title: Design, synthesis, and anti-proliferative evaluation of [1,1'-biphenyl]-4-ols as inhibitor of HUVEC migration and tube formation.
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.
authors: Pharmacy College of West China of Sichuan University, Chengdu, Sichuan 610065, China.
authors: Yan
authors: Y
authors: Ran
authors: Liang
authors: L
authors: Ma
authors: Xuewei
authors: X
authors: Wang
authors: Jinying
authors: J
authors: Chen
authors: Guangcheng
authors: G
authors: Wang
authors: Aihua
authors: A
authors: Peng
authors: Lijuan
authors: L
authors: Chen
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002465:Cell Movement / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D006367:HeLa Cells; D056945:Hep G2 Cells; D061307:Human Umbilical Vein Endothelial Cells / Q000166:cytology* / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D018919:Neovascularization, Physiologic / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D020533:Angiogenesis Inhibitors; D001713:Biphenyl Compounds