Abstract
In the course of our ongoing program dedicated to the synthesis of anti-proliferative compounds, we prepared new troglitazone derivatives bearing a biphenyle moiety. The chromane heterocycle was further replaced by imidazole and triazole derivatives. Many compounds exhibited fair to high activity towards various cancer cell lines. Among them, compound 17b reduced cell viability leading to only 22-34% viable cells in four cancer cell lines at 10 µM, but unfortunately also led to a low (13%) cell viability of non-malignant primary cultured human hepatocytes at 200 µM. Interestingly, compound 11b also reduced cell viability in colon and liver cancer cell lines (29% and 24% cell viability respectively at 10 µM), but maintained a high cell viability of non-malignant hepatocytes (reaching 71% cell viability at 200 µM), thus exhibiting a huge selectivity.
Keywords: Cancer, Chromane, Hepatotoxicity, Imidazole, Thiazolidine-2, 4-dione, Triazole, Troglitazone.
Letters in Drug Design & Discovery
Title:Synthesis and Anti-Proliferative Activity of New Biphenyle-Benzylidenethiazolidine- 2,4-dione Bis-Adducts Containing Various Heterocyclic Cores
Volume: 11 Issue: 3
Author(s): Maxime Meyer, Sandra Kuntz, Isabelle Grillier-Vuissoz, Helene Martin, Lysiane Richert, Stephane Flament, Yves Chapleur and Michel Boisbrun
Affiliation:
Keywords: Cancer, Chromane, Hepatotoxicity, Imidazole, Thiazolidine-2, 4-dione, Triazole, Troglitazone.
Abstract: In the course of our ongoing program dedicated to the synthesis of anti-proliferative compounds, we prepared new troglitazone derivatives bearing a biphenyle moiety. The chromane heterocycle was further replaced by imidazole and triazole derivatives. Many compounds exhibited fair to high activity towards various cancer cell lines. Among them, compound 17b reduced cell viability leading to only 22-34% viable cells in four cancer cell lines at 10 µM, but unfortunately also led to a low (13%) cell viability of non-malignant primary cultured human hepatocytes at 200 µM. Interestingly, compound 11b also reduced cell viability in colon and liver cancer cell lines (29% and 24% cell viability respectively at 10 µM), but maintained a high cell viability of non-malignant hepatocytes (reaching 71% cell viability at 200 µM), thus exhibiting a huge selectivity.
Export Options
About this article
Cite this article as:
Meyer Maxime, Kuntz Sandra, Grillier-Vuissoz Isabelle, Martin Helene, Richert Lysiane, Flament Stephane, Chapleur Yves and Boisbrun Michel, Synthesis and Anti-Proliferative Activity of New Biphenyle-Benzylidenethiazolidine- 2,4-dione Bis-Adducts Containing Various Heterocyclic Cores, Letters in Drug Design & Discovery 2014; 11 (3) . https://dx.doi.org/10.2174/15701808113106660080
DOI https://dx.doi.org/10.2174/15701808113106660080 |
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
-
RNA Binding Protein/RNA Element Interactions and the Control of Translation
Current Protein & Peptide Science Genome-wide Analysis of Myelodysplastic Syndromes
Current Pharmaceutical Design Efficient Silencing of Hepatitis B Virus by Helper-dependent Adenovirus Vector-mediated Delivery of Artificial Antiviral Primary Micro RNAs
MicroRNA Novel Chemotherapeutic Agents - The Contribution of Scorpionates
Current Medicinal Chemistry Recent Patents in Antiviral siRNAs
Recent Patents on Anti-Infective Drug Discovery Potential Therapeutic Application of Chondroitin Sulfate/Dermatan Sulfate
Current Drug Discovery Technologies The Cytotoxic and Mechanistic Effects of Aaptamine on Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Biomarkers for Early Detection of Liver Cancer: Focus on Clinical Evaluation
Protein & Peptide Letters Novel Therapeutic Strategies for Dementia
CNS & Neurological Disorders - Drug Targets Molecular Pathology of Sarcomas
Reviews on Recent Clinical Trials Synthetic Approaches to Functionalized Lipids for Protein Monolayer Crystallizations
Current Organic Chemistry CEBP Epigenetic Dysregulation as a Drug Target for the Treatment of Hematologic and Gynecologic Malignancies
Current Drug Targets Small Molecules Modulating Biogenesis or Processing of microRNAs with Therapeutic Potentials
Current Medicinal Chemistry Diabetes Gene Therapy: Potential and Challenges
Current Gene Therapy Performance of Feature Selection Methods
Current Genomics Drugging Cell Cycle Kinases in Cancer Therapy
Current Drug Targets Rhein Derivatives, A Promising Pivot?
Mini-Reviews in Medicinal Chemistry Combating P-glycoprotein-Mediated Multidrug Resistance Using Therapeutic Nanoparticles
Current Pharmaceutical Design Production of Lentivectors for Clinical Use
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Thioredoxin System Modulation by Plant and Fungal Secondary Metabolites
Current Medicinal Chemistry