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.
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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 |
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