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Updated: Sep 28, 2025
Single Molecule Analysis of Laser Localized Psoralen Adducts
Published on: April 20, 2017
Relationship Between the Structure of Alkylpsoralens and Their Antiproliferative Activity in HL60 Cells
Satoru Kawaii1, Y U Matsuoka2, Hideki Noguchi2
1Laboratory of Bio-organic Chemistry, Tokyo Denki University, Hatoyama, Japan; kawaii@mail.dendai.ac.jp.
Background/Aim:
As part of our continuing investigation in coumarin derivatives as potential anticancer substances, a series of alkylpsoralens were synthesized, and their antiproliferative activity was evaluated in leukemic HL60 cells.
Materials And Methods:
Alkylpsoralens were systematically synthesized from the combination of several chloroketones and 7-hydroxycoumarin derivatives.
Results:
Among the compounds synthesized, 4,4',8-trimethylpsoralen demonstrated the most potent activity (IC50=6.6 μM).
Conclusion:
The correlation between the alkylation pattern and antiproliferative activity showed the importance of the C4-methyl and C8-methyl moieties in the psoralen nucleus as well as the importance of lipophilicity for their antiproliferative activity.
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