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
-
Prokinetic Agents and QT Prolongation: A Familiar Scene with New Actors
Current Drug Safety Patent Selections
Recent Patents on DNA & Gene Sequences SPR Imaging Biosensor for Aspartyl Cathepsins: Sensor Development and Application for Biological Material
Protein & Peptide Letters Transcatheter Aortic Valve Implantation Infective Endocarditis: Current Data and Implications on Prophylaxis and Management
Current Pharmaceutical Design The Epidermal Growth Factor Receptor as a Therapeutic Target in Glioblastoma Multiforme and other Malignant Neoplasms
Anti-Cancer Agents in Medicinal Chemistry Serum Cortisol, Hepcidin and Thyroid Hormone Levels in Neonates with Late-Onset Sepsis; Methodological Issues on Diagnostic and Prognostic Studies
Infectious Disorders - Drug Targets Hybrid Magnetic Nanostructures For Cancer Diagnosis And Therapy
Anti-Cancer Agents in Medicinal Chemistry Laparoscopic Approach for Surgical Staging in Early Endometrial Cancer
Current Women`s Health Reviews Analysis of DNA Microarray Data
Current Topics in Medicinal Chemistry Inhibition of NF-kB Activation and Cytokines Production in THP-1 Monocytes by 2-Styrylchromones
Medicinal Chemistry The Role of Ghrelin Signals in Breast Cancer- A Systematic Review
Current Signal Transduction Therapy Dihydroartemisinin and its Analogs: A New Class of Antitubercular Agents
Current Topics in Medicinal Chemistry Interplay of Drug-Metabolizing Enzymes and Transporters in Drug Absorption and Disposition
Current Drug Metabolism Immunoglobulin G Expression and its Potential Role in Primary and Metastatic Breast Cancers
Current Molecular Medicine Synthesis and Biological Evaluation of Quinazoline Derivatives as Potential Anticancer Agents (II)
Anti-Cancer Agents in Medicinal Chemistry Multidrug Resistance: Retrospect and Prospects in Anti-Cancer Drug Treatment
Current Medicinal Chemistry Better Targeting Melanoma: Options Beyond Surgery and Conventional Chemotherapy
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Anti-Cancer/Anti-Tumor
Current Bioactive Compounds Epigallocatechin-3-gallate(EGCG): Mechanisms and the Combined Applications
Combinatorial Chemistry & High Throughput Screening Role of p53 Gene in Breast Cancer: Focus on Mutation Spectrum and Therapeutic Strategies
Current Pharmaceutical Design