One-Pot Synthesis of Coumarin-Indomethacin Hybrids as COX-2 Targeting Probes for Cancer Imaging.

One-Pot Synthesis of Coumarin-Indomethacin Hybrids as COX-2 Targeting Probes for Cancer Imaging. ChemMedChem. 2021 Feb 14;: Authors: Kamkaew A, Wet-Osot S, Pewklang T, Chansaenpak K, Chudapongse N, Lai RY 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-IDM4 was found to be the best of this series as it presented significant binding to COX-2 and exhibited higher fluorescent intensity in cancer cell compared to that in the normal cells.  Therefore, in the light of drug development tool, this new hybrid system could be a potential targeted probe for COX-2 over-expressed inflammation and cancer cells tracking. PMID: 33586347 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research