Abstract
A series of novel Schiff bases -benzothiazole hybrids was designed, synthesized and evaluated for their anticancer activity by MTT assay and western blot method. Antiproliferative screening indicated that compound containing dihydroxy substituents had potent inhibitory activity with IC50 value 34µg/ml against SKOV3, A2780-S and A2780-CR cell lines. It showed more potent cytotoxicity in combination with cisplatin and paclitaxel than alone in the selected cell lines (SKOV3, A2780 and A2780-CR models). The in vitro cytotoxicity of the compounds on IOSE 364 cell line was evaluated to establish the selectivity. Molecular docking study exhibited good binding against epidermal growth factor receptor, which was further ascertained by immunoblot assay using specific antibody against phosphorylated EGFR, and thus unravelling the targeted anticancer mechanism.
Keywords: A2780-CR, A2780-PR, A2780-S, benzothiazole, schiff bases, SKOV3.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design and Synthesis of Novel Schiff Base-Benzothiazole Hybrids as Potential Epidermal Growth Factor Receptor (EGFR) Inhibitors
Volume: 16 Issue: 6
Author(s): Meenakshi Singh, Sudhir Kumar Singh, Bhushan Thakur, Pritha Ray and Sushil K. Singh
Affiliation:
Keywords: A2780-CR, A2780-PR, A2780-S, benzothiazole, schiff bases, SKOV3.
Abstract: A series of novel Schiff bases -benzothiazole hybrids was designed, synthesized and evaluated for their anticancer activity by MTT assay and western blot method. Antiproliferative screening indicated that compound containing dihydroxy substituents had potent inhibitory activity with IC50 value 34µg/ml against SKOV3, A2780-S and A2780-CR cell lines. It showed more potent cytotoxicity in combination with cisplatin and paclitaxel than alone in the selected cell lines (SKOV3, A2780 and A2780-CR models). The in vitro cytotoxicity of the compounds on IOSE 364 cell line was evaluated to establish the selectivity. Molecular docking study exhibited good binding against epidermal growth factor receptor, which was further ascertained by immunoblot assay using specific antibody against phosphorylated EGFR, and thus unravelling the targeted anticancer mechanism.
Export Options
About this article
Cite this article as:
Singh Meenakshi, Singh Kumar Sudhir, Thakur Bhushan, Ray Pritha and Singh K. Sushil, Design and Synthesis of Novel Schiff Base-Benzothiazole Hybrids as Potential Epidermal Growth Factor Receptor (EGFR) Inhibitors, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (6) . https://dx.doi.org/10.2174/1871520615666151007160115
DOI https://dx.doi.org/10.2174/1871520615666151007160115 |
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
-
Novel Aminopeptidase N Inhibitors with Improved Antitumor Activities
Letters in Drug Design & Discovery Nanotechnology Applications for Diffuse Intrinsic Pontine Glioma
Current Neuropharmacology Phytochemicals: Key to Effective Anticancer Drugs
Mini-Reviews in Organic Chemistry Isatoic Anhydride: A Fascinating and Basic Molecule for the Synthesis of Substituted Quinazolinones and Benzo di/triazepines
Current Organic Chemistry Application of Gene Therapy in Diabetes Care
Infectious Disorders - Drug Targets Best Practices and Emerging Trends for Market Access to Personalised Medicine in the US and EU: Learnings for Global Developed and Emerging Markets
Current Pharmacogenomics and Personalized Medicine Integrins and Cancer: Gene Expression, Epigenetics and Metastasis
Current Genomics Contribution of Platelet-Derived CD40 Ligand to Inflammation, Thrombosis and Neoangiogenesis
Current Medicinal Chemistry Anti-Angiogenic and Anti-Inflammatory Effects of Statins: Relevance to Anti-Cancer Therapy
Current Cancer Drug Targets Coumarin Compounds in Medicinal Chemistry: Some Important Examples from the Last Years
Current Topics in Medicinal Chemistry Docetaxel (Taxotere) in the Treatment of Non-Small Cell Lung Cancer
Current Medicinal Chemistry The Role of Mast Cells in the Structural Alterations of the Airways as a Potential Mechanism in the Pathogenesis of Severe Asthma
Current Pharmaceutical Design Optical and Multimodal Peptide-Based Probes for In Vivo Molecular Imaging
Anti-Cancer Agents in Medicinal Chemistry Predicting Drug Efficacy Using Integrative Models for Chronic Respiratory Diseases
Inflammation & Allergy - Drug Targets (Discontinued) Muscarinic Acetylcholine Receptor-Interacting Proteins (mAChRIPs): Targeting the Receptorsome
Current Drug Targets Targeting Vascular Endothelial Growth Factor Pathway in First-Line Treatment of Metastatic Colorectal Cancer: State-of-the-Art and Future Perspectives in Clinical and Molecular Selection of Patients
Current Cancer Drug Targets The STAT3 Inhibitor Stattic Impairs Cardiomyocyte Mitochondrial Function Through Increased Reactive Oxygen Species Formation
Current Pharmaceutical Design Targeted Tumor Diagnosis and Therapy with Peptide Hormones as Radiopharmaceuticals
Anti-Cancer Agents in Medicinal Chemistry Navigational Bronchoscopy in the Evaluation of the Peripheral Pulmonary Nodule.
Current Respiratory Medicine Reviews Retinoids in Cancer Chemoprevention
Current Cancer Drug Targets