巴比酮类似物的合成、结构-活性关系及作为抗增殖和抗血管生成剂的生物评价。
Synthesis, structure-activity relationships and biological evaluation of barbigerone analogues as anti-proliferative and anti-angiogenesis agents.
机构信息
State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China; College of Chemistry and Chemical Engineering, Jishou University, Jishou 416000, China.
State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China.
出版信息
Bioorg Med Chem Lett. 2014 Jul 15;24(14):3158-63. doi: 10.1016/j.bmcl.2014.04.121. Epub 2014 May 16.
A series of barbigerone analogues (7a-7w, 13a-13x) were designed, synthesized and biologically evaluated for their anti-proliferative and anti-angiogenic activities. Among these compounds, compound 13a exhibited the most potent inhibitory effect on the proliferation of HUVECs, HepG2, A375, U251, B16, and HCT116 cells (IC50=3.80, 0.28, 1.58, 3.50, 1.09 and 0.68 μM, respectively). Compound 13a inhibited the angiogenesis in zebrafish embryo assay in a concentration-dependent manner. Furthermore, 13a also effectively inhibited the migration and capillary like tube formation of human umbilical vein endothelial cell in vitro. These results support the further investigation of this class of compounds as potential anti-proliferative and anti-angiogenesis agents.
设计、合成了一系列巴尔比酮类似物（7a-7w，13a-13x），并对其抗增殖和抗血管生成活性进行了生物评价。在这些化合物中，化合物 13a 对 HUVECs、HepG2、A375、U251、B16 和 HCT116 细胞的增殖表现出最强的抑制作用（IC50=3.80、0.28、1.58、3.50、1.09 和 0.68 μM）。化合物 13a 以浓度依赖的方式抑制斑马鱼胚胎中的血管生成。此外，13a 还能有效抑制人脐静脉内皮细胞的体外迁移和毛细血管样管形成。这些结果支持进一步研究这类化合物作为潜在的抗增殖和抗血管生成剂。
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