One‐Pot Synthesis of Coumarin–Indomethacin Hybrids as COX‐2 Targeting Probes for Cancer Imaging

Abstract Facile synthesis of 6‐ or 7‐substituted coumarin‐indomathacin hybrids (Coum‐IDM) has been developed for specific cyclooxygenase‐2 (COX‐2) binding along with their intrinsic fluorescent properties. A mild and rapid condensation/dehydrative cyclization of 2‐hydroxy benzaldehyde with activated indomethacin was carried out in one step under ultrasound irradiation. Coum‐IDM 4 was found to be the best of this series as it presented significant binding to COX‐2 and exhibited higher fluorescent intensity in cancer cells than in normal cells. Therefore, in the light of drug development tools, this new hybrid system could be a potential targeted probe for COX‐2‐overexpressed inflammation and cancer‐cell tracking.