Synthetic Mono/di-halogenated Coumarin Derivatives and Their Anticancer Properties

Author(s): Kabange Kasumbwe, Katharigatta N. Venugopala, Viresh Mohanlall, Bharti Odhav

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 17 , Issue 2 , 2017

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Graphical 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.

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Article Details

Year: 2017
Published on: 11 January, 2017
Page: [276 - 285]
Pages: 10
DOI: 10.2174/1871520616666160926112508
Price: $65

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