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.
Graphical Abstract
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
-
Prediction of Cancer Rescue p53 Mutants In Silico Using Naïve Bayes Learning Methodology
Protein & Peptide Letters Chemoprevention of Colorectal Cancer: Ready for Routine Use?
Current Topics in Medicinal Chemistry Methotrexate-Induced Pneumonitis: Heterogeneity of Bronchoalveolar Lavage and Differences between Cancer and Rheumatoid Arthritis
Inflammation & Allergy - Drug Targets (Discontinued) The Fate of Nanoparticles In Vivo and the Strategy of Designing Stealth Nanoparticle for Drug Delivery
Current Drug Targets Targeted Therapies in the Treatment of Advanced Renal Cell Carcinoma
Recent Patents on Anti-Cancer Drug Discovery Antineoplastic Chemotherapy Induced QTc Prolongation
Current Drug Safety Current Strategies to Target the Anti-Apoptotic Bcl-2 Protein in Cancer Cells
Current Medicinal Chemistry Design of Lipophilic Prodrugs to Improve Drug Delivery and Efficacy
Current Drug Targets Immune Checkpoint Inhibitors for Non-small-cell Lung Cancer: Does that Represent a ‘New Frontier’?
Anti-Cancer Agents in Medicinal Chemistry Computational Approaches for Predicting Causal Missense Mutations in Cancer Genome Projects
Current Bioinformatics The Human L1 Element: A Potential Biomarker in Cancer Prognosis, Current Status and Future Directions
Current Molecular Medicine From Na+/K+-ATPase and Cardiac Glycosides to Cytotoxicity and Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Synthesis and Evaluation of New Thiazolyl Hydrazone Derivatives as Potential Anticancer Agents
Letters in Drug Design & Discovery The Therapeutical Potential of a Novel Pterocarpanquinone LQB-118 to Target Inhibitor of Apoptosis Proteins in Acute Myeloid Leukemia Cells
Anti-Cancer Agents in Medicinal Chemistry Microgravity Alters Cancer Growth and Progression
Current Cancer Drug Targets STAT5 and STAT5 Inhibitors in Hematological Malignancies
Anti-Cancer Agents in Medicinal Chemistry Differentiation Potential of Human Retinoblastoma Cells
Current Pharmaceutical Biotechnology Metabolic Effects of Resveratrol in Mammals - a Link Between Improved Insulin Action and Aging
Current Aging Science An Overview on 2-arylquinolin-4(1H)-ones and Related Structures as Tubulin Polymerisation Inhibitors
Current Topics in Medicinal Chemistry Driving Neural Stem Cells Towards a Desired Phenotype
Current Stem Cell Research & Therapy