Abstract
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.
- Received January 26, 2022.
- Revision received February 15, 2022.
- Accepted February 16, 2022.
- Copyright © 2022 International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.
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