The indole scaffold represents a privileged pharmacophore in drug discovery that is associated with a wide range of biological activities. Building upon our recent advancements in developing a regioselective synthetic methodology toward functionalized indole derivatives, we have successfully identified candidates with potential anti-inflammatory properties, through screening their ability to inhibit cyclooxygenase (COX) enzymes <i>in vitro</i>. Furthermore, a cytotoxicity assay against 8 different cell lines revealed a candidate with selective cytotoxicity against a HepG2 liver cancer cell line. Herein, we will discuss our efforts towards the design, synthesis and evaluation of 6-hydroxyindole-7-carboxylate derivatives as potential anti-inflammatory and anti-cancer compounds. Our discussion will also include an investigation on cell death mechanism and cell cycle arrest of selected compounds.

Design and synthesis of 6-hydroxyindole-7-carboxylates with anti-inflammatory and anti-cancer activities

ACS Fall 2021

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