Design and Synthesis of Coumarin Derivatives as Novel PI3K Inhibitors

Background: Coumarins possess a broad spectrum of biological activities and are important pharmacophores in drug developments. Since aberrant upregulation of PI3K/Akt signaling is related to uncontrolled tumor cell proliferation, enhanced migration, and adhesion-independent tumor growth, it is of interests to find novel coumarin derivatives as anticancer agents targeting the PI3K/Akt signaling pathway. Keywords: Anticancer agents, apoptosis, coumarins, Friedel-Crafts alkylation, inhibitors, Pechman reaction, PI3K, PI3K/Akt signal pathway.