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Molecules 2012, 17(7), 8091-8104; doi:10.3390/molecules17078091

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

1,†, 2,†, 2, 2, 2, 2 and 1,2,*
1 Pharmacy College of West China of Sichuan University, Chengdu, Sichuan 610065, China 2 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China These authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 10 May 2012 / Revised: 11 June 2012 / Accepted: 20 June 2012 / Published: 5 July 2012
(This article belongs to the Section Medicinal Chemistry)
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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 (IC50 = 47.0 vs. 52.6 μM) and showed significant blocking effects on the proliferation of C26, Hela, K562, A549, and HepG2 (IC50 = 15.0, 25.0, 21.2, 29.5, and 13.0 μM, respectively), superior to those of honokiol (IC50 = 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.
Keywords: biphenol; endothelial cell; anti-proliferative; migration; tube formation biphenol; endothelial cell; anti-proliferative; migration; tube formation
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Ran, Y.; Ma, L.; Wang, X.; Chen, J.; Wang, G.; Peng, A.; Chen, L. Design, Synthesis, and Anti-Proliferative Evaluation of [1,1′-biphenyl]-4-ols as Inhibitor of HUVEC Migration and Tube Formation. Molecules 2012, 17, 8091-8104.

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