Antitumor activity estradiol analogues – Prof Annie Joubert
Prof Annie Joubert
Title of the project
Investigation into the antitumor activity of novel in silico-designed estradiol analogues.
A major challenge in cancer research is to find agents that target cancer cells while leaving normal cells unharmed. Computational methods for the discovery of targets and identifying lead compounds against these targets are playing a key role in the discovery and development of new pharmaceutically relevant drugs. Hitherto, this research focus entailed the in silico-design and synthesis of newly-designed anticancer compounds. In silico design and chemical synthesis has been conducted successfully and subsequent detailed elucidation of each compound’s biochemical pathway of signalling was investigated to verify potential anticancer activity in cancer cell lines to complement the improvement of analogues with therapeutic potential. These methods make it possible to preselect potential anticancer compounds (computer modeling) for subsequent synthesis by a pharmaceutical company.
This research project was centered on improving treatments to enable the anticancer drug to affect only the cancer cell and at low dosages with less frequent treatment intervals. The research focused on cancer types of national and international relevance and data generated contributed to the search for potential anticancer agents that target cancer cells while leaving non-tumorigenic cells unharmed. The research also led to job creation and the prospects for students to further their postgraduate careers. Postgraduate students received opportunities to scientifically communicate their findings internationally and nationally via conference contributions and research visits. This contributed towards building the economy and implementing ‘scarce skills’ training in the working environment.
- 17-Beta-Estradiol Analog Inhibits Cell Proliferation by Induction of Apoptosis in Breast Cell Lines
- 2_Methoxyestradiol-bis-sulphamate A promising anticancer agent in an esophageal carcinoma (SNO) cell line
- Effects of a 17-beta estradiol analogue on gene expression and morphology
- In vitro changes in mitochondrial potential aggresome formation and caspase activity by a novel 17-b-estradiol analogue in breast adenocarcinoma cells
- Molecular crosstalk between apoptosis and autophagy
- Novel Estradiol Analogue Induces Apoptosis and Autophagy in Esophageal Carcinoma cells
- Signaling Pathways of ESE-16
- Sulphamoylated 2-Methoxyestradiol Analogues Induce Apoptosis in Adenocarcinoma Cell Lines