Abstract |
Coumarins are naturally-occurring compounds that have attracted considerable interest due to their numerous biological activities depending on their pattern of substitution on the coumarin molecule. In this present investigation, we synthesized 3-(4-nitrophenyl)coumarin derivatives (9a-e) and evaluated their in vitro cytotoxic effect on human lung (A549), breast (MDA-MB-231) and prostate (PC3) cancer cell lines for 48 h using crystal violet dye binding assay. Cytotoxic effects of the most active compound on normal human lung (MRC-9) and breast (MCF-10A) cell lines, cell cycle analysis using flow cytometry and mitochondrial membrane potential ( MMP) using Tetramethyl Rhodamine Methyl Ester (TMRM; rhodamine-123) fluorescent dye were also examined. Among the compounds that were evaluated, 9c showed cytotoxic effect (active), caused significant cells arrest (p<0.05) in G0/G1 and S phases of cell cycle and loss of MMP in A459, MDA-MB-231 and PC3 cell lines. Additionally, the cytotoxic effect of 9c was compared to reference drugs ( Coumarin and Docetaxel) for comparative study. These results further demonstrate that acetoxy group at C-7 and C-8 positions of 9c are responsible for the observed cytotoxic effect in these cancer cell lines.
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Authors | Musiliyu A Musa, Lekan M Latinwo, Clifford Virgile, Veera L D Badisa, Akintunde J Gbadebo |
Journal | Bioorganic chemistry
(Bioorg Chem)
Vol. 58
Pg. 96-103
(Feb 2015)
ISSN: 1090-2120 [Electronic] United States |
PMID | 25553414
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 2014 Elsevier Inc. All rights reserved. |
Chemical References |
- 7,8-diacetoxy-3-(4-nitrophenyl)coumarin
- Antineoplastic Agents
- Coumarins
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Topics |
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology)
- Carbon-13 Magnetic Resonance Spectroscopy
- Cell Cycle
(drug effects)
- Cell Line, Tumor
- Coumarins
(chemical synthesis, chemistry, pharmacology)
- Drug Screening Assays, Antitumor
- Humans
- In Vitro Techniques
- Proton Magnetic Resonance Spectroscopy
- Spectrometry, Mass, Electrospray Ionization
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