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

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,* email
Received: 10 May 2012; in revised form: 11 June 2012 / Accepted: 20 June 2012 / Published: 5 July 2012
(This article belongs to the Section Medicinal Chemistry)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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
PDF Full-text Download PDF Full-Text [634 KB, uploaded 18 June 2014 19:50 CEST]

Export to BibTeX |
EndNote


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.

AMA 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(7):8091-8104.

Chicago/Turabian Style

Ran, Yan; Ma, Liang; Wang, Xuewei; Chen, Jinying; Wang, Guangcheng; Peng, Aihua; Chen, Lijuan. 2012. "Design, Synthesis, and Anti-Proliferative Evaluation of [1,1′-biphenyl]-4-ols as Inhibitor of HUVEC Migration and Tube Formation." Molecules 17, no. 7: 8091-8104.


Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert