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 |
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 Synthetic Lethality Approaches for Drug Combinations and Early Drug Development
Current Cancer Drug Targets Rapid Screening of Different Types of Antitumor Compound Groups from Traditional Chinese Medicine by Hollow Fiber Cell Fishing with High Performance Liquid Chromatography
Combinatorial Chemistry & High Throughput Screening Pharmacokinetic Profiles of Anticancer Herbal Medicines in Humans and the Clinical Implications
Current Medicinal Chemistry Application of NMR Metabolomics to Search for Human Disease Biomarkers
Combinatorial Chemistry & High Throughput Screening The Role of Metabolism in Toxicity of Polycyclic Aromatic Hydrocarbons and their Non-genotoxic Modes of Action
Current Drug Metabolism Breast Cancer in the Personal Genomics Era
Current Genomics Synchrotron Radiation in Life Sciences
Protein & Peptide Letters Review of Dose-intense Platinum and/or Paclitaxel Containing Chemotherapy in Advanced and Recurrent Epithelial Ovarian Cancer
Current Pharmaceutical Design Editorial (Thematic Issue: Combined Cancer Therapy)
Current Pharmaceutical Design IP6 & Inositol in Cancer Prevention and Therapy
Current Cancer Therapy Reviews Editorial [Hot Topic: Radiopharmaceuticals: Pre-Clinical Evaluation (Guest Editor: Maria Filomena Botelho)]
Current Radiopharmaceuticals Avian Cytokines - An Overview
Current Pharmaceutical Design Design and Synthesis of Some Newer Pyrimidine Hydroxamates as Histone Deacetylase Inhibitors
Current Enzyme Inhibition Evaluating Intestinal Permeability by Measuring Plasma Endotoxin and Diamine Oxidase in Children with Acute Lymphoblastic Leukemia Treated with High-dose Methotrexate
Anti-Cancer Agents in Medicinal Chemistry Biomarkers Determining Cardiovascular Risk in Patients with Kidney Disease
Current Medicinal Chemistry New Alkyl-Lipid Blockers of SK3 Channels Reduce Cancer Cell Migration and Occurrence of Metastasis
Current Cancer Drug Targets Renal and Hepatic Kinetics of Tc-99m-labelled Hexakis-methoxy-isobutyl Isonitrile
Drug Metabolism Letters C-KIT Signaling in Cancer Treatment
Current Pharmaceutical Design Role of Wnt/β-catenin Signaling in Drug Resistance of Pancreatic Cancer
Current Pharmaceutical Design Neurochemical and Neuropharmacological Aspects of Circadian Disruptions: An Introduction to Asynchronization
Current Neuropharmacology