Imidazoquinolines are interesting heterocyclic systems. Different fusion sites between the imidazole five membered ring and quinoline generate different imidazoquinolines, at least nine distinct combinations can be identified for this scaffold. Interestingly, diverse biopharmaceutical applications and uses can also be delineated according to each specific imidazoquinoline. Pertinent to these facts, this book includes a purposeful survey covering the various biological, pharmaceutical and industrial applications in addition to the different synthetic approaches for the possible imidazoquinolines. More specifically, the 1H-imidazo[4, 5-c]quinoline nucleus is of a significant importance. Many members belonging to this specific nucleus are reported to possess anticancer, antimicrobial and immunomodifing properties. In an attempt to explore further applications for this specific nucleus, two imidazo[4, 5-c]quinoline-based projects were established and biologically screened.