Design, synthesis, and anti-proliferative evaluation of [1,1'-biphenyl]-4-ols as inhibitor of HUVEC migration and tube formation |
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Authors: | Yan Ran Liang Ma Xuewei Wang Jinying Chen Guangcheng Wang Aihua Peng Lijuan Chen |
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Institution: | Pharmacy College of West China of Sichuan University, Chengdu, Sichuan 610065, China. |
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Abstract: | Allylated biphenol neolignans contain a variety of chemopreventive entities that have been used as anti-tumor drug leads. Herein, 37 allylated biphenols were evaluated for anti-proliferative activity by the MTT assay and inhibitory effect on the migration and tube formation of HUVECs featuring anti-angiogenic properties. 3-(2-Methylbut-3-en-2-yl)-3′,5′-bis(trifluoromethyl)-1,1′-biphenyl]-4-ol (5c) exerted an inhibitory effect on HUVECs compared to honokiol (IC?? = 47.0 vs. 52.6 μM) and showed significant blocking effects on the proliferation of C26, Hela, K562, A549, and HepG2 (IC?? = 15.0, 25.0, 21.2, 29.5, and 13.0 μM, respectively), superior to those of honokiol (IC?? = 65.1, 62.0, 42.0, 75.0, and 55.4 μM, respectively). Importantly, compound 5c inhibited the migration and capillary-like tube formation of HUVECs in vitro. |
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