الفهرس | Only 14 pages are availabe for public view |
Abstract A new series of bis(furan-based chalcone) derivatives linked to aliphatic linkers, with the furan units positioned at the A- or B-rings, synthesized and evaluated as anti-cancer agents. Chalcones 5a{u2013}c, in which the furan ring is designed to be a B-ring obtained by the reactions of Knoevenagel condensation of the suitable bis(acetyl) compounds 3a{u2013}c alongside with 2 equivalents of furan-2- aldehyde. Likewise, the condensation of bis(aldehydes) 7a{u2013}c with two equivalents of 2-acetylfuran afforded the corresponding chalcones 9a{u2013}c, in which the furan rings signify the chalcones{u2019} A-rings, in outstanding yields. The synthesized compounds have been characterized fully via 1HNMR, 13C- NMR, and elemental analysis. The in vitro anticancer activity of prepared compounds was tested against the following cell lines A549, HCT116, HepG2, PC3, A431, and BJ1 by MTT assay. Analysis of gene expression of skin and lung cancer-related genes, comet assay, and DNA fragmentation assay were also performed. Compounds 9a and 9c were found to be promising, with an IC50 of (24.9 and 13.7 og mlA new series of bis(furan-based chalcone) derivatives linked to aliphatic linkers, with the furan units positioned at the A- or B-rings, synthesized and evaluated as anti-cancer agents. Chalcones 5a{u2013}c, in which the furan ring is designed to be a B-ring obtained by the reactions of Knoevenagel condensation of the suitable bis(acetyl) compounds 3a{u2013}c alongside with 2 equivalents of furan-2- aldehyde. Likewise, the condensation of bis(aldehydes) 7a{u2013}c with two equivalents of 2-acetylfuran afforded the corresponding chalcones 9a{u2013}c, in which the furan rings signify the chalcones{u2019} A-rings, in outstanding yields |