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Synthesis and cytotoxic evaluation of usnic acid benzylidene derivatives as potential anticancer agents. 2021
Van-Kieu Nguyen, and
Jirapast Sichaem, and
Huu-Hung Nguyen, and
Xuan Hieu Nguyen, and
Thi-Thu-Loi Huynh, and
Thi-Phuong Nguyen, and
Nakorn Niamnont, and
Dinh-Hung Mac, and
Duc-Dung Pham, and
Warinthorn Chavasiri, and
Kim-Phi-Phung Nguyen, and
Thuc-Huy Duong
Center of Excellence in Natural Products Chemistry, Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok, Thailand.
A series of usnic acid benzylidene derivatives (groups I-V) were designed, synthesized and evaluated for their anticancer activity in the search for potentially new anticancer agents. Compounds 1a, 5b, 2b, 2e and 2f exhibited the most potent cytotoxcity against K562 cell line with IC50 values of 10.0 ± 3.6, 5.6 ± 0.4, 8.8 ± 1.0, 4.5 ± 0.1 and 8.4 ± 0.4 μM, respectively. It is noteworthy that compound 2e displayed potent cytotoxicity against K562 cells without any cytotoxic effect on HEK293 normal cell line.
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