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Synthesis and in vitro evaluation of 3-(4-nitrophenyl)coumarin derivatives in tumor cell lines.

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.
AuthorsMusiliyu A Musa, Lekan M Latinwo, Clifford Virgile, Veera L D Badisa, Akintunde J Gbadebo
JournalBioorganic chemistry (Bioorg Chem) Vol. 58 Pg. 96-103 (Feb 2015) ISSN: 1090-2120 [Electronic] United States
PMID25553414 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014 Elsevier Inc. All rights reserved.
Chemical References
  • 7,8-diacetoxy-3-(4-nitrophenyl)coumarin
  • Antineoplastic Agents
  • Coumarins
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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