Abstract:
2-Methoxyestradiol is a 17-beta estradiol derivative with antitumor activity. Due to low
bioavailability, a new estrogen analogue was in silico-designed. The latter, a sulphamoylated
analogue of 2-methoxyestradiol, was evaluated for its potential antiproliferative effect by
means of expression microarray analysis and transmission electron microscopy in the highly
metastatic breast adenocarcinoma (MDA-MB-231) cell line. Data indicate changes in gene
expression pertaining to induction of apoptosis and autophagy as types of cell death, arrest of
the cell cycle, and impairment of the cytoskeleton and induction of reactive oxygen species.
Transmission electron microscopy confirmed morphological characteristics of apoptosis and
autophagy. Altered cell cycle- and cytoskeletal-related gene expression profiles demonstrated
that the estradiol analogue acts as an antimitotic agent in this highly metastatic breast cell
line. Data also showed that the newly designed estrogen analogue exerts an antiproliferative
effect in this cancer cell line culminating in both apoptosis and autophagy as type of cell
death paving the way for further investigations into its potential as anticancer agent.
