Medium benzene-fused oxacycles with the 5-fluorouracil moiety: synthesis, antiproliferative activities and apoptosis induction in breast cancer cells

Benzo-Fused Seven- and Six-Membered Derivatives Linked to Pyrimidines or Purines Induce Apoptosis of Human Metastatic Breast Cancer MCF-7 Cells In Vitro

“…In this way we have reported the synthesis and anticancer activities of compounds 3 (Campos et al, 1997), 4-6 (Saniger et al, 2003a), 7 , 8-9 (Saniger et al, 2003a) and trans-10 (Saniger et al, 2003b) (Figure 1). In all cases, the linkage between the 5-FU moiety and the seven-membered ring was carried out through its N-1 atom.…”

“…c Determined by flow cytometry: see ref. (Saniger et al, 2003a). d Apoptosis was determined using an annexin V-based assay (Chadderton et al, 2000).…”

Apoptosis as a Therapeutic Target in Cancer and Cancer Stem Cells: Novel Strategies and Futures Perspectives

“…We have reported the synthesis and anticancer activities of compounds 1-5 [16] and trans-6 [17] (Figure 1). In all cases, the linkage between the 5-FU moiety and the seven-membered ring was carried out through its N-1 atom.…”

“…[117]. b Determined by flow cytometry: see [16]. c Apoptosis was determined using an annexin V-based assay [113].…”

“…Moreover, these strategies overcome the adverse effects associated with cytotoxic drugs and increase their anti-cancer activity. Novel antitumour drugs have been synthesised such as 5-FU O,N-acetals and benzo-fused seven-membered O,N-acetal in which the 5-FU moiety was changed for the naturallyoccurring pyrimidine base uracil, which induced cell cycle-mediated apoptosis in breast and colon cancer cells [16,17,18,19]. The mechanism of action of these drugs was mainly centred on positive apoptosis regulatory pathway genes, and the repression of genes involved in carcinogenesis, proliferation and tumour invasion.…”