Abstract
British developed Bisdioxopiperazine compound (Biz compounds) {ICRF-159 or ICRF-187 (razoxane, Raz)} which was the first agent ever to be observed inhibiting and controlling the spontaneous pulmonary metastases of murine Lewis Lung Carcinoma (LLC) tumor model worldwide. Since 1980, two new Biz compounds {probimane (Pro, AT-2153, MST-2) and MST-16} have been synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, PR China, based on structural modifications from British developed Biz compounds. Despite some similarities and differences of structural and pharmacological activities observed between Raz, Pro and MST-16, the systematic comparisons of their pharmacological activities and mechanisms, especially on neoplasm metastases, are still much needed. This work demonstrates that Biz compounds may inhibit tumor cell migration in vitro through a Matrigel-Coated Transwell plate assay and a wound-healing assay by using three human mammary tumor cell lines (MDA-MB-231, MDA-MB-435 and MDA-MB-468). Pro, ICRF-187 and MST-16 affect the network of actin assembly. We conclude that Biz compounds might inhibit neoplasm metastases via affecting a cascade of GTPases, cell skeleton polarizations and cell movements.
Keywords: Bisdioxopiperazine compounds, razoxane, probimane, MST-16, neoplasm metastasis, cell movement, GTPses, actin, mammary cancer, MTX assay, cell migration
Anti-Cancer Agents in Medicinal Chemistry
Title: Cell Biological Manifestations of Bisdioxopiperazines: Treatment of Human Tumor Cell Lines in Culture
Volume: 10 Issue: 9
Author(s): Da-Yong Lu, Ding-Ren Lu and Jian Ding
Affiliation:
Keywords: Bisdioxopiperazine compounds, razoxane, probimane, MST-16, neoplasm metastasis, cell movement, GTPses, actin, mammary cancer, MTX assay, cell migration
Abstract: British developed Bisdioxopiperazine compound (Biz compounds) {ICRF-159 or ICRF-187 (razoxane, Raz)} which was the first agent ever to be observed inhibiting and controlling the spontaneous pulmonary metastases of murine Lewis Lung Carcinoma (LLC) tumor model worldwide. Since 1980, two new Biz compounds {probimane (Pro, AT-2153, MST-2) and MST-16} have been synthesized at the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, PR China, based on structural modifications from British developed Biz compounds. Despite some similarities and differences of structural and pharmacological activities observed between Raz, Pro and MST-16, the systematic comparisons of their pharmacological activities and mechanisms, especially on neoplasm metastases, are still much needed. This work demonstrates that Biz compounds may inhibit tumor cell migration in vitro through a Matrigel-Coated Transwell plate assay and a wound-healing assay by using three human mammary tumor cell lines (MDA-MB-231, MDA-MB-435 and MDA-MB-468). Pro, ICRF-187 and MST-16 affect the network of actin assembly. We conclude that Biz compounds might inhibit neoplasm metastases via affecting a cascade of GTPases, cell skeleton polarizations and cell movements.
Export Options
About this article
Cite this article as:
Lu Da-Yong, Lu Ding-Ren and Ding Jian, Cell Biological Manifestations of Bisdioxopiperazines: Treatment of Human Tumor Cell Lines in Culture, Anti-Cancer Agents in Medicinal Chemistry 2010; 10 (9) . https://dx.doi.org/10.2174/187152010794479843
DOI https://dx.doi.org/10.2174/187152010794479843 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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
Related Articles
-
Application of Diet-derived Taste Active Components for Clinical Nutrition: Perspectives from Ancient AyurvedicMedical Science, Space Medicine, and Modern Clinical Nutrition
Current Pharmaceutical Design The Endocannabinoid System in Parkinsons Disease
Current Pharmaceutical Design Molecule of the Month
Current Topics in Medicinal Chemistry Will Antiangiogenic Agents be a Future for Mesothelioma Therapy?
Current Medicinal Chemistry Preface
Current Pharmaceutical Design Role of Progesterone in Human Astrocytomas Growth
Current Topics in Medicinal Chemistry Current Trends in the Chemotherapy of Colorectal Cancer
Current Medicinal Chemistry Organ Preservation by the Association of Chemotherapy and Radiotherapy in Invasive Bladder Cancer
Current Drug Therapy Monoclonal Antibodies Against Epidermal Growth Factor Receptor in Advanced Colorectal Carcinoma: Clinical Efficacy and Markers of Sensitivity&#
Reviews on Recent Clinical Trials The Effect of Lipoic Acid on Macro and Trace Metal Levels in Living Tissues Exposed to Oxidative Stress
Anti-Cancer Agents in Medicinal Chemistry Efficient Colonic Delivery of DsiRNA by Pectin-Coated Polyelectrolyte Complex Nanoparticles: Preparation, Characterization and Improved Gastric Survivability
Current Drug Delivery Aryl and Acyclic Unsaturated Derivatives of Thioguanine and 6- Mercaptopurine: Synthesis and Cytotoxic Activity
Letters in Drug Design & Discovery Vitamin D Analogs as Modulators of Vitamin D Receptor Action
Current Topics in Medicinal Chemistry Synthesis, Molecular Docking Study, and Cytotoxic Activity of 1,3,5-triaryl Pyrazole Derivatives
Letters in Drug Design & Discovery Bone Marker in Women with Breast Cancer
Current Biomarkers (Discontinued) Delivery Systems for Birch-bark Triterpenoids and their Derivatives in Anticancer Research
Current Medicinal Chemistry Nuclear Hormone Receptor Signals as New Therapeutic Targets for Urothelial Carcinoma
Current Cancer Drug Targets A Potencial Theranostic Agent for EGF-R Expression Tumors: 177Lu- DOTA-Nimotuzumab
Current Radiopharmaceuticals Structural Comparison of Gene Relevance Networks for Breast Cancer Tissues in Different Grades
Combinatorial Chemistry & High Throughput Screening Polymeric Materials and Formulation Technologies for Modified-Release Tablet Development
Mini-Reviews in Medicinal Chemistry