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
-
A Medicinal Chemist’s Perspective Towards Structure Activity Relationship of Heterocycle Based Anticancer Agents
Current Topics in Medicinal Chemistry The Psychopharmacology of Appetite: Targets for Potential Anti-Obesity Agents
Current Medicinal Chemistry - Central Nervous System Agents Curcumin and Immunity
Current Bioactive Compounds Bioactive Peptides in Preventative Healthcare: An Overview of Bioactivities and Suggested Methods to Assess Potential Applications
Current Pharmaceutical Design Genetically Engineered Elastin-based Biomaterials for Biomedical Applications
Current Medicinal Chemistry Evaluation of a Genetic Counseling Aid for Hereditary Breast and Ovarian Cancer
Applied Clinical Research, Clinical Trials and Regulatory Affairs New Organ-Specific Drug Strategies Interfering in Signaling Pathways: Kinase Inhibitors and Other New Developmental Drugs in HCC
Current Signal Transduction Therapy Therapeutic Potential of Hammerhead Ribozymes in the Treatment of Hyper-Proliferative Diseases
Current Pharmaceutical Biotechnology Antiangiogenesis and Radiotherapy: What Is the Role of Combined Modality Treatment?
Current Medicinal Chemistry - Anti-Cancer Agents Active Targeted Drug Delivery for Microbes Using Nano-Carriers
Current Topics in Medicinal Chemistry Delineation of Current Development of Antimitotic Compounds Targeting Cytoskeletal Protein Tubulin and Microtubule in the Cancer Therapy
Current Chemical Biology Synthesis, Molecular Docking Study, and Cytotoxic Activity of 3,4-diaryl-5-(4-pyridinyl)-1,2,4-oxadiazole
Medicinal Chemistry Computational Drug Repositioning: A Lateral Approach to Traditional Drug Discovery?
Current Topics in Medicinal Chemistry Synthesis, Characterization, Molecular Docking, In Vitro Biological Evaluation and In Vitro Cytotoxicity Study of Novel Thiazolidine-4-One Derivatives as Anti-Breast Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry MicroRNAs and Physical Activity
MicroRNA Molecular Profiles of Sentinel and Non-Sentinel Lymph Nodes in Breast Cancer Progression and Prognosis
Current Cancer Therapy Reviews Autism Spectrum Disorder Detection with Machine Learning Methods
Current Psychiatry Research and Reviews Genes that Modulate the Sensitivity for Anti-Microtubule Drug-Mediated Chemotherapy
Current Cancer Drug Targets Geminin as A Molecular Target for the Development of New Anticancer Drugs
Mini-Reviews in Medicinal Chemistry Design, Synthesis and Evaluation of Quinoline-based Small Molecule Inhibitor of STAT3
Letters in Drug Design & Discovery