Design, synthesis, and anti-proliferative evaluation of [1,1′-biphenyl]-4-ols as inhibitor of HUVEC migration and tube formation

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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 50 = 47.0 vs. 52.6 μM) and showed significant blocking effects on the proliferation of C26, Hela, K562, A549, and HepG2 (IC 50 = 15.0, 25.0, 21.2, 29.5, and 13.0 μM, respectively), superior to those of honokiol (IC 50 = 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. © 2012 by the authors.

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Ran, Y., Ma, L., Wang, X., Chen, J., Wang, G., Peng, A., & Chen, L. (2012). Design, synthesis, and anti-proliferative evaluation of [1,1′-biphenyl]-4-ols as inhibitor of HUVEC migration and tube formation. Molecules, 17(7), 8091–8104. https://doi.org/10.3390/molecules17078091

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