Abstract
A series of symmetrical Schiff base derivatives (L1-L7) were designed by a one-pot condensation reaction of various aldehyde/ketone compounds with hydrazine under mild conditions (room temperature, 3 days), using ether as solvent and acetic acid as catalyst. The target products were characterized and analysed by 1H and 13C NMR, FT-IR and liquid chromatography mass spectrometry (LC/MS). Our research focuses on the identification of synthetically chemotherapeutic substances able to inhibit, delay, or reverse the process of carcinogenesis in several stages. The target compounds presenting two regions for SAR evaluation were screened for their activity toward MDA-MB-241 breast cancer cell proliferation for the first time. Compound (1E, 2E)-1,2-bis(1-(3-nitrophenyl)ethylidene) hydrazine (L6) showed significant inhibitory activity (IC50 = 7.08 µg/mL).
Keywords: Schiff bases, heterocycles, nitro, antitumor activity, breast cancer, cell proliferation.
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of Certain Symmetrical Schiff Bases as Inhibitors of MDA-MB-241 Human Breast Cancer Cell Proliferation
Volume: 13 Issue: 3
Author(s): Smaail Radi, Said Tighadouini, Olivier Feron, Olivier Riant and Yahia N. Mabkhot
Affiliation:
Keywords: Schiff bases, heterocycles, nitro, antitumor activity, breast cancer, cell proliferation.
Abstract: A series of symmetrical Schiff base derivatives (L1-L7) were designed by a one-pot condensation reaction of various aldehyde/ketone compounds with hydrazine under mild conditions (room temperature, 3 days), using ether as solvent and acetic acid as catalyst. The target products were characterized and analysed by 1H and 13C NMR, FT-IR and liquid chromatography mass spectrometry (LC/MS). Our research focuses on the identification of synthetically chemotherapeutic substances able to inhibit, delay, or reverse the process of carcinogenesis in several stages. The target compounds presenting two regions for SAR evaluation were screened for their activity toward MDA-MB-241 breast cancer cell proliferation for the first time. Compound (1E, 2E)-1,2-bis(1-(3-nitrophenyl)ethylidene) hydrazine (L6) showed significant inhibitory activity (IC50 = 7.08 µg/mL).
Export Options
About this article
Cite this article as:
Radi Smaail, Tighadouini Said, Feron Olivier, Riant Olivier and Mabkhot N. Yahia, Synthesis and Evaluation of Certain Symmetrical Schiff Bases as Inhibitors of MDA-MB-241 Human Breast Cancer Cell Proliferation, Letters in Drug Design & Discovery 2016; 13 (3) . https://dx.doi.org/10.2174/1570180812999150812165510
DOI https://dx.doi.org/10.2174/1570180812999150812165510 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
![](/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
-
Nanoemulsion Encapsulation and In Vitro SLN Models of Delivery for Cytotoxic Methotrexate
Current Drug Discovery Technologies DNA Methyltransferases Inhibitors from Natural Sources
Current Topics in Medicinal Chemistry Chemokines and their Receptors in Gut Homeostasis and Disease
Current Immunology Reviews (Discontinued) A Support Subset Algorithm and Its Application to Information Security Risk Assessment
Recent Patents on Engineering Design and Synthesis of Tri-substituted Imidazole Derivatives as CD73 Inhibitors for Their Anticancer Activity
Letters in Drug Design & Discovery Apigenin Bioisosteres: Synthesis and Evaluation of their Antioxidant, Antimicrobial, and Anticancer Activities
Letters in Organic Chemistry Depression has a Strong Relationship to Alterations in the Immune, Endocrine and Neural System
Current Psychiatry Reviews Proteasome Inhibitors in Cancer Therapy
Current Drug Targets Targeting Therapeutic and Imaging Agents to Folate Receptor Positive Tumors
Current Pharmaceutical Biotechnology Metabolomics: A Revolution for Novel Cancer Marker Identification
Combinatorial Chemistry & High Throughput Screening Molecular Pathways in the Progression of Hormone-Independent and Metastatic Prostate Cancer
Current Cancer Drug Targets A Structural Insight into Hydroxamic Acid Based Histone Deacetylase Inhibitors for the Presence of Anticancer Activity
Current Medicinal Chemistry Lipid-based siRNA Delivery Systems: Challenges, Promises and Solutions Along the Long Journey
Current Pharmaceutical Biotechnology Targeting Different Pathways Using Novel Combination Therapy in Triple Negative Breast Cancer
Current Cancer Drug Targets Nanomedicine and its Application in Treatment of Microglia-mediated Neuroinflammation
Current Medicinal Chemistry The Neurotensinergic System: A Target for Cancer Treatment
Current Medicinal Chemistry Drug Resistance: Challenges to Effective Therapy
Current Cancer Drug Targets CuAAC Click Chemistry Accelerates the Discovery of Novel Chemical Scaffolds as Promising Protein Tyrosine Phosphatases Inhibitors
Current Medicinal Chemistry Adenosine Analogues as Opposite Modulators of the Cisplatin Resistance of Ovarian Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Synthetic Androgens as Designer Supplements
Current Neuropharmacology