Faculty of Chemical Engineering and Technology, Department of Organic Chemistry, University of Zagreb, Marulićev trg 20, P.O. Box 177, HR-10000 Zagreb, Croatia.
Eur J Med Chem. 2013 Jan;59:111-9. doi: 10.1016/j.ejmech.2012.11.009. Epub 2012 Nov 16.
In this manuscript the synthesis and biological activity of novel heterocyclic derivatives of benzofuran-2-carboxamides 3a-j and 6a-f is presented. Biological evaluation in vitro revealed that only few compounds exerted concentration-depended antiproliferative effects on tumour cell lines at micromolar concentrations. In particular, 2-imidazolynyl substituted compound 6f showed selectivity on SK-BR-3 cell line while 2-N-acetamidopyridyl substituted 3h and 2-imidazolynyl substituted amide 3i showed selective concentration-dependent antiproliferative effects on SW620 cell line. Compounds 3h and 6f induced apoptosis while compound 3i acted through a cell death mechanism other than apoptosis.
本文介绍了苯并呋喃-2-甲酰胺 3a-j 和 6a-f 的新型杂环衍生物的合成和生物活性。体外生物评价表明，只有少数化合物在微摩尔浓度下对肿瘤细胞系表现出浓度依赖性的抗增殖作用。特别是，2-咪唑啉基取代化合物 6f 对 SK-BR-3 细胞系具有选择性，而 2-N-乙酰氨基吡啶基取代的 3h 和 2-咪唑啉基取代的酰胺 3i 对 SW620 细胞系表现出选择性浓度依赖性的抗增殖作用。化合物 3h 和 6f 诱导细胞凋亡，而化合物 3i 通过不同于凋亡的细胞死亡机制起作用。
