title: Cytotoxic activity of new acetoxycoumarin derivatives in cancer cell lines.
abstract: BACKGROUND
  Coumarin and their derivatives are important and useful compounds with diverse pharmacological properties. In the present study, we evaluated the in vitro cytotoxic activity of new acetoxycoumarin derivatives: 4-(7-methoxy-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (1), 4-(1-methyl-3-oxo-3H-benzo[f]chromen-2-yl)phenyl acetate (2), 4-(6-propionamido-4-methyl-2-oxo-2H-chromen-3-yl) phenyl acetate (3), 4-(7-acetoxy-2-oxo-4-phenyl-2H-chromen-3-yl)phenyl acetate (4), 4-(2-oxo-4-phenyl-2H-chromen-3-yl)phenyl acetate (5), 4-(6-bromo-2-oxo-4-phenyl-2H-chromen-3-yl)phenyl acetate (6), 4-(7-(diethylamino)-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (7), 4-(6,8-dibromo-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (8) against A549 human lung cancer, CRL 1548 rat liver cancer and CRL 1439 normal rat liver cells.
  
  
  METHODS
  The cytotoxic activity was evaluated by crystal violet dye-binding assay. The effect of compounds 5 and 7 on different phases of the cell cycle was determined using flow cytometry.
  
  
  RESULTS
  In the A549 lung cancer cell line, the 50% lethal dose (LD50) values for compounds 1-4, 6 and 8 were found to be >100 μM while those for 5 and 7 were 89.3 and 48.1 μM, respectively after 48 h treatment. In the CRL 1548 liver cancer cell line, only compound 7 showed toxicity, with an LD50 of 45.1 μM. Compounds 5 and 7 caused different cell phase arrest in lung and liver cancer cell lines.
  
  
  CONCLUSIONS
  The results indicate that 4-(7-(diethylamino)-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate (7) had the highest cytotoxic activity in all of the examined cell lines.
authors: Department of Chemistry, College of Arts and Sciences, Florida A&M University, 219 Jones Hall, Tallahassee, FL 32307, USA. musiliyu.musa@famu.edu
authors: Musiliyu A
authors: MA
authors: Musa
authors: Veera L D
authors: VL
authors: Badisa
authors: Lekan M
authors: LM
authors: Latinwo
authors: John
authors: J
authors: Cooperwood
authors: Andre
authors: A
authors: Sinclair
authors: Ahkinyala
authors: A
authors: Abdullah
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D002460:Cell Line; D045744:Cell Line, Tumor; D003374:Coumarins / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008099:Liver / Q000166:cytology / Q000187:drug effects; D008113:Liver Neoplasms / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D051381:Rats
chemical_list: D000970:Antineoplastic Agents; D003374:Coumarins