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Synthesis and cytotoxic evaluation of usnic acid benzylidene derivatives as potential anticancer agents

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journal contribution
posted on 2019-07-13, 07:21 authored by Van-Kieu Nguyen, Jirapast Sichaem, Huu-Hung Nguyen, Xuan Hieu Nguyen, Thi-Thu-Loi Huynh, Thi-Phuong Nguyen, Nakorn Niamnont, Dinh-Hung Mac, Duc-Dung Pham, Warinthorn Chavasiri, Kim-Phi-Phung Nguyen, Thuc-Huy Duong

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.

Funding

The study was supported by Science and Technology Incubator Youth Program, managed by the Center for Science and Technology Development, Ho Chi Minh Communist Youth Union, the contract number is “03/2018 / HĐ-KHCN-VƯ”.

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