Abstract
The present study involves the design and synthesis of naphthoflavones as antiproliferative agents. The strategy presents naphthoflavones as hybrids of naphthyl based chalcones and flavones. A panel of human cancer cell lines were employed for the cytotoxicity studies. DK-13 exhibited significant cytoxicity against MiaPaCa-2 cell lines with IC50 value of 1.93 μM and 5.63 μM against MCF-7 cell lines. The compound DK-13 was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining, and mitochondrial membrane potential loss. The cell phase distribution studies indicated an increase from 11.26 % (control sample) to 55.19 % (sample treated with 20 μM compound DK-13) in the apoptotic population.
Keywords: Apoptosis, naphthoflavones, cytotoxicity, cell lines, design.
Anti-Cancer Agents in Medicinal Chemistry
Title:Naphthoflavones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation
Volume: 16 Issue: 7
Author(s): Dinesh Kumar, Onkar Singh, Kunal Nepali, PMS Bedi, Arem Qayum, Shashank Singh and Subheet K. Jain
Affiliation:
Keywords: Apoptosis, naphthoflavones, cytotoxicity, cell lines, design.
Abstract: The present study involves the design and synthesis of naphthoflavones as antiproliferative agents. The strategy presents naphthoflavones as hybrids of naphthyl based chalcones and flavones. A panel of human cancer cell lines were employed for the cytotoxicity studies. DK-13 exhibited significant cytoxicity against MiaPaCa-2 cell lines with IC50 value of 1.93 μM and 5.63 μM against MCF-7 cell lines. The compound DK-13 was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining, and mitochondrial membrane potential loss. The cell phase distribution studies indicated an increase from 11.26 % (control sample) to 55.19 % (sample treated with 20 μM compound DK-13) in the apoptotic population.
Export Options
About this article
Cite this article as:
Kumar Dinesh, Singh Onkar, Nepali Kunal, Bedi PMS, Qayum Arem, Singh Shashank and K. Jain Subheet, Naphthoflavones as Antiproliferative Agents: Design, Synthesis and Biological Evaluation, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (7) . https://dx.doi.org/10.2174/1871520616666160204113536
DOI https://dx.doi.org/10.2174/1871520616666160204113536 |
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
-
Role of Drug Metabolism in the Cytotoxicity and Clinical Efficacy of Anthracyclines
Current Drug Metabolism Effect of Selenium Enrichment of <i>Lenzites betulinus</i> and <i>Trametes hirsuta</i> Mycelia on Antioxidant, Antifungal and Cytostatics Potential
Current Pharmaceutical Biotechnology BRAF Inhibitor Therapy for Melanoma, Thyroid and Colorectal Cancers: Development of Resistance and Future Prospects
Current Cancer Drug Targets α-Methylene-γ-lactones as a Novel Class of Anti-leukemic Agents
Anti-Cancer Agents in Medicinal Chemistry iPSCs Derived from Malignant Tumor Cells: Potential Application for Cancer Research
Current Stem Cell Research & Therapy Patent Selections
Recent Patents on Inflammation & Allergy Drug Discovery Type I Interferons: Ancient Peptides with Still Under-Discovered Anti-Cancer Properties
Protein & Peptide Letters Optimization of Lentiviral Vectors Generation for Biomedical and Clinical Research Purposes: Contemporary Trends in Technology Development and Applications
Current Gene Therapy Approaches to Quantification of RNA Targets by PCR Based Techniques
Current Genomics The Medicinal Chemistry Implications of the Anticancer Effects of Aspirin and Other NSAIDs
Mini-Reviews in Medicinal Chemistry Tyrosine Kinase Inhibitors – A Review on Pharmacology, Metabolism and Side Effects
Current Drug Metabolism Yin and Yang of Polyphenols in Cancer Prevention: A Short Review
Anti-Cancer Agents in Medicinal Chemistry Novel and Emerging Drugs for Acute Lymphoblastic Leukemia
Current Cancer Drug Targets Editorial [Hot Topic: Beyond Chemotherapy: Future Directions in Lymphoma Treatment (Guest Editor: Thomas Decker)]
Current Drug Targets “Momordica balsamina: A Medicinal and Neutraceutical Plant for Health care Management”. Comments: Biotechnological Potential of M. balsamina Revealed
Current Pharmaceutical Biotechnology Bladder Cancer: A Simple Model Becomes Complex
Current Genomics ROCK Inhibitors as Emerging Therapeutic Candidates for Sarcomas
Current Cancer Drug Targets The Stem Cell Factor Receptor/c-Kit as a Drug Target in Cancer
Current Cancer Drug Targets Yeast as a Powerful Model System for the Study of Apoptosis Regulation by Protein Kinase C Isoforms
Current Pharmaceutical Design Aminopeptidases of Malaria Parasites: New Targets for Chemotherapy
Infectious Disorders - Drug Targets