Faculty of Science Research Talk : Semi-Synthesis, Biological Evaluation, Structure-Activity Relationship and Docking Studies of Cardamonin Analogues As Novel Anticancer Agents

Name: Mohd Khalid Break – School of Pharmacy

Chairperson: Dr New Siu Yee

Title : Semi-Synthesis, Biological Evaluation, Structure-Activity Relationship and  Docking Studies of Cardamonin Analogues As Novel Anticancer Agents  

Abstract: 

Cancer has been regarded as a leading cause of deaths worldwide with lung cancer being responsible for the majority of cases globally while nasopharyngeal cancer (NPC) mostly affecting populations in Asia. In this study, several novel analogues of the natural product cardamonin were semi-synthesized, characterized and tested against A549 (lung) and HK1 (NPC) cell lines followed by molecular docking studies on the most potent analogues. Results have generally shown that cardamonin and its active analogues exhibited higher activity against HK1 than A549 cells while substituting cardamonin’s hydroxyl groups with non-polar or bulky substituents resulted in loss of activity.  Moreover, modifications to the carbonyl group of cardamonin resulted in a decrease in activity, however, complexation with metal ions has managed to produce highly cytotoxic compounds with IC50 values as low as 0.86µM for the copper complex. These results suggest that some of the semi-synthesized analogues can act as lead compounds for the development of potent anti-cancer agents.