Química Nova (Jan 2011)

Chemical modifications of a natural xanthone and antimicrobial activity against multidrug resistant Staphylococcus aureus and cytotoxicity against human tumor cell lines

  • Ana Camila Micheletti,
  • Neli Kika Honda,
  • Dênis Pires de Lima,
  • Adilson Beatriz,
  • Maria Rita Sant'ana,
  • Nadia Cristina Pereira Carvalho,
  • Maria de Fatima Cepa Matos,
  • Lyara Meira Marinho Queiróz,
  • Danielle Bogo,
  • José Roberto Zorzatto

DOI
https://doi.org/10.1590/S0100-40422011000600019
Journal volume & issue
Vol. 34, no. 6
pp. 1014 – 1020

Abstract

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A series of 15 ω-aminoalkoxylxanthones containing methyl, ethyl, propyl, tert-butylamino and piperidinyl moieties were synthesized from a natural xanthone isolated from a lichen species. These compounds were tested for their in vitro antibacterial properties against Gram-positive and Gram-negative bacteria and cytotoxicity against a number of human tumor cell lines was too evaluated. The newly synthesized derivatives revealed selective activity against Staphylococcus aureus (Gram-positive), and the most promising results are for a multidrug resistant strain, for which six of these compounds showed good activity (MICs 4 µg/mL). Many derivatives inhibited tumor cells growth and most compounds were active on multiple lines.

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