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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
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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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 (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 3.0).

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MDPI and ACS Style

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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