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. 2019 Feb 15;29(4):619-622.
doi: 10.1016/j.bmcl.2018.12.048. Epub 2018 Dec 22.

Synthetically modified methoxsalen for enhanced cytotoxicity in light and dark reactions

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

Synthetically modified methoxsalen for enhanced cytotoxicity in light and dark reactions

Christophe D Guillon et al. Bioorg Med Chem Lett. .

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.

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Figures

Figure 1.
Figure 1.
Core furocoumarin structure and the most common numbering system:
Scheme 1.
Scheme 1.
Syntheses of Compounds (3) to (9):
See this image and copyright information in PMC

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