Design, Synthesis, and Anti-Proliferative Evaluation of [1,1′-biphenyl]-4-ols as Inhibitor of HUVEC Migration and Tube Formation

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ID: 263107
2012
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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 (<strong>5c</strong>) exerted an inhibitory effect on HUVECs compared to honokiol (IC<sub>50</sub> = 47.0 <em>vs.</em> 52.6 μM) and showed significant blocking effects on the proliferation of C26, Hela, K562, A549, and HepG2 (IC<sub>50</sub> = 15.0, 25.0, 21.2, 29.5, and 13.0 μM, respectively), superior to those of honokiol (IC<sub>50</sub> = 65.1, 62.0, 42.0, 75.0, and 55.4 μM, respectively). Importantly, compound <strong>5c</strong> inhibited the migration and capillary-like tube formation of HUVECs <em>in vitro</em>.
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Year 2012
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