Abstract
The development of a series of potent and selective antitumour agents, the 2-(4- aminophenyl)benzothiazoles, is described. The original lead compound in this series, CJM 126, exhibits nanomolar in vitro activity against certain human breast cancer cell lines. Structure-activity relationship studies within this simple antitumour benzothiazole pharmacophore revealed that 2-(4-aminophenyl) benzothiazoles bearing a 3- methyl, 3-bromo, 3-iodo or 3-chloro substituent are especially potent, extending the spectrum of in vitro antitumour activity to ovarian, lung, renal and colon carcinoma cell lines with a remarkable selectivity profile (NCI analysis). Other interesting features of this series include the highly unusual transient biphasic dose response relationship and possible unique mechanism of action (NCI COMPARE analysis). 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) has been selected as the lead compound in this series on the basis of superior in vivo results.
Current Medicinal Chemistry
Title: The Discovery of the Potent and Selective Antitumour Agent 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) and Related Compounds
Volume: 8 Issue: 2
Author(s): T. D. Bradshaw, M.F. G. Stevens and A. D. Westwell
Affiliation:
Abstract: The development of a series of potent and selective antitumour agents, the 2-(4- aminophenyl)benzothiazoles, is described. The original lead compound in this series, CJM 126, exhibits nanomolar in vitro activity against certain human breast cancer cell lines. Structure-activity relationship studies within this simple antitumour benzothiazole pharmacophore revealed that 2-(4-aminophenyl) benzothiazoles bearing a 3- methyl, 3-bromo, 3-iodo or 3-chloro substituent are especially potent, extending the spectrum of in vitro antitumour activity to ovarian, lung, renal and colon carcinoma cell lines with a remarkable selectivity profile (NCI analysis). Other interesting features of this series include the highly unusual transient biphasic dose response relationship and possible unique mechanism of action (NCI COMPARE analysis). 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) has been selected as the lead compound in this series on the basis of superior in vivo results.
Export Options
About this article
Cite this article as:
Bradshaw D. T., Stevens G. M.F. and Westwell D. A., The Discovery of the Potent and Selective Antitumour Agent 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203) and Related Compounds, Current Medicinal Chemistry 2001; 8 (2) . https://dx.doi.org/10.2174/0929867013373714
DOI https://dx.doi.org/10.2174/0929867013373714 |
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
-
Role of P-Glycoprotein in the Intestinal Absorption of Tanshinone IIA, a Major Active Ingredient in the Root of Salvia miltiorrhiza Bunge
Current Drug Metabolism A Fluorescent Alkyllysophospholipid Analog Exhibits Selective Cytotoxicity Against the Hormone-Insensitive Prostate Cancer Cell Line PC3
Anti-Cancer Agents in Medicinal Chemistry Formulation, Optimization and <i>In vitro / In vivo</i> Characterization of Spray Dried Doxorubicin Loaded Folic Acid Conjugated Gelatin Nanoparticles
Current Molecular Pharmacology Regulation of Polymorphonuclear Leukocyte-Intestinal Epithelial Cell Interactions: Signalling Events and Potential Drug Targets
Current Signal Transduction Therapy The Emerging Role of Metabotropic Glutamate Receptors in the Pathophysiology of Chronic Stress-Related Disorders
Current Neuropharmacology Pharmacological Tools to Activate Microglia and their Possible use to Study Neural Network Patho-physiology
Current Neuropharmacology Radiolabelled Probes Targeting Infection and Inflammation for Personalized Medicine
Current Pharmaceutical Design Distinctive Phenotype Identification for Breast Cancer Genotypes Among Hereditary Breast Cancer Mutated Genes
Current Bioinformatics Reflecting Back to Bring Nitric Oxide Research to the Laboratory
Current Medicinal Chemistry Anticancer Evaluation of 3,4,5,4'-trans-tetramethoxystilbene (DMU-212) and Its Analogs Against an Extensive Panel of Human Tumor Cell Lines
Letters in Drug Design & Discovery Signalling Pathways Activated by Ultraviolet Radiation: Role in Ocular and Cutaneous Health
Current Pharmaceutical Design Application of Mesenchymal Stem Cells in Melanoma: A Potential Therapeutic Strategy for Delivery of Targeted Agents
Current Medicinal Chemistry Targeting Histone Deacetylases for the Treatment of Immune, Endocrine & Metabolic Disorders
Endocrine, Metabolic & Immune Disorders - Drug Targets Curcumin as an Adjunct Therapy and microRNA Modulator in Breast Cancer
Current Pharmaceutical Design In Silico and Biochemical Analyses Identify Quinone Reductase 2 as a Target of Piceatannol
Current Medicinal Chemistry Chemical Structure Characteristics and Bioactivity of Small Molecule FAK Inhibitors
Anti-Cancer Agents in Medicinal Chemistry Methionine-Derived Metabolites in Apoptosis: Therapeutic Opportunities for Inhibitors of their Metabolism in Chemoresistant Cancer Cells
Current Medicinal Chemistry The Delivery of Personalised, Precision Medicines <i>via</i> Synthetic Proteins
Drug Delivery Letters Fatty Acid Synthase: A Target for the Reversal of Liver Steatosis
Current Enzyme Inhibition Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres
Current Pharmaceutical Design