Abstract

Chalcone derivatives are known for their numerous biological activities which include the interference of microtubule dynamics instability and are good candidates as an antimitotic agent that can be beneficial in the treatment of cancer. In the work described here, two series of chalcone derivatives including two newly synthesised derivatives were assessed for their antiproliferative activity and inhibition and promoting effects of tubulin polymerization. Antiproliferative activity was evaluated using the Microculture Tetrazolium (MTT) Assay while disruption of the mictotubule dynamics instability was investigated by the Tubulin Polymerization Assay. Both assays were carried out using human colon adenocarcinoma grade II (HT-29) cells. Compounds in series 5 showed strong inhibitory activity on the growth of HT-29 cells with IC₅₀ ranging from 19.26 to 36.95 µM. Two of the chalcone derivatives, compound 5a and 5c were found to be active as an inhibitor and a promoter towards the microtubule dynamics respectively. Compounds with a dimethoxy benzene group on Ring B showed inhibitory effect of the HT-29 cells growth while furan on Ring A showed inhibitory effect on tubulin polymerization. These compounds are worthy to be investigated further as potential antimitotic agents.

Keywords: Chalcone, antiproliferative, inhibitor, promoter, tubulin, polymerization.

Graphical Abstract