The synthesis and biological evaluation of cyclohexenone derived natural product

Abstract

Many cyclohexenone natural products, such as 2-crotonyloxymethyl-(4R,5R,6R)- 4,5,6-trihydroxycyclohex-2-enone (COTC), exhibit anti-cancer properties. Due to their cytotoxicity towards a number of cancer cell lines, a large number of studies have been carried out to understand their mechanisms of action as well as to enhance their anti-cancer activities. The aim of this project was concerned with the optimisation of the antiproliferative activity of COTC and the synthetic drug WP1066, where we sought to link derivatives of COTC and the synthetic drug WP1066 together with a PEG-based linker. The cytotoxicity of a number of synthesised compounds was tested against cancer cell lines MDA-MB231 and A549. In addition, to help better understand the mechanism of action of these compounds computational studies were carried out.