Abstract
Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-γ (PPAR- γ) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-γ agonists, novel analogues of oxazol-5-ones (3a-3q) were designed and virtually analyzed for their molecular and drug like properties. The newly synthesized compounds were further evaluated for their preliminary cytotoxicity in a panel of eight cancer cell lines using four concentrations at 10- fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. All the compounds demonstrated distinct effect in the extent of cytotoxicity in the breast cancer cell line MCF-7 with 3g specifically exhibiting partial PPAR-γ agonist activity and adipogenesis stimulating ability.
Keywords: Akt/mTOR/p70S6 signalling, Cancer, Sulforhodamine B.
Anti-Cancer Agents in Medicinal Chemistry
Title:Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines
Volume: 14 Issue: 6
Author(s): Tanushree Pal, Hardik Joshi and C.S. Ramaa
Affiliation:
Keywords: Akt/mTOR/p70S6 signalling, Cancer, Sulforhodamine B.
Abstract: Recent era aims at developing safer partial Peroxisome proliferator-activated receptor-γ (PPAR- γ) agonists in order to dodge the toxicity issues related to full agonists. With a view to develop non-thiazolidinediones as partial PPAR-γ agonists, novel analogues of oxazol-5-ones (3a-3q) were designed and virtually analyzed for their molecular and drug like properties. The newly synthesized compounds were further evaluated for their preliminary cytotoxicity in a panel of eight cancer cell lines using four concentrations at 10- fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. All the compounds demonstrated distinct effect in the extent of cytotoxicity in the breast cancer cell line MCF-7 with 3g specifically exhibiting partial PPAR-γ agonist activity and adipogenesis stimulating ability.
Export Options
About this article
Cite this article as:
Pal Tanushree, Joshi Hardik and Ramaa C.S., Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines, Anti-Cancer Agents in Medicinal Chemistry 2014; 14 (6) . https://dx.doi.org/10.2174/1871520614666140528155118
DOI https://dx.doi.org/10.2174/1871520614666140528155118 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- 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
-
Improvement of Tumor Localization of Photosensitizers for Photodynamic Therapy and Its Application for Tumor Diagnosis
Current Topics in Medicinal Chemistry Angiogenesis: A Target for Cancer Therapy
Current Pharmaceutical Design Thiol Proteases: Inhibitors and Potential Therapeutic Targets
Current Medicinal Chemistry Synthesis, Biological Evaluation and Molecular Docking Studies Against EGFR Tyrosine Kinase of 3,5-bis(substituted benzylidene)-1- ethylpiperidin-4-one Analogues
Letters in Organic Chemistry BRCA Mutational Status is a Promising Predictive Biomarker for Platinum- based Chemotherapy in Triple-Negative Breast Cancer
Current Drug Targets Can the Status of the Breast and Ovarian Cancer Susceptibility Gene 1 Product (BRCA1) Predict Response to Taxane-Based Cancer Therapy?
Anti-Cancer Agents in Medicinal Chemistry Nanoparticulate Drug Delivery to Colorectal Cancer: Formulation Strategies and Surface Engineering
Current Pharmaceutical Design Anti-VEGF Strategies – from Antibodies to Tyrosine Kinase Inhibitors: Background and Clinical Development in Human Cancer
Current Pharmaceutical Design Raloxifene and Cardiovascular Health: Its Relationship to Lipid and Glucose Metabolism, Hemostatic and Inflammation Factors and Cardiovascular Function in Postmenopausal Women
Current Pharmaceutical Design Preface
Current Radiopharmaceuticals Withdrawal Notice: Electrophoresis as a Tool for Early Cancer Diagnosis
Anti-Cancer Agents in Medicinal Chemistry The Therapeutic Target Hsp90 and Cancer Hallmarks
Current Pharmaceutical Design Mutation Mechanisms of Breast Cancer among the Female Population in China
Current Bioinformatics Exploring PLAC1 Structure and Underlying Mechanisms to Design a Derivative Vaccine Against Breast Cancer Progression; <i>In-Silico</i> Study
Current Proteomics Risk Factors for Node Affectation and Recurrence in Endometrial Cancer
Current Women`s Health Reviews Tyrosine Kinase Inhibitors – A Review on Pharmacology, Metabolism and Side Effects
Current Drug Metabolism Understanding the Molecular Mechanisms of Rifaximin in the Treatment of Gastrointestinal Disorders – A Focus on the Modulation of Host Tissue Function
Mini-Reviews in Medicinal Chemistry Induced Pluripotent Stem Cells (iPSCs) Derived from Different Cell Sources and their Potential for Regenerative and Personalized Medicine
Current Molecular Medicine Graphical Abstracts
Letters in Drug Design & Discovery Heat Shock Protein 70s as Potential Molecular Targets for Colon Cancer Therapeutics
Current Medicinal Chemistry