Journal
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 17, Issue 2, Pages 276-285Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520616666160926112508
Keywords
Synthetic coumarins; MTT assay; anticancer; apoptosis
Categories
Funding
- National Research Foundation, South Africa
- Durban University of Technology
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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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