Laboratory of Organic Synthesis, Catalysis and Biochemistry (LOSCB), Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA.
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1848-50. doi: 10.1016/j.bmcl.2010.01.144. Epub 2010 Feb 2.
A series of ethacrynic acid analogues, lacking the alpha,beta-unsaturated carbonyl unit, was synthesized and subsequently evaluated for their ability to inhibit the migration of human breast cancer cells, MCF-7/AZ. Several of the analogues were already active in the low micromolar range, whereas ethacrynic acid itself shows no potential to inhibit the migration of these cancer cells. Preliminary studies show that the presence of one or more methoxy groups at the phenyl ring of ethacrynic acid is important in order for the ethacrynic acid analogues to demonstrate an inhibitory effect on the migration.
一系列缺乏α，β-不饱和羰基单元的依他尼酸类似物被合成，并随后评估其抑制人乳腺癌细胞 MCF-7/AZ 迁移的能力。几种类似物已经在低微摩尔范围内具有活性，而依他尼酸本身没有抑制这些癌细胞迁移的潜力。初步研究表明，依他尼酸苯环上存在一个或多个甲氧基对于依他尼酸类似物表现出对迁移的抑制作用是重要的。
