Abstract
In this study, we tried to improve the anticancer properties of two potential cytostatic agents based on benzo[c]fluorene, benfluron and dimefluron, by the synthesis of their C-7 derivatives. In the new derivatives, we observed the effect in Ehrlich tumour-bearing mice as well as in human MCF-7, BT-549 and MDA-MB-231 cells. All of the compounds tested showed a strong inhibitory effect in vitro. When tested in vivo, their systemic toxicity in vivo was promisingly low. Benfluron and its O-methyloxime as well as dimefluron and its oxime, thiosemicarbazone and hydrazone inhibited tumour growth in vivo. Only benfluron and hydrazone of dimefluron prolonged the survival. Proliferating cell nuclear antigen (PCNA) protein was decreased in tumours treated with benfluron and O-methyloxime of dimefluron in cancer tissue. Benfluron thiosemicarbazone increased the infiltration of tumour with T-lymphocytes. Taken together, all derivatives were more cytotoxic then their parent compounds, but not necessarily more effective in vivo.
Keywords: Anticancer effects, benzo[c]fluorene derivatives, cytotoxicity, MCF-7, solid Ehrlich tumour, synthesis.
Letters in Drug Design & Discovery
Title:Novel Derivatives of Benfluron and Dimefluron Synthesis and Anticancer activity
Volume: 12 Issue: 10
Author(s): Lenka Sucha, Marek Kolenic, Jiri Kratochvil, Milan Pour, Milan Nobilis, Eva Cermakova, Martina Rezacova and Pavel Tomsik
Affiliation:
Keywords: Anticancer effects, benzo[c]fluorene derivatives, cytotoxicity, MCF-7, solid Ehrlich tumour, synthesis.
Abstract: In this study, we tried to improve the anticancer properties of two potential cytostatic agents based on benzo[c]fluorene, benfluron and dimefluron, by the synthesis of their C-7 derivatives. In the new derivatives, we observed the effect in Ehrlich tumour-bearing mice as well as in human MCF-7, BT-549 and MDA-MB-231 cells. All of the compounds tested showed a strong inhibitory effect in vitro. When tested in vivo, their systemic toxicity in vivo was promisingly low. Benfluron and its O-methyloxime as well as dimefluron and its oxime, thiosemicarbazone and hydrazone inhibited tumour growth in vivo. Only benfluron and hydrazone of dimefluron prolonged the survival. Proliferating cell nuclear antigen (PCNA) protein was decreased in tumours treated with benfluron and O-methyloxime of dimefluron in cancer tissue. Benfluron thiosemicarbazone increased the infiltration of tumour with T-lymphocytes. Taken together, all derivatives were more cytotoxic then their parent compounds, but not necessarily more effective in vivo.
Export Options
About this article
Cite this article as:
Sucha Lenka, Kolenic Marek, Kratochvil Jiri, Pour Milan, Nobilis Milan, Cermakova Eva, Rezacova Martina and Tomsik Pavel, Novel Derivatives of Benfluron and Dimefluron Synthesis and Anticancer activity, Letters in Drug Design & Discovery 2015; 12 (10) . https://dx.doi.org/10.2174/1570180812666150529204508
DOI https://dx.doi.org/10.2174/1570180812666150529204508 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
The Prognostic Value of Long Non-Coding RNA <i>SNHG7</i> in Human Cancer: A Meta-Analysis
Current Pharmaceutical Biotechnology Role of Nicotinic Acetylcholine Receptors in Cardiovascular Physiology and Pathophysiology: Current Trends and Perspectives
Current Vascular Pharmacology Screening Novel SAHA Derivatives as Anti-lung Carcinoma Agents: Synthesis, Biological Evaluation, Docking Studies and Further Mechanism Research between Apoptosis and Autophagyetween Apoptosis and Autophagy
Anti-Cancer Agents in Medicinal Chemistry Combined Chemotherapy or Biotherapy with Jasmonates: Targeting Energy Metabolism for Cancer Treatment
Current Pharmaceutical Biotechnology Molecular Target-Guided Tumor Therapy with Natural Products Derived from Traditional Chinese Medicine
Current Medicinal Chemistry Comparative Proteomics of Liver of the Diabetic Obese db/db and Non-Obese or Diabetic Mice
Current Proteomics Potential of Nanocarriers in Genetic Immunization
Recent Patents on Drug Delivery & Formulation Regulators of Chemokine Receptor Activity as Promising Anticancer Therapeutics
Current Cancer Drug Targets DLX6-AS1: An Indispensable Cancer-related Long Non-coding RNA
Current Pharmaceutical Design Photoprotective Carotenoids Lutein and Zeaxanthin: Their Role in AMD
Current Nutrition & Food Science Effect of Curcumin on Pro-angiogenic Factors in the Xenograft Model of Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry Airway Stents: Current Practice and Future Directions
Current Respiratory Medicine Reviews A Review on Development and Characterization of a Cost-effective Targeted Quality-driven Antimalarial Product with an Emphasis on Phytosomes
Current Drug Targets Alteration of Cholinergic System in Keratinocytes Cells Produces Acantholysis: A Possible Use of Cholinergic Drugs in Pemphigus Vulgaris
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Pharmacological Cyclin-Dependent Kinase Inhibitors (PCIs) as Potential Antiviral Drugs
Anti-Infective Agents in Medicinal Chemistry Environmental Risk Assessment of Replication Competent Viral Vectors Applied in Clinical Trials: Potential Effects of Inserted Sequences
Current Gene Therapy Piecing the Fragments Together: Dynamical Insights into the Enhancement of BRD4-BD1 (BET Protein) Druggability in Cancer Chemotherapy Using Novel 8-methyl-pyrrolo[1,2-a]pyrazin-1(2H)-one Derivatives
Current Pharmaceutical Biotechnology The Critical Role of Vascular Endothelial Growth Factor in Tumor Angiogenesis
Current Cancer Drug Targets Peptides to Target Tumor Vasculature and Lymphatics for Improved Anti-Angiogenesis Therapy
Current Cancer Drug Targets Cell Metabolism Under Microenvironmental Low Oxygen Tension Levels in Stemness, Proliferation and Pluripotency
Current Molecular Medicine