Cu-Catalyzed ligand-free synthesis of rosuvastatin based novel indole derivatives as potential anticancer agents

Abstract

Rosuvastatin based novel indole derivatives designed as potential anti-cancer agents were synthesized via a newly developed ligand-free, simple, straightforward and inexpensive one-pot method. The methodology involved a Cu-catalyzed coupling-cyclization of a rosuvastatin based alkyne with o-iodoanilides in the presence of CuI and K₂CO₃ in PEG-400. Three of the synthesized compounds showed promising anti-proliferative activities against cancer cell lines and an increase of p21 mRNA expression and apoptotic effects in zebrafish embryos/larvae.