1,8-naphthyridine derivatives having rigid ring structure display rich photophysical properties, and have broad application in recognizing metal ions, biomolecules as well as in supramolecular or coordination chemistry, some of them have been already used in clinical treatment. In this contribution, recent research developments of 1,8-naphthyridine derivatives, including their structures, spectroscopic properties and wide application in biological medicine field are introduced.