Anticancer activity of (1,2,3,5-tetrahydro-4,1-benzoxazepine-3-yl)-pyrimidines and -purines against the MCF-7 cell line: Preliminary cDNA microarray studies

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

“…Compounds 48 and 57 were selected to identify the molecular key targets of its anti-cancer activity (Díaz-Gavilán et al, 2008a). Completion of the human genome sequence and the advent of DNA microarrays using cDNAs enhanced the detection and identification of hundreds of differentially expressed genes in response to anticancer drugs.…”

“…One of the more important results in the current study was the ability of 48 to modulate the expression of genes involved in apoptosis or its delay of mitosis. This effect can be explained by the accumulation of cells in the G 2 /M checkpoint of cell cycle, particularly GP132, the receptor for an unknown ligand, which activates a G2 alpha protein (Díaz-Gavilán et al, 2008a). This is transcriptionally upregulated by stress-inducing and cell-damaging agents and that is involved in caspasemediated apoptosis (Lin & Ye, 2003).…”

“…However, 57 induced the down-regulation of a gene involved in the metastatic progression of cancer such as RAC1, a Ras-like protein member of the Rho family of the GTPase key downstream target in Ras signalling (Baugher et al, 2005). The studies by microarray technology showed that the main molecular targets of some of these compounds (48 and 57) are pro-apoptotic genes with protein kinase activity such as GP132, ERN1 or RAC1, which prevent the metastatic progression (Díaz-Gavilán et al, 2008a).…”

NMR studies of new heterocycles tethered to purine moieties with anticancer activity

“…Many active compounds have been developed to face this problem in recent years . Some purine derivatives with an interesting antiproliferative activity have been previously synthesized by combining benzo‐fused heterocycles linked to substituted purines . In order to improve the activity and have a deeper idea of the structure–activity relationship, new compounds have been obtained.…”

Stereoselective Synthesis of (3R)‐3‐Alkyl‐4,1‐Benzoxazepine‐2,5‐Diones

“…The benzoxazepines belong to a group of heterocyclic compounds with significant importance and application in biological and medicinal chemistry . Enantiomeric purity is highly desirable in the pharmaceutical industry, as usually only one isomer of a drug is biologically active, while its isomers may display toxic or other side effects .…”