Abstract
This dissertation is focused on the design and synthesis of the indole system compounds as anticancer drugs, and a study on their structure-activity relationship (SAR) outlined as follows. For the anticancer drug design we intend to make antimitotic agents to disrupt the cancer cell’s cell cycle. In our study, there are two stages. At the initial stage, we use microtubules as the anticancer target to design the drug. Then, we change the target to the Aurora kinase A. In this series indole compound that we prepared, we found that the compound which has the 3-methyl pyrazole as the heterocyclic part can be the Aurora kinase A inhibitor, and the highest case can inhibit around 77% Aurora kinase A. The compound 9c has the anticancer bioactivity of 2.6 μM (IC50) against the HCT116 (human colon cancer - 116 cell line). Furthermore we use this compound as the lead compound to make the SAR (structure -activity relationship) for further study and optimization.