title: Synthesis and anticancer activity of 7-hydroxycoumarinyl gallates.
abstract: BACKGROUND
  The search for anti-cancer agents includes naturally occurring substances and theirs modifications. Therefore we invented and designed compounds that represent fused derivatives of gallic acid with coumarins.
  
  
  METHODS
  As a result, a series of 8 novel esters of gallic acid and 7-hydroxycoumarins were synthesized and evaluated for anticancer activity. The structures of the compounds were established by IR, (1)H, (13)C NMR and HR MS spectra. The esters were assayed for antiproliferative activity against human leukemia HL-60 and prostate cancer DU145 cell lines. The activity of novel esters was evaluated by cell viability assays as well as by analysis of cell cycle and cell death mechanism.
  
  
  RESULTS
  The esters were found to be of similar or higher activity than gallic acid. No pronounced harmful effect was observed in non-cancer cells.
  
  
  CONCLUSIONS
  The novel compounds represent an excellent starting point for the further optimization and the design of therapeutically effective anti-cancerous drugs.
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Warszawa, Poland. Electronic address: ehejchman@wum.edu.pl.
authors.forename: Elżbieta
authors.initials: E
authors.lastname: Hejchman
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Warszawa, Poland; Department of Drug Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Warszawa, Poland.
authors.forename: Przemysław
authors.initials: P
authors.lastname: Taciak
authors.affiliation: Department of Histology and Embryology, Center for Biostructure Research, Medical University of Warsaw, Warszawa, Poland.
authors.forename: Sebastian
authors.initials: S
authors.lastname: Kowalski
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Warszawa, Poland.
authors.forename: Dorota
authors.initials: D
authors.lastname: Maciejewska
authors.affiliation: Department of Histology and Embryology, Center for Biostructure Research, Medical University of Warsaw, Warszawa, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Czajkowska
authors.affiliation: Department of Histology and Embryology, Center for Biostructure Research, Medical University of Warsaw, Warszawa, Poland.
authors.forename: Julia
authors.initials: J
authors.lastname: Borowska
authors.affiliation: Department of Transplantology and Central Tissue Bank, Center for Biostructure Research, Medical University of Warsaw, Warszawa, Poland. Electronic address: izamlynar@esculap.pl.
authors.forename: Dariusz
authors.initials: D
authors.lastname: Śladowski
authors.affiliation: Department of Histology and Embryology, Center for Biostructure Research, Medical University of Warsaw, Warszawa, Poland.
authors.forename: Izabela
authors.initials: I
authors.lastname: Młynarczuk-Biały
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005707:Gallic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology; D006801:Humans; D013329:Structure-Activity Relationship; D014468:Umbelliferones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D014468:Umbelliferones; D005707:Gallic Acid
keywords: Anticancer activity; Apoptosis; Cell cycle; Coumarin derivatives; Gallates