Coumarins are an important class of phytochemicals, a chemical defense presumed to be secreted by plants. More recently, Coumarins have gathered popularity for their basis in anti-cancer agents. This paper dives into the organic synthesis of two 3-substituted coumarins from o-vanillin using the Knoevenagel condensation reaction. The 3-substituted coumarin were characterized using melting point analysis, 1H-NMR, and UV-Vis spectroscopy. In addition, the anticancer activity of synthesized 3-substituted coumarin compounds were assayed against topoisomeraseIIα, which is the target enzyme of FDA approved anti-cancer drug etoposide since it is an active enzyme in cancer cell replication. The demonstrated procedures can be used as an undergraduate senior project that traverses through several classes that chemistry majors take.


We would like to acknowledge the Department of Chemistry, Physics, & Astronomy at Georgia College & State University for their funding and access to the laboratories. We would also like to thank Jiang lab, Tennessee Tech University for providing the facilities to purify the topoisomeraseIIα enzyme.