Abstract
Background: Coumarins are naturally occurring plant metabolites and several synthetic coumarin analogues are known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties.
Objective; Keeping this promising pharmacological properties in mind, in the present investigation, mono/dihalogenated coumarin analogues CMRN1-CMRN7 have been synthesized and evaluated for their anticancer activity.
Method: The cytotoxicity potential of the test compounds was evaluated against UACC-62, MCF-7 and PBM (Peripheral Blood Mononuclear) cell lines using MTT assay. The apoptotic potential of the coumarin compounds was evaluated against UACC-62 cell by assessing membrane change, mitochondria membrane potential, pro-apoptotic changes were investigated using the AnnexinV-PI staining, JC-1, caspase-3 enzyme kits respectively on flow cytometer.
Results: The test compounds CMRN1, CMRN2, CMRN4 and CMRN5 have strongly suppressed the cell proliferation of UACC-62 and MCF-7 cancer cell lines. Furthermore the test compounds CMRN1, CMRN2, CMRN4 and CMRN5 exerted antiproliferative effects through apoptosis induction against UACC-62.
Conclusion: Compounds CMRN1, CMRN2, CMRN4 and CMRN5 can be considered as lead compounds to arrive at a promising anticancer agents.
Keywords: Synthetic coumarins, MTT assay, anticancer, apoptosis.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthetic Mono/di-halogenated Coumarin Derivatives and Their Anticancer Properties
Volume: 17 Issue: 2
Author(s): Kabange Kasumbwe, Katharigatta N. Venugopala, Viresh Mohanlall and Bharti Odhav
Affiliation:
Keywords: Synthetic coumarins, MTT assay, anticancer, apoptosis.
Abstract: Background: Coumarins are naturally occurring plant metabolites and several synthetic coumarin analogues are known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties.
Objective; Keeping this promising pharmacological properties in mind, in the present investigation, mono/dihalogenated coumarin analogues CMRN1-CMRN7 have been synthesized and evaluated for their anticancer activity.
Method: The cytotoxicity potential of the test compounds was evaluated against UACC-62, MCF-7 and PBM (Peripheral Blood Mononuclear) cell lines using MTT assay. The apoptotic potential of the coumarin compounds was evaluated against UACC-62 cell by assessing membrane change, mitochondria membrane potential, pro-apoptotic changes were investigated using the AnnexinV-PI staining, JC-1, caspase-3 enzyme kits respectively on flow cytometer.
Results: The test compounds CMRN1, CMRN2, CMRN4 and CMRN5 have strongly suppressed the cell proliferation of UACC-62 and MCF-7 cancer cell lines. Furthermore the test compounds CMRN1, CMRN2, CMRN4 and CMRN5 exerted antiproliferative effects through apoptosis induction against UACC-62.
Conclusion: Compounds CMRN1, CMRN2, CMRN4 and CMRN5 can be considered as lead compounds to arrive at a promising anticancer agents.
Export Options
About this article
Cite this article as:
Kasumbwe Kabange, Venugopala N. Katharigatta, Mohanlall Viresh and Odhav Bharti, Synthetic Mono/di-halogenated Coumarin Derivatives and Their Anticancer Properties, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (2) . https://dx.doi.org/10.2174/1871520616666160926112508
DOI https://dx.doi.org/10.2174/1871520616666160926112508 |
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
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
-
Meet Our Editorial Board Member:
Central Nervous System Agents in Medicinal Chemistry Cholesterol-Rich Nanoemulsions (LDE) for Drug Targeting of Cholesteryl-Succinyl- 5-Fluorouracil Conjugate
Current Nanoscience DNA Microarray-Based Gene Expression Profiling in Cancer: Aiding Cancer Diagnosis, Assessing Prognosis and Predicting Response to Therapy
Current Pharmacogenomics Paullones as Inhibitors of Protein Kinases
Current Topics in Medicinal Chemistry Mammogram Classification Based on Morphological Component Analysis (MCA) and Curvelet Decomposition
Neuroscience and Biomedical Engineering (Discontinued) The Toll-Like Receptor Radical Cycle Pathway: A New Drug Target in Immune-Related Chronic Fatigue
CNS & Neurological Disorders - Drug Targets Simultaneous Analysis of Vanillin and Coumarin in Mangrove Plants and Commercial Food Products Using UPLC-ESI-MS/MS
Current Analytical Chemistry ADAM17 as a Therapeutic Target in Multiple Diseases
Current Pharmaceutical Design Human Complex Trait Genetics: Lifting the Lid of the Genomics Toolbox - from Pathways to Prediction
Current Genomics Crocetin as an Active Secondary Metabolite of Saffron Stigma and Anticancer Effects
Current Cancer Therapy Reviews The Synergistic Effects of DNA-Targeted Chemotherapeutics and Histone Deacetylase Inhibitors As Therapeutic Strategies for Cancer Treatment
Current Medicinal Chemistry Substrates and Inhibitors of Human Multidrug Resistance Associated Proteins and the Implications in Drug Development
Current Medicinal Chemistry The Pro-Survival Function of Akt Kinase can be Overridden or Altered to Contribute to Induction of Apoptosis
Current Cancer Drug Targets Clinical Development of Experimental Virus-Mediated Gene Therapy for Malignant Glioma
Anti-Cancer Agents in Medicinal Chemistry Radiotracers in Oncology
Current Radiopharmaceuticals PAF Receptor and Tumor Growth
Current Drug Targets Pidotimod and Immunological Activation in Individuals Infected with HIV
Current HIV Research New Platinum and Ruthenium Complexes - the Latest Class of Potential Chemotherapeutic Drugs - a Review of Recent Developments in the Field
Mini-Reviews in Medicinal Chemistry PET Radioligands for In Vivo Visualization of Neuroinflammation
Current Pharmaceutical Design Inhibitors for Metastasis Development
Recent Patents on Anti-Cancer Drug Discovery