Synthesis and evaluation of novel curcumin conjugates and hybrids as potential anticancer agents

Abstract

Cancer is the deadliest disease characterised by uncontrolled division of abnormal cells According to WHO cancer is the second leading cause of deaths worldwide There are many types of cancers affecting different parts of the body Treatment methods for cancer include surgery radiation therapy chemotherapy immunotherapy hormone therapy targeted drug therapy etc Targeted drug therapy is advantageous as it specifically attacks cancer cells by targeting specific genes or proteins or by inhibiting enzymes In targeted drug therapy natural products offer advantages over synthetic molecules due to their biocompatibility chemical diversity and biochemical specificity Vincristine vinblastine taxol and several other natural products are being used for the treatment of cancer Though natural products offer several advantages they have some limitations like requirement of several separation cycles safety concerns toxicity etc But Curcumin is an exceptional natural product and it is extremely safe even at high doses Though curcumin is safe and has contra distinct biological activities its application becomes limited due to poor solubility and bioavailability Hence this study aims at synthesis of novel curcumin conjugates and hybrids with improved properties and enhanced activity All the compounds were synthesised using optimised and improvised reaction conditions thoroughly characterised and screened on a panel of representative cell lines for determining in vitro cytotoxicity using MTT assay The most potent compound was subjected to cell biology experiments to assess the mode of cell death. In silico molecular docking studies, determination of drug likeness and ADMET properties were determined and results correlated with experimental results newline