Synthetically modified methoxsalen for enhanced cytotoxicity in light and dark reactions

  • Bioorg Med Chem Lett. 2019 Feb 15;29(4):619-622. doi: 10.1016/j.bmcl.2018.12.048.
Christophe D Guillon  1 ,  Yi-Hua Jan  2 ,  Natalie Foster  3 ,  Joel Ressner  3 ,  Diane E Heck  4 ,  Jeffrey D Laskin  2 ,  Ned D Heindel  3
Affiliations
  • 1. Department of Chemistry, Lehigh University, Bethlehem, PA 18015 USA. Electronic address: [email protected].
  • 2. Department of Environmental and Occupational Health, Rutgers University School of Public Health, Piscataway, NJ 08854, USA.
  • 3. Department of Chemistry, Lehigh University, Bethlehem, PA 18015 USA.
  • 4. Department of Environmental Health Science, New York Medical College, Valhalla, NY 10595, USA.
PMID: 30638875 DOI: 10.1016/j.bmcl.2018.12.048
Abstract

Linear furocoumarins, also known as psoralens, are clinically useful photo-activated pharmaceuticals employed to address hyperproliferative skin diseases. Seven diverse cytotoxic pharmacophores have been synthetically attached to 8-methoxypsoralen via a 5-amino functionality. The resulting unique set of compounds was evaluated for dark and light toxicity against PAM212 keratinocytes in culture.

Keywords
8-MOP; 8-Methoxypsoralen; Dark-reaction toxicity; Keratinocytes; PAM212; Phototoxicity.