bharath Gajjela , Bare A.L. Grant, Leng Jing, Bukhari Nasir Abbas Syed *, Qin Hua-Li *, Recent Developments on Phenstatins as Potent Antimitotic Agents, Current Medicinal Chemistry 2018; 25 (20) . https://dx.doi.org/10.2174/0929867324666171106162048
DOI https://dx.doi.org/10.2174/0929867324666171106162048 |
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
- 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
-
Evaluation of Vitamin C as a Personalized Adjuvant Medicine: Pharmacogenomic Studies
Current Pharmacogenomics and Personalized Medicine Histone Deacetylase Inhibitors: A New Wave of Molecular Targeted Anticancer Agents
Recent Patents on Anti-Cancer Drug Discovery MicroRNAs in Organogenesis and Disease
Current Molecular Medicine Estrogen Receptor-α: Plasma Membrane Localization and Functions
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Poly(ADP-Ribosylation): Beneficial Effects of Its Inhibition
Current Enzyme Inhibition Circular RNAs and Glioma: Small Molecule with Big Actions
Current Molecular Medicine Fragment Based Strategies for Discovery of Novel HIV-1 Reverse Transcriptase and Integrase Inhibitors
Current Topics in Medicinal Chemistry Targeting ATP7A to Increase the Sensitivity of Neuroblastoma Cells to Retinoid Therapy
Current Cancer Drug Targets FoxO1 Inhibitors: The Future Medicine for Metabolic Disorders?
Current Diabetes Reviews Extracellular Ca<sup>2+</sup> Selectively Enhances Adriamycin-induced Cell Death in Human Hepatoma Cells
Current Cancer Drug Targets Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT
Current Medicinal Chemistry Interplay Between Cholesterol and Homocysteine in the Exacerbation of Amyloid-β Toxicity in Human Neuroblastoma Cells
CNS & Neurological Disorders - Drug Targets Exploring Protein-Protein Interactions with Synthetic Peptide Arrays
Mini-Reviews in Organic Chemistry The Paths to Neurodegeneration in Genetic Parkinson's Disease
CNS & Neurological Disorders - Drug Targets Antineoplastic Potential of Medicinal Plants
Recent Patents on Biotechnology Combination of Salinomycin and AZD3463 Reveals Synergistic Effect on Reducing the Viability of T98G Glioblastoma Cells
Anti-Cancer Agents in Medicinal Chemistry Potential Interactions between miRNAs and Hypoxia: A New Layer in Cancer Hypoxia
Anti-Cancer Agents in Medicinal Chemistry Drug Targets from Genetics: Alpha-Synuclein
CNS & Neurological Disorders - Drug Targets Functional Biomarkers: an Approach to Bridge Pharmacokinetics and Pharmacodynamics in Pediatric Clinical Trials
Current Pharmaceutical Design Peroxisome Proliferator Activated Receptor Gamma Coactivator 1 Alpha: An Emerging Target for Neuroprotection in Parkinson’s Disease
CNS & Neurological Disorders - Drug Targets