Abstract
Phenothiazines and its related compounds have shown diverse biological activities including psychotropic, anticancer and other pharmacological activities. Recent studies have suggested the possible interactions between phenothiazines and their physiological targets or potential receptors. New types of phenothiazine, such as half-mustard type phenothiazines and benzo[a]phenothiazines, have been synthesized. These compounds stimulated T-cell blast formation, natural killer cell activity (possibly via activation of monocytes and macrophages) and antibody-dependent cellular cytotoxicity of human peripheral blood mononuclear cells, and showed cytotoxicity against several human cancer cell lines. Benzo[a]phenothiazines induced monocytic differentiation and apoptotic cell death (characterized by internucleosomal DNA fragmentation) in human myelogenous leukemic cell lines, but not in other cancer cell lines. These compounds also induced antimicrobial activity in vivo, possibly by host-mediated immunopotentia tion. On the other hand, phenothiazines did not induce such immunopotentiation activity, but showed direct antibacterial activity in vitro. There was positive relation between their radical intensity and biological activities. These compounds did not show any apparent mutagenic activity, but rather be antimutagenic. These data suggest their possible applicability of half-mustard type phenothiazines and benzo[a]phenothiazines for cancer chemotherapy.
Keywords: Antitumor, Phenothiazines, Anticancer, Psychotropic, Benzo, T cell blast formation, Natural killer cell activity, Antimicrobial activity, GABA receptor
Current Drug Targets
Title: Antitumor Potential and Possible Targets of Phenothiazine-Related Compounds
Volume: 1 Issue: 3
Author(s): Noboru Motohashi, Masami Kawase, Setsuo Saito and Hiroshi Sakagami
Affiliation:
Keywords: Antitumor, Phenothiazines, Anticancer, Psychotropic, Benzo, T cell blast formation, Natural killer cell activity, Antimicrobial activity, GABA receptor
Abstract: Phenothiazines and its related compounds have shown diverse biological activities including psychotropic, anticancer and other pharmacological activities. Recent studies have suggested the possible interactions between phenothiazines and their physiological targets or potential receptors. New types of phenothiazine, such as half-mustard type phenothiazines and benzo[a]phenothiazines, have been synthesized. These compounds stimulated T-cell blast formation, natural killer cell activity (possibly via activation of monocytes and macrophages) and antibody-dependent cellular cytotoxicity of human peripheral blood mononuclear cells, and showed cytotoxicity against several human cancer cell lines. Benzo[a]phenothiazines induced monocytic differentiation and apoptotic cell death (characterized by internucleosomal DNA fragmentation) in human myelogenous leukemic cell lines, but not in other cancer cell lines. These compounds also induced antimicrobial activity in vivo, possibly by host-mediated immunopotentia tion. On the other hand, phenothiazines did not induce such immunopotentiation activity, but showed direct antibacterial activity in vitro. There was positive relation between their radical intensity and biological activities. These compounds did not show any apparent mutagenic activity, but rather be antimutagenic. These data suggest their possible applicability of half-mustard type phenothiazines and benzo[a]phenothiazines for cancer chemotherapy.
Export Options
About this article
Cite this article as:
Motohashi Noboru, Kawase Masami, Saito Setsuo and Sakagami Hiroshi, Antitumor Potential and Possible Targets of Phenothiazine-Related Compounds, Current Drug Targets 2000; 1 (3) . https://dx.doi.org/10.2174/1389450003349191
DOI https://dx.doi.org/10.2174/1389450003349191 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
Drug-Targeted Approach with Polymer Nanocomposites for Improved Therapeutics
Polymer nanocomposites have been recognized as an advanced and cutting-edge technique in drug targeting administration. These materials combine the unique features of nanoparticles with the adaptability of polymers to produce highly personalized drug administration devices. Integrating nanoparticles containing pharmaceuticals into a polymer matrix enables researchers to regulate the rates at ...read more
RNA Molecules in the Treatment of Human Diseases
Messenger and non-coding RNAs, including long and small transcripts, are mediators of gene expression. Gene expression at the RNA level shows significant aberrations in human diseases, including cancer, leukemia, lymphoma, cardiovascular diseases, and neurological disorders. Human transcripts serve either as biomarkers of diagnosis, prognosis, prediction of treatment response and/or therapy ...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
Related Articles
-
Application of dsRNA in Cancer Immunotherapy: Current Status and Future Trends
Anti-Cancer Agents in Medicinal Chemistry Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
Current Medicinal Chemistry Shared Signaling Pathways Between Endocrine and Immune System Receptors: The Model of Gamma Chain
Current Signal Transduction Therapy Proteomics to Unravel Platelet-Related Diseases and Identify Novel Anti-Platelet Drugs
Current Medicinal Chemistry MicroRNAs Associated with Overweight and Obesity in Childhood: A Systematic Review
MicroRNA Isoflavones, their Glycosides and Glycoconjugates. Synthesis and Biological Activity
Current Organic Chemistry Emerging Roles of MicroRNA-22 in Human Disease and Normal Physiology
Current Molecular Medicine Copper Complexes of Bioactive Ligands with Superoxide Dismutase Activity
Mini-Reviews in Medicinal Chemistry Organ Preservation by the Association of Chemotherapy and Radiotherapy in Invasive Bladder Cancer
Current Drug Therapy Contemporary Formulations for Drug Delivery of Anticancer Bioactive Compounds
Recent Patents on Anti-Cancer Drug Discovery An Overview of Phytochemical and Pharmacological Profile of <i>Morus alba</i> Linn
Current Bioactive Compounds Role of Peroxisome Proliferator-Activated Receptor Gamma (PPARγ) in Different Disease States: Recent Updates
Current Medicinal Chemistry Biology and Impact of Signal Transducers and Activators of Transcription and Their Regulators as Targets in Cancer Therapy
Current Signal Transduction Therapy Prevention and Therapy of Prostate Cancer: An Update on Alternatives for Treatment and Future Perspectives
Current Drug Therapy Rho Kinase and Angiogenesis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) NF-κB Blockers Gifted by Mother Nature: Prospectives in Cancer Cell Chemosensitization
Current Pharmaceutical Design Eph as a Target in Inflammation
Endocrine, Metabolic & Immune Disorders - Drug Targets Metabolic Response Assessment in Non-Small Cell Lung Cancer Patients after Platinum-Based Therapy: A Preliminary Analysis
Current Medical Imaging Soy Saponins and the Anticancer Effects of Soybeans and Soy-Based Foods
Current Medicinal Chemistry - Anti-Cancer Agents Insight to Physiology and Pathology of Zinc(II) Ions and Their Actions in Breast and Prostate Carcinoma
Current Medicinal Chemistry