کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1394389 | 1501157 | 2013 | 9 صفحه PDF | دانلود رایگان |
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.
Biological evaluation of benzofuran-2-carboxamides revealed several selective compounds bearing strong concentration-depended effects on tumour cells (micromolar range). The most active compounds induced apoptosis through activation of caspases or mitotic catastrophe.Figure optionsDownload as PowerPoint slideHighlights
► Heteroaromatic benzo[b]furan carboxamides as potential antiproliferative compounds.
► Several selective compounds with concentration-depended effects on tumour cells.
► Selectivity towards SK-BR-3, MiaPaCa-2 and SW620 cells in the micromolar range.
► Induced apoptosis through activation of caspases or a mitotic catastrophe.
Journal: European Journal of Medicinal Chemistry - Volume 59, January 2013, Pages 111–119