IN VITRO AND IN VIVO ANTI-CANCER EFFECTS OF 2-ETHYL-3-O-SULPHAMOYL-ESTRA-1,3,5(10)15- TETRAENE-3-OL-17-ONE AND 2-ETHYL-3-O-SULPHAMOYL-ESTRA-1,3,5(10)16-TETRAENE

摘要

In the design of anti-cancer therapeutics, it is not merely a matter of demonstrating that the proposed compounds kill cells. Required is information on the mode, mechanism and signalling pathways of the cell death(s) induced, the molecule's anti-proliferative effects, reduction in malignant cell migratory capacity, inhibition of neoplastic cell invasion and anti-angiogenic effects to potentially prevent neovascularisation of tumours. 2-Ethyl-3-O-sulphamoyl-estra-1,3,5(10)15-tetraene-3-ol-17one (C9) and 2-ethyl-3-O-sulphamoyl-estra-1,3,5(10)16-tetraene (C19) are novel, sulphamoylated 2-methoxyestradiol analogues designed and synthesized by our research team with the aim of improving the potency and pharmacokinetic constraints of the parent compound's anti-cancer properties. The aim of this project was to analyse both these compounds on two cells lines (HeLa and MDA-MB231) for their ability to perform as anti-cancer therapeutic agents in the areas mentioned above. Previously, we have reported that C19 induces apoptosis and possibly autophagy in cervical adenoma HeLa cells.