Synthesis, Biological Assay, and SAR of Potential Anticancer Lipophilic Fluoroquinolones (FQs) and Pyridoquinoxalines (PQs) Conjugated to Gold Nanoparticles for Synergistic and Proapoptogenic Cytotoxicity Drug Design and Targeted Delivery.

In a world where cancer continues to be a major health problem, the urgency continues to find new effective treatments. This work involved the synthesis of more than 10 anticancer fluoroquinolones (FQs) and pyridoquinoxaline (PQ) derivatives originating from FQs and studied their cytotoxicity, anti-adhesion, anti-invasion, and pro-apoptotic properties. Synthesis of the new compounds of the PQ series was carried out by reacting 1-cyclopropyl-6-fluoro-8-nitro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid with L-proline, 3 and 4-hydroxy proline derivatives (compounds 2a-2f), followed by reductive cyclization to yield compounds 3a-3f.